Proteins > Poly [ADP-ribose] polymerase 1
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Poly [ADP-ribose] polymerase 1
A poly [ADP-ribose] polymerase 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P09874]
Synonyms
PARP-1;
EC 2.4.2.30;
ADP-ribosyltransferase diphtheria toxin-like 1;
ARTD1;
DNA ADP-ribosyltransferase PARP1;
2.4.2.-;
NAD(+) ADP-ribosyltransferase 1;
ADPRT 1;
Poly[ADP-ribose] synthase 1;
Protein poly-ADP-ribosyltran
Research
Bioassay Publications (119)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 23 (19.33) | 29.6817 |
2010's | 65 (54.62) | 24.3611 |
2020's | 31 (26.05) | 2.80 |
Compounds (53)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
niacinamide | Homo sapiens (human) | IC50 | 187.0070 | 6 | 7 |
1,5-dihydroxyisoquinoline | Homo sapiens (human) | IC50 | 0.3293 | 2 | 3 |
3-aminobenzamide | Homo sapiens (human) | IC50 | 20.4915 | 14 | 16 |
3-aminobenzamide | Homo sapiens (human) | Ki | 3.5750 | 4 | 4 |
4-amino-1,8-naphthalimide | Homo sapiens (human) | IC50 | 0.0650 | 3 | 4 |
phenanthridone | Homo sapiens (human) | IC50 | 0.3445 | 7 | 8 |
5-aminoisoquinolinone | Homo sapiens (human) | IC50 | 1.2336 | 5 | 7 |
benzamide | Homo sapiens (human) | IC50 | 15.8000 | 3 | 3 |
pj-34 | Homo sapiens (human) | IC50 | 0.1096 | 13 | 17 |
1-hydroxyphthalazine | Homo sapiens (human) | IC50 | 12.0000 | 1 | 1 |
chlorthenoxazin | Homo sapiens (human) | IC50 | 8.5000 | 1 | 1 |
isocarbostyril | Homo sapiens (human) | IC50 | 3.5045 | 2 | 2 |
flavone | Homo sapiens (human) | IC50 | 1.3902 | 1 | 2 |
2,4(1h,3h)-quinazolinedione | Homo sapiens (human) | IC50 | 8.1000 | 1 | 1 |
4-hydroxybenzamide | Homo sapiens (human) | IC50 | 280.0000 | 1 | 1 |
naphthalimides | Homo sapiens (human) | IC50 | 1.4000 | 1 | 1 |
4-fluorobenzamide | Homo sapiens (human) | IC50 | 200.0000 | 1 | 1 |
5-iodo-6-amino-1,2-benzopyrone | Homo sapiens (human) | IC50 | 13.1470 | 1 | 2 |
alantolactone | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
4-aminobenzamide | Homo sapiens (human) | IC50 | 1,800.0000 | 1 | 1 |
4-Methoxybenzamide | Homo sapiens (human) | IC50 | 57.0000 | 1 | 1 |
3-methoxybenzamide | Homo sapiens (human) | IC50 | 17.0000 | 1 | 1 |
3',4'-dihydroxyflavone | Homo sapiens (human) | IC50 | 1.2795 | 1 | 2 |
3,4-dihydro-5-methyl-1(2h)-isoquinolinone | Homo sapiens (human) | IC50 | 0.2467 | 3 | 3 |
3,4-dihydro-5-methyl-1(2h)-isoquinolinone | Homo sapiens (human) | Ki | 0.0700 | 1 | 1 |
1-oxo-1,2,3,4-tetrahydroisoquinoline | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
cyclo(alanylalanyl) | Homo sapiens (human) | IC50 | 900.0000 | 1 | 1 |
N-[4-[[[4-(4-methoxyphenyl)-4-oxanyl]methylamino]-oxomethyl]phenyl]-2-furancarboxamide | Homo sapiens (human) | IC50 | 1.8000 | 1 | 1 |
ha 1100 | Homo sapiens (human) | IC50 | 27.0000 | 1 | 1 |
apigenin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
luteolin | Homo sapiens (human) | IC50 | 4.2329 | 1 | 2 |
amentoflavone | Homo sapiens (human) | IC50 | 0.1023 | 3 | 3 |
3',4',7-trihydroxyflavone | Homo sapiens (human) | IC50 | 7.5429 | 1 | 2 |
adenosine diphosphate (hydroxymethyl)pyrrolidinediol | Homo sapiens (human) | IC50 | 1,000.0000 | 1 | 1 |
ag 14361 | Homo sapiens (human) | Ki | 0.0058 | 1 | 1 |
gpi 6150 | Homo sapiens (human) | IC50 | 0.1345 | 1 | 2 |
rucaparib | Homo sapiens (human) | IC50 | 0.0659 | 16 | 19 |
rucaparib | Homo sapiens (human) | Ki | 0.0014 | 5 | 5 |
3,4-dihydro-5-(4-(1-piperidinyl)butoxy)-1(2h)-isoquinolinone | Homo sapiens (human) | IC50 | 3.2458 | 3 | 4 |
veliparib | Homo sapiens (human) | IC50 | 5.6074 | 20 | 24 |
veliparib | Homo sapiens (human) | Ki | 0.0046 | 4 | 4 |
olaparib | Homo sapiens (human) | IC50 | 0.1741 | 65 | 68 |
olaparib | Homo sapiens (human) | Ki | 0.0008 | 1 | 1 |
niraparib | Homo sapiens (human) | IC50 | 0.0032 | 2 | 2 |
niraparib | Homo sapiens (human) | IC50 | 0.0278 | 15 | 17 |
niraparib | Homo sapiens (human) | Ki | 0.0032 | 1 | 1 |
cep 26401 | Homo sapiens (human) | IC50 | 30.0000 | 1 | 1 |
iwr-1 endo | Homo sapiens (human) | IC50 | 55.6125 | 4 | 4 |
nms-p118 | Homo sapiens (human) | IC50 | 0.0595 | 2 | 2 |
g007-lk | Homo sapiens (human) | IC50 | 100.0000 | 2 | 2 |
nu 1025 | Homo sapiens (human) | Ki | 0.0500 | 2 | 2 |
2-methyl-4(3h)-quinazolinone | Homo sapiens (human) | IC50 | 3.4050 | 2 | 2 |
4-hydroxyquinazoline | Homo sapiens (human) | IC50 | 12.5284 | 4 | 5 |
1,4-Dihydrothieno[3,2-d]pyrimidin-4-one | Homo sapiens (human) | IC50 | 14.0000 | 1 | 1 |
xav939 | Homo sapiens (human) | IC50 | 2.9925 | 15 | 17 |
2-(4-methoxyphenyl)-1H-quinazolin-4-one | Homo sapiens (human) | IC50 | 1.0993 | 3 | 3 |
bmn 673 | Homo sapiens (human) | IC50 | 0.0023 | 9 | 9 |
bmn 673 | Homo sapiens (human) | Ki | 0.0010 | 3 | 3 |
me0328 | Homo sapiens (human) | IC50 | 4.2975 | 3 | 4 |
nvp-tnks656 | Homo sapiens (human) | IC50 | 19.0000 | 1 | 1 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
pj-34 | Homo sapiens (human) | EC50 | 0.0200 | 1 | 1 |
pj-34 | Homo sapiens (human) | Kd | 0.1100 | 1 | 1 |
rucaparib | Homo sapiens (human) | EC50 | 0.0108 | 2 | 2 |
rucaparib | Homo sapiens (human) | Kd | 0.0032 | 1 | 1 |
veliparib | Homo sapiens (human) | EC50 | 27.2350 | 6 | 6 |
veliparib | Homo sapiens (human) | Kd | 0.0023 | 2 | 2 |
olaparib | Homo sapiens (human) | EC50 | 2.6804 | 6 | 6 |
olaparib | Homo sapiens (human) | Kd | 1.3278 | 4 | 4 |
niraparib | Homo sapiens (human) | EC50 | 0.0240 | 2 | 2 |
niraparib | Homo sapiens (human) | EC50 | 7.8020 | 4 | 4 |
niraparib | Homo sapiens (human) | Kd | 0.0010 | 1 | 1 |
nms-p118 | Homo sapiens (human) | Kd | 0.0159 | 3 | 3 |
xav939 | Homo sapiens (human) | Kd | 0.6200 | 1 | 1 |
bmn 673 | Homo sapiens (human) | EC50 | 0.0027 | 3 | 3 |
bmn 673 | Homo sapiens (human) | Kd | 0.0011 | 1 | 1 |
Drugs with Other Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
niraparib | Homo sapiens (human) | EC90 | 0.2200 | 1 | 1 |
niraparib | Homo sapiens (human) | EC90 | 0.0450 | 1 | 1 |
niraparib | Homo sapiens (human) | IC90 | 0.0493 | 3 | 3 |
Design, synthesis and biological evaluation of pyridazino[3,4,5-de]quinazolin-3(2H)-one as a new class of PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 25, Issue:11, 2015
Identification of novel PARP-1 inhibitors: Drug design, synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 25, Issue:20, 2015
Design, synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 23, Issue:7, 2013
Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.Journal of medicinal chemistry, , Jun-24, Volume: 53, Issue:12, 2010
Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors.Molecular pharmacology, , Volume: 74, Issue:6, 2008
Design and synthesis of poly ADP-ribose polymerase-1 inhibitors. 2. Biological evaluation of aza-5[H]-phenanthridin-6-ones as potent, aqueous-soluble compounds for the treatment of ischemic injuries.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors.Molecular pharmacology, , Volume: 74, Issue:6, 2008
Modeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationship analysis.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
Medicinal chemistry approaches of poly ADP-Ribose polymerase 1 (PARP1) inhibitors as anticancer agents - A recent update.European journal of medicinal chemistry, , Mar-01, Volume: 165, 2019
Identification of low micromolar dual inhibitors for aldose reductase (ALR2) and poly (ADP-ribose) polymerase (PARP-1) using structure based design approach.Bioorganic & medicinal chemistry letters, , 06-01, Volume: 27, Issue:11, 2017
Design, synthesis and biological evaluation of pyridazino[3,4,5-de]quinazolin-3(2H)-one as a new class of PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 25, Issue:11, 2015
Identification of novel PARP-1 inhibitors: Drug design, synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 25, Issue:20, 2015
Design, synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 23, Issue:7, 2013
Synthesis and SAR optimization of quinazolin-4(3H)-ones as poly(ADP-ribose)polymerase-1 inhibitors.European journal of medicinal chemistry, , Volume: 50, 2012
Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 20, Issue:2, 2010
Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.Journal of medicinal chemistry, , Jun-24, Volume: 53, Issue:12, 2010
Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors.Molecular pharmacology, , Volume: 74, Issue:6, 2008
Discovery of potent and selective PARP-1 and PARP-2 inhibitors: SBDD analysis via a combination of X-ray structural study and homology modeling.Bioorganic & medicinal chemistry, , Mar-01, Volume: 14, Issue:5, 2006
Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone.Journal of medicinal chemistry, , Aug-11, Volume: 48, Issue:16, 2005
Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.Journal of medicinal chemistry, , Oct-21, Volume: 47, Issue:22, 2004
Potentiation of cytotoxic drug activity in human tumour cell lines, by amine-substituted 2-arylbenzimidazole-4-carboxamide PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , May-17, Volume: 14, Issue:10, 2004
Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase.Journal of medicinal chemistry, , Aug-12, Volume: 47, Issue:17, 2004
Modeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationship analysis.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase.Journal of medicinal chemistry, , Nov-02, Volume: 43, Issue:22, 2000
Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors.Molecular pharmacology, , Volume: 74, Issue:6, 2008
Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
Modeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationship analysis.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 24, Issue:12, 2014
Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.Journal of medicinal chemistry, , Jun-24, Volume: 53, Issue:12, 2010
Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors.Molecular pharmacology, , Volume: 74, Issue:6, 2008
Design and synthesis of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors. Part 3: In vitro evaluation of 1,3,4,5-tetrahydro-benzo[c][1,6]- and [c][1,7]-naphthyridin-6-ones.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 13, Issue:15, 2003
Design and synthesis of poly ADP-ribose polymerase-1 inhibitors. 2. Biological evaluation of aza-5[H]-phenanthridin-6-ones as potent, aqueous-soluble compounds for the treatment of ischemic injuries.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Synthesis of substituted 5[H]phenanthridin-6-ones as potent poly(ADP-ribose)polymerase-1 (PARP1) inhibitors.Bioorganic & medicinal chemistry letters, , Jul-09, Volume: 11, Issue:13, 2001
Modeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationship analysis.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
One-pot tandem Hurtley-retro-Claisen-cyclisation reactions in the synthesis of 3-substituted analogues of 5-aminoisoquinolin-1-one (5-AIQ), a water-soluble inhibitor of PARPs.Bioorganic & medicinal chemistry, , Sep-01, Volume: 21, Issue:17, 2013
5-Benzamidoisoquinolin-1-ones and 5-(ω-carboxyalkyl)isoquinolin-1-ones as isoform-selective inhibitors of poly(ADP-ribose) polymerase 2 (PARP-2).Journal of medicinal chemistry, , Apr-14, Volume: 54, Issue:7, 2011
Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors.Molecular pharmacology, , Volume: 74, Issue:6, 2008
Discovery and structure-activity relationships of modified salicylanilides as cell permeable inhibitors of poly(ADP-ribose) glycohydrolase (PARG).Journal of medicinal chemistry, , Aug-11, Volume: 54, Issue:15, 2011
Design and synthesis of poly ADP-ribose polymerase-1 inhibitors. 2. Biological evaluation of aza-5[H]-phenanthridin-6-ones as potent, aqueous-soluble compounds for the treatment of ischemic injuries.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Modeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationship analysis.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
From PARP1 to TNKS2 Inhibition: A Structure-Based Approach.ACS medicinal chemistry letters, , May-14, Volume: 11, Issue:5, 2020
Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors.Journal of medicinal chemistry, , 02-23, Volume: 60, Issue:4, 2017
Evaluation and Structural Basis for the Inhibition of Tankyrases by PARP Inhibitors.ACS medicinal chemistry letters, , Jan-09, Volume: 5, Issue:1, 2014
Synthesis, [¹⁸F] radiolabeling, and evaluation of poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors for in vivo imaging of PARP-1 using positron emission tomography.Bioorganic & medicinal chemistry, , Mar-01, Volume: 22, Issue:5, 2014
Synthesis and SAR optimization of quinazolin-4(3H)-ones as poly(ADP-ribose)polymerase-1 inhibitors.European journal of medicinal chemistry, , Volume: 50, 2012
Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.Journal of medicinal chemistry, , Jun-24, Volume: 53, Issue:12, 2010
Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3.Journal of medicinal chemistry, , May-14, Volume: 52, Issue:9, 2009
Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.Journal of medicinal chemistry, , Feb-12, Volume: 52, Issue:3, 2009
Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors.Molecular pharmacology, , Volume: 74, Issue:6, 2008
Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , Oct-01, Volume: 15, Issue:19, 2005
Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.Journal of medicinal chemistry, , Jun-24, Volume: 53, Issue:12, 2010
Modeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationship analysis.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
Medicinal chemistry approaches of poly ADP-Ribose polymerase 1 (PARP1) inhibitors as anticancer agents - A recent update.European journal of medicinal chemistry, , Mar-01, Volume: 165, 2019
Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 18, Issue:18, 2008
Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.Journal of medicinal chemistry, , Oct-21, Volume: 47, Issue:22, 2004
Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Structure-based design, synthesis, and evaluation of inhibitors with high selectivity for PARP-1 over PARP-2.European journal of medicinal chemistry, , Jan-05, Volume: 227, 2022
Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Small-molecule inhibitors of breast cancer-related targets: Potential therapeutic agents for breast cancer.European journal of medicinal chemistry, , Jan-15, Volume: 210, 2021
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Discovery of isoquinolinone and naphthyridinone-based inhibitors of poly(ADP-ribose) polymerase-1 (PARP1) as anticancer agents: Structure activity relationship and preclinical characterization.Bioorganic & medicinal chemistry, , 12-15, Volume: 28, Issue:24, 2020
[no title available]Journal of medicinal chemistry, , 06-13, Volume: 62, Issue:11, 2019
Medicinal chemistry approaches of poly ADP-Ribose polymerase 1 (PARP1) inhibitors as anticancer agents - A recent update.European journal of medicinal chemistry, , Mar-01, Volume: 165, 2019
Design, synthesis and anticancer activities evaluation of novel 5H-dibenzo[b,e]azepine-6,11-dione derivatives containing 1,3,4-oxadiazole units.Bioorganic & medicinal chemistry letters, , 03-01, Volume: 28, Issue:5, 2018
Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors.Journal of medicinal chemistry, , 02-23, Volume: 60, Issue:4, 2017
Proteome-wide Profiling of Clinical PARP Inhibitors Reveals Compound-Specific Secondary Targets.Cell chemical biology, , Dec-22, Volume: 23, Issue:12, 2016
Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 26, Issue:16, 2016
Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) PolymerJournal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 2016
Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination.Journal of medicinal chemistry, , Apr-23, Volume: 58, Issue:8, 2015
Identification of novel PARP-1 inhibitors: Drug design, synthesis and biological evaluation.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 25, Issue:20, 2015
Evaluation and Structural Basis for the Inhibition of Tankyrases by PARP Inhibitors.ACS medicinal chemistry letters, , Jan-09, Volume: 5, Issue:1, 2014
Synthesis and biological evaluation of isoindoloisoquinolinone, pyroloisoquinolinone and benzoquinazolinone derivatives as poly(ADP-ribose) polymerase-1 inhibitors.Bioorganic & medicinal chemistry, , Feb-01, Volume: 23, Issue:3, 2015
Synthesis of isoquinolinone-based tetracycles as poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors.Bioorganic & medicinal chemistry, , Nov-01, Volume: 17, Issue:21, 2009
Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors.Molecular pharmacology, , Volume: 74, Issue:6, 2008
Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
[no title available]Journal of medicinal chemistry, , 06-13, Volume: 62, Issue:11, 2019
Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors.European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors.Journal of medicinal chemistry, , 02-23, Volume: 60, Issue:4, 2017
Discovery of 2-substituted 1H-benzo[d]immidazole-4-carboxamide derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors with in vivo anti-tumor activity.European journal of medicinal chemistry, , May-26, Volume: 132, 2017
Proteome-wide Profiling of Clinical PARP Inhibitors Reveals Compound-Specific Secondary Targets.Cell chemical biology, , Dec-22, Volume: 23, Issue:12, 2016
Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 26, Issue:16, 2016
Novel tricyclic poly (ADP-ribose) polymerase-1/2 inhibitors with potent anticancer chemopotentiating activity: Design, synthesis and biological evaluation.Bioorganic & medicinal chemistry, , 10-01, Volume: 24, Issue:19, 2016
Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) PolymerJournal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 2016
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.Journal of medicinal chemistry, , Sep-10, Volume: 58, Issue:17, 2015
Benzimidazole derivatives as potential dual inhibitors for PARP-1 and DHODH.Bioorganic & medicinal chemistry, , Aug-01, Volume: 23, Issue:15, 2015
Discovery and structure-activity relationship of novel 2,3-dihydrobenzofuran-7-carboxamide and 2,3-dihydrobenzofuran-3(2H)-one-7-carboxamide derivatives as poly(ADP-ribose)polymerase-1 inhibitors.Journal of medicinal chemistry, , Jul-10, Volume: 57, Issue:13, 2014
7-Azaindole-1-carboxamides as a new class of PARP-1 inhibitors.Bioorganic & medicinal chemistry, , Feb-01, Volume: 22, Issue:3, 2014
Novel PARP-1 inhibitors based on a 2-propanoyl-3H-quinazolin-4-one scaffold.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose)polymerase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 23, Issue:16, 2013
Design, synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , Apr-01, Volume: 23, Issue:7, 2013
Synthesis and evaluation of a new generation of orally efficacious benzimidazole-based poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors as anticancer agents.Journal of medicinal chemistry, , Nov-12, Volume: 52, Issue:21, 2009
Discovery of the Poly(ADP-ribose) polymerase (PARP) inhibitor 2-[(R)-2-methylpyrrolidin-2-yl]-1H-benzimidazole-4-carboxamide (ABT-888) for the treatment of cancer.Journal of medicinal chemistry, , Jan-22, Volume: 52, Issue:2, 2009
Dual-target inhibitors of poly (ADP-ribose) polymerase-1 for cancer therapy: Advances, challenges, and opportunities.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Selective degradation of PARP2 by PROTACs via recruiting DCAF16 for triple-negative breast cancer.European journal of medicinal chemistry, , Jun-05, Volume: 236, 2022
Design, synthesis and mechanism studies of novel dual PARP1/BRD4 inhibitors against pancreatic cancer.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Targeting Enhancer of Zeste Homolog 2 for the Treatment of Hematological Malignancies and Solid Tumors: Candidate Structure-Activity Relationships Insights and Evolution Prospects.Journal of medicinal chemistry, , 05-26, Volume: 65, Issue:10, 2022
Synthesis and in vitro biological evaluation of 3-ethyl-1,5-naphthyridin-2(1H)-one derivatives as potent PARP-1 selective inhibitors and PARP-1 DNA trappers.Bioorganic & medicinal chemistry letters, , 12-15, Volume: 78, 2022
Rational design, synthesis and biological evaluation of dual PARP-1/2 and TNKS1/2 inhibitors for cancer therapy.European journal of medicinal chemistry, , Jul-05, Volume: 237, 2022
Design, synthesis and pharmacological evaluation of new PARP1 inhibitors by merging pharmacophores of olaparib and the natural product alantolactone.European journal of medicinal chemistry, , Oct-05, Volume: 240, 2022
Synthesis and biological evaluation of a tumor-selective degrader of PARP1.Bioorganic & medicinal chemistry, , 09-01, Volume: 69, 2022
Design, synthesis and antitumor activity study of PARP-1/HDAC dual targeting inhibitors.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 71, 2022
[no title available]Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
[no title available]Journal of medicinal chemistry, , 12-09, Volume: 64, Issue:23, 2021
Design, synthesis and biological evaluation of novel molecules as potent PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , 09-01, Volume: 47, 2021
Discovery of novel and potent PARP/PI3K dual inhibitors for the treatment of cancer.European journal of medicinal chemistry, , May-05, Volume: 217, 2021
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Identification of 2-substituted pyrrolo[1,2-b]pyridazine derivatives as new PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , 01-01, Volume: 31, 2021
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
Pyridazine as a privileged structure: An updated review on anticancer activity of pyridazine containing bioactive molecules.European journal of medicinal chemistry, , Jan-01, Volume: 209, 2021
Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP.Journal of medicinal chemistry, , 06-10, Volume: 64, Issue:11, 2021
Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Discovery of SK-575 as a Highly Potent and Efficacious Proteolysis-Targeting Chimera Degrader of PARP1 for Treating Cancers.Journal of medicinal chemistry, , 10-08, Volume: 63, Issue:19, 2020
Discovery of isoquinolinone and naphthyridinone-based inhibitors of poly(ADP-ribose) polymerase-1 (PARP1) as anticancer agents: Structure activity relationship and preclinical characterization.Bioorganic & medicinal chemistry, , 12-15, Volume: 28, Issue:24, 2020
[no title available]Bioorganic & medicinal chemistry letters, , 04-15, Volume: 30, Issue:8, 2020
[no title available]Journal of medicinal chemistry, , 01-09, Volume: 63, Issue:1, 2020
Discovery of naphthacemycins as a novel class of PARP1 inhibitors.Bioorganic & medicinal chemistry letters, , 08-01, Volume: 29, Issue:15, 2019
Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review.Bioorganic & medicinal chemistry, , 09-15, Volume: 27, Issue:18, 2019
Discovery of novel functionalized 1,2,4-triazoles as PARP-1 inhibitors in breast cancer: Design, synthesis and antitumor activity evaluation.European journal of medicinal chemistry, , Nov-15, Volume: 182, 2019
[no title available]Journal of medicinal chemistry, , 06-13, Volume: 62, Issue:11, 2019
Controlling cellular distribution of drugs with permeability modifying moieties.MedChemComm, , Jun-01, Volume: 10, Issue:6, 2019
Discovery of Novel Bromophenol-Thiosemicarbazone Hybrids as Potent Selective Inhibitors of Poly(ADP-ribose) Polymerase-1 (PARP-1) for Use in Cancer.Journal of medicinal chemistry, , 03-28, Volume: 62, Issue:6, 2019
Design and synthesis of 2-(4,5,6,7-tetrahydrothienopyridin-2-yl)-benzoimidazole carboxamides as novel orally efficacious Poly(ADP-ribose)polymerase (PARP) inhibitors.European journal of medicinal chemistry, , Feb-10, Volume: 145, 2018
Examination of Diazaspiro Cores as Piperazine Bioisosteres in the Olaparib Framework Shows Reduced DNA Damage and Cytotoxicity.Journal of medicinal chemistry, , 06-28, Volume: 61, Issue:12, 2018
Olaparib hydroxamic acid derivatives as dual PARP and HDAC inhibitors for cancer therapy.Bioorganic & medicinal chemistry, , 08-01, Volume: 25, Issue:15, 2017
Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors.Journal of medicinal chemistry, , 02-23, Volume: 60, Issue:4, 2017
Discovery of novel quinazoline-2,4(1H,3H)-dione derivatives as potent PARP-2 selective inhibitors.Bioorganic & medicinal chemistry, , 08-01, Volume: 25, Issue:15, 2017
Design, synthesis and biological evaluation of 4-amidobenzimidazole acridine derivatives as dual PARP and Topo inhibitors for cancer therapy.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
Discovery, mechanism and metabolism studies of 2,3-difluorophenyl-linker-containing PARP1 inhibitors with enhanced in vivo efficacy for cancer therapy.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
Discovery of 2-substituted 1H-benzo[d]immidazole-4-carboxamide derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors with in vivo anti-tumor activity.European journal of medicinal chemistry, , May-26, Volume: 132, 2017
Proteome-wide Profiling of Clinical PARP Inhibitors Reveals Compound-Specific Secondary Targets.Cell chemical biology, , Dec-22, Volume: 23, Issue:12, 2016
Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 26, Issue:16, 2016
Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) PolymerJournal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 2016
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.Journal of medicinal chemistry, , Sep-10, Volume: 58, Issue:17, 2015
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 25, Issue:24, 2015
Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination.Journal of medicinal chemistry, , Apr-23, Volume: 58, Issue:8, 2015
Synthesis and Evaluation of a Radioiodinated Tracer with Specificity for Poly(ADP-ribose) Polymerase-1 (PARP-1) in Vivo.Journal of medicinal chemistry, , Nov-12, Volume: 58, Issue:21, 2015
Synthesis and biological evaluation of substituted 4-(thiophen-2-ylmethyl)-2H-phthalazin-1-ones as potent PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 24, Issue:16, 2014
Nitric oxide (NO) releasing poly ADP-ribose polymerase 1 (PARP-1) inhibitors targeted to glutathione S-transferase P1-overexpressing cancer cells.Journal of medicinal chemistry, , Mar-27, Volume: 57, Issue:6, 2014
Discovery and structure-activity relationship of novel 2,3-dihydrobenzofuran-7-carboxamide and 2,3-dihydrobenzofuran-3(2H)-one-7-carboxamide derivatives as poly(ADP-ribose)polymerase-1 inhibitors.Journal of medicinal chemistry, , Jul-10, Volume: 57, Issue:13, 2014
7-Azaindole-1-carboxamides as a new class of PARP-1 inhibitors.Bioorganic & medicinal chemistry, , Feb-01, Volume: 22, Issue:3, 2014
Novel PARP-1 inhibitors based on a 2-propanoyl-3H-quinazolin-4-one scaffold.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 24, Issue:12, 2014
Design, synthesis, and biological evaluation of a series of benzo[de][1,7]naphthyridin-7(8H)-ones bearing a functionalized longer chain appendage as novel PARP1 inhibitors.Journal of medicinal chemistry, , Apr-11, Volume: 56, Issue:7, 2013
Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose)polymerase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 23, Issue:16, 2013
4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1.Journal of medicinal chemistry, , Oct-23, Volume: 51, Issue:20, 2008
[no title available],
Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination.Journal of medicinal chemistry, , Apr-23, Volume: 58, Issue:8, 2015
Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.Journal of medicinal chemistry, , Nov-26, Volume: 52, Issue:22, 2009
Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
Medicinal chemistry approaches of poly ADP-Ribose polymerase 1 (PARP1) inhibitors as anticancer agents - A recent update.European journal of medicinal chemistry, , Mar-01, Volume: 165, 2019
Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors.Journal of medicinal chemistry, , 02-23, Volume: 60, Issue:4, 2017
Proteome-wide Profiling of Clinical PARP Inhibitors Reveals Compound-Specific Secondary Targets.Cell chemical biology, , Dec-22, Volume: 23, Issue:12, 2016
Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 26, Issue:16, 2016
Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) PolymerJournal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 2016
Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination.Journal of medicinal chemistry, , Apr-23, Volume: 58, Issue:8, 2015
7-Azaindole-1-carboxamides as a new class of PARP-1 inhibitors.Bioorganic & medicinal chemistry, , Feb-01, Volume: 22, Issue:3, 2014
Novel PARP-1 inhibitors based on a 2-propanoyl-3H-quinazolin-4-one scaffold.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 24, Issue:2, 2014
Discovery of novel benzo[b][1,4]oxazin-3(4H)-ones as poly(ADP-ribose)polymerase inhibitors.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 23, Issue:16, 2013
Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors.Journal of medicinal chemistry, , Nov-26, Volume: 52, Issue:22, 2009
Small-Molecule Inhibitors of Tankyrases as Prospective Therapeutics for Cancer.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
Discovery of novel, induced-pocket binding oxazolidinones as potent, selective, and orally bioavailable tankyrase inhibitors.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Structural basis of selective inhibition of human tankyrases.Journal of medicinal chemistry, , Feb-09, Volume: 55, Issue:3, 2012
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
[no title available]Journal of medicinal chemistry, , 08-26, Volume: 64, Issue:16, 2021
Discovery of 2-[1-(4,4-Difluorocyclohexyl)piperidin-4-yl]-6-fluoro-3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide (NMS-P118): A Potent, Orally Available, and Highly Selective PARP-1 Inhibitor for Cancer Therapy.Journal of medicinal chemistry, , Sep-10, Volume: 58, Issue:17, 2015
Design and Discovery of an Orally Efficacious Spiroindolinone-Based Tankyrase Inhibitor for the Treatment of Colon Cancer.Journal of medicinal chemistry, , 04-23, Volume: 63, Issue:8, 2020
Discovery of Novel Spiroindoline Derivatives as Selective Tankyrase Inhibitors.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Medicinal chemistry approaches of poly ADP-Ribose polymerase 1 (PARP1) inhibitors as anticancer agents - A recent update.European journal of medicinal chemistry, , Mar-01, Volume: 165, 2019
Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.Journal of medicinal chemistry, , Oct-21, Volume: 47, Issue:22, 2004
Synthesis and SAR optimization of quinazolin-4(3H)-ones as poly(ADP-ribose)polymerase-1 inhibitors.European journal of medicinal chemistry, , Volume: 50, 2012
Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.Journal of medicinal chemistry, , Jun-24, Volume: 53, Issue:12, 2010
Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors.Molecular pharmacology, , Volume: 74, Issue:6, 2008
Modeling of poly(ADP-ribose)polymerase (PARP) inhibitors. Docking of ligands and quantitative structure-activity relationship analysis.Journal of medicinal chemistry, , Nov-08, Volume: 44, Issue:23, 2001
Small-Molecule Inhibitors of Tankyrases as Prospective Therapeutics for Cancer.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
Discovery of Novel Spiroindoline Derivatives as Selective Tankyrase Inhibitors.Journal of medicinal chemistry, , 04-11, Volume: 62, Issue:7, 2019
Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors.Journal of medicinal chemistry, , 02-23, Volume: 60, Issue:4, 2017
Structure-activity relationships of 2-arylquinazolin-4-ones as highly selective and potent inhibitors of the tankyrases.European journal of medicinal chemistry, , Aug-08, Volume: 118, 2016
Design and Discovery of 2-Arylquinazolin-4-ones as Potent and Selective Inhibitors of Tankyrases.ACS medicinal chemistry letters, , Dec-12, Volume: 4, Issue:12, 2013
Structure-efficiency relationship of [1,2,4]triazol-3-ylamines as novel nicotinamide isosteres that inhibit tankyrases.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Fragment-based ligand design of novel potent inhibitors of tankyrases.Journal of medicinal chemistry, , Jun-13, Volume: 56, Issue:11, 2013
Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket.Journal of medicinal chemistry, , Feb-14, Volume: 56, Issue:3, 2013
Structural basis of selective inhibition of human tankyrases.Journal of medicinal chemistry, , Feb-09, Volume: 55, Issue:3, 2012
[1,2,4]triazol-3-ylsulfanylmethyl)-3-phenyl-[1,2,4]oxadiazoles: antagonists of the Wnt pathway that inhibit tankyrases 1 and 2 via novel adenosine pocket binding.Journal of medicinal chemistry, , Feb-09, Volume: 55, Issue:3, 2012
Structural basis for the interaction between tankyrase-2 and a potent Wnt-signaling inhibitor.Journal of medicinal chemistry, , Jul-22, Volume: 53, Issue:14, 2010
Small-Molecule Inhibitors of Tankyrases as Prospective Therapeutics for Cancer.Journal of medicinal chemistry, , 04-14, Volume: 65, Issue:7, 2022
Discovery and Optimization of 2-Arylquinazolin-4-ones into a Potent and Selective Tankyrase Inhibitor Modulating Wnt Pathway Activity.Journal of medicinal chemistry, , 09-12, Volume: 62, Issue:17, 2019
Structure-activity relationships of 2-arylquinazolin-4-ones as highly selective and potent inhibitors of the tankyrases.European journal of medicinal chemistry, , Aug-08, Volume: 118, 2016
Discovery of 4-Hydroxyquinazoline Derivatives as Small Molecular BET/PARP1 Inhibitors That Induce Defective Homologous Recombination and Lead to Synthetic Lethality for Triple-Negative Breast Cancer Therapy.Journal of medicinal chemistry, , 05-12, Volume: 65, Issue:9, 2022
Recent advances in DDR (DNA damage response) inhibitors for cancer therapy.European journal of medicinal chemistry, , Feb-15, Volume: 230, 2022
Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development.Journal of medicinal chemistry, , 12-24, Volume: 63, Issue:24, 2020
Discovery of isoquinolinone and naphthyridinone-based inhibitors of poly(ADP-ribose) polymerase-1 (PARP1) as anticancer agents: Structure activity relationship and preclinical characterization.Bioorganic & medicinal chemistry, , 12-15, Volume: 28, Issue:24, 2020
Medicinal chemistry approaches of poly ADP-Ribose polymerase 1 (PARP1) inhibitors as anticancer agents - A recent update.European journal of medicinal chemistry, , Mar-01, Volume: 165, 2019
Discovery, mechanism and metabolism studies of 2,3-difluorophenyl-linker-containing PARP1 inhibitors with enhanced in vivo efficacy for cancer therapy.European journal of medicinal chemistry, , Sep-29, Volume: 138, 2017
Design, synthesis and biological evaluation of novel 5-fluoro-1H-benzimidazole-4-carboxamide derivatives as potent PARP-1 inhibitors.Bioorganic & medicinal chemistry letters, , 08-15, Volume: 26, Issue:16, 2016
Discovery and Characterization of (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly(ADP-ribose) PolymerJournal of medicinal chemistry, , Jan-14, Volume: 59, Issue:1, 2016
Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination.Journal of medicinal chemistry, , Apr-23, Volume: 58, Issue:8, 2015
Chemical probes to study ADP-ribosylation: synthesis and biochemical evaluation of inhibitors of the human ADP-ribosyltransferase ARTD3/PARP3.Journal of medicinal chemistry, , Dec-12, Volume: 56, Issue:23, 2013
PARP inhibitor with selectivity toward ADP-ribosyltransferase ARTD3/PARP3.ACS chemical biology, , Aug-16, Volume: 8, Issue:8, 2013
Enables
This protein enables 30 target(s):
Target | Category | Definition |
DNA binding | molecular function | Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw] |
chromatin binding | molecular function | Binding to chromatin, the network of fibers of DNA, protein, and sometimes RNA, that make up the chromosomes of the eukaryotic nucleus during interphase. [GOC:jl, ISBN:0198506732, PMID:20404130] |
damaged DNA binding | molecular function | Binding to damaged DNA. [GOC:jl] |
RNA binding | molecular function | Binding to an RNA molecule or a portion thereof. [GOC:jl, GOC:mah] |
NAD+ ADP-ribosyltransferase activity | molecular function | Catalysis of the reaction: NAD+ + (ADP-D-ribosyl)(n)-acceptor = nicotinamide + (ADP-D-ribosyl)(n+1)-acceptor. [EC:2.4.2.30] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
nucleotidyltransferase activity | molecular function | Catalysis of the transfer of a nucleotidyl group to a reactant. [ISBN:0198506732] |
enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
protein kinase binding | molecular function | Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl] |
nuclear estrogen receptor binding | molecular function | Binding to a nuclear estrogen receptor. [GOC:ai] |
nucleosome binding | molecular function | Binding to a nucleosome, a complex comprised of DNA wound around a multisubunit core and associated proteins, which forms the primary packing unit of DNA into higher order structures. [GOC:mah] |
ubiquitin protein ligase binding | molecular function | Binding to a ubiquitin protein ligase enzyme, any of the E3 proteins. [GOC:vp] |
identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
protein homodimerization activity | molecular function | Binding to an identical protein to form a homodimer. [GOC:jl] |
histone deacetylase binding | molecular function | Binding to histone deacetylase. [GOC:jl] |
NAD binding | molecular function | Binding to nicotinamide adenine dinucleotide, a coenzyme involved in many redox and biosynthetic reactions; binding may be to either the oxidized form, NAD+, or the reduced form, NADH. [GOC:ai] |
RNA polymerase II-specific DNA-binding transcription factor binding | molecular function | Binding to a sequence-specific DNA binding RNA polymerase II transcription factor, any of the factors that interact selectively and non-covalently with a specific DNA sequence in order to modulate transcription. [GOC:dph, GOC:vw] |
R-SMAD binding | molecular function | Binding to a receptor-regulated SMAD signaling protein. [GOC:BHF, GOC:vk, PMID:19114992] |
NAD DNA ADP-ribosyltransferase activity | molecular function | Catalysis of the transfer of the ADP-ribose group of NAD+ to a residue in double-stranded DNA. [PMID:27471034, PMID:29361132, PMID:29520010] |
transcription regulator activator activity | molecular function | A molecular function regulator that increases the activity of a transcription regulator via direct binding and/or post-translational modification. [PMID:9597751] |
NAD+-protein-serine ADP-ribosyltransferase activity | molecular function | Catalysis of the reaction: L-seryl-[protein] + NAD+ = H+ + nicotinamide + O-(ADP-D-ribosyl)-L-seryl-[protein]. [PMID:32028527, PMID:33186521, RHEA:58232] |
NAD+- protein-aspartate ADP-ribosyltransferase activity | molecular function | Catalysis of the reaction: L-aspartyl-[protein] + NAD+ = 4-O-(ADP-D-ribosyl)-L-aspartyl-[protein] + nicotinamide. [PMID:19764761, PMID:25043379, RHEA:54424] |
NAD+-protein-glutamate ADP-ribosyltransferase activity | molecular function | Catalysis of the reaction: L-glutamyl-[protein] + NAD+ = 5-O-(ADP-D-ribosyl)-L-glutamyl-[protein] + nicotinamide. [PMID:19764761, PMID:25043379, RHEA:58224] |
NAD+-protein-tyrosine ADP-ribosyltransferase activity | molecular function | Catalysis of the reaction: L-tyrosyl-[protein] + NAD+ = H+ + nicotinamide + O-(ADP-D-ribosyl)-L-tyrosyl-[protein]. [PMID:29954836, PMID:30257210, RHEA:58236] |
NAD+-protein-histidine ADP-ribosyltransferase activity | molecular function | Catalysis of the reaction: L-histidyl-[protein] + NAD+ = H+ + Nt-(ADP-D-ribosyl)-L-histidyl-[protein] + nicotinamide. [PMID:35393539] |
NAD+-histone H2BS6 serine ADP-ribosyltransferase activity | molecular function | Catalysis of the transfer of ADP-ribose groups to the serine-6 or an equivalent residue of the N-terminal tail of histone H2B. [PMID:34874266] |
NAD+-histone H3S10 serine ADP-ribosyltransferase activity | molecular function | Catalysis of the transfer of ADP-ribose groups to the serine-10 or an equivalent residue of the N-terminal tail of histone H3. [PMID:34874266] |
NAD+-histone H2BE35 glutamate ADP-ribosyltransferase activity | molecular function | Catalysis of the transfer of ADP-ribose groups to the glutamate-35 residue of the N-terminal tail of histone H2B (or an equivalent residue). [PMID:32822587] |
NAD+-protein ADP-ribosyltransferase activity | molecular function | Catalysis of the reaction: amino acyl-[protein] + NAD+ = H+ + (ADP-D-ribosyl)-amino acyl-[protein] + nicotinamide. [PMID:1899243] |
Located In
This protein is located in 10 target(s):
Target | Category | Definition |
chromosome, telomeric region | cellular component | The end of a linear chromosome, required for the integrity and maintenance of the end. A chromosome telomere usually includes a region of telomerase-encoded repeats the length of which rarely exceeds 20 bp each and that permits the formation of a telomeric loop (T-loop). The telomeric repeat region is usually preceded by a sub-telomeric region that is gene-poor but rich in repetitive elements. Some telomeres only consist of the latter part (for eg. D. melanogaster telomeres). [GOC:elh] |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
nuclear envelope | cellular component | The double lipid bilayer enclosing the nucleus and separating its contents from the rest of the cytoplasm; includes the intermembrane space, a gap of width 20-40 nm (also called the perinuclear space). [ISBN:0198547684] |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
nucleolus | cellular component | A small, dense body one or more of which are present in the nucleus of eukaryotic cells. It is rich in RNA and protein, is not bounded by a limiting membrane, and is not seen during mitosis. Its prime function is the transcription of the nucleolar DNA into 45S ribosomal-precursor RNA, the processing of this RNA into 5.8S, 18S, and 28S components of ribosomal RNA, and the association of these components with 5S RNA and proteins synthesized outside the nucleolus. This association results in the formation of ribonucleoprotein precursors; these pass into the cytoplasm and mature into the 40S and 60S subunits of the ribosome. [ISBN:0198506732] |
mitochondrion | cellular component | A semiautonomous, self replicating organelle that occurs in varying numbers, shapes, and sizes in the cytoplasm of virtually all eukaryotic cells. It is notably the site of tissue respiration. [GOC:giardia, ISBN:0198506732] |
membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
nuclear body | cellular component | Extra-nucleolar nuclear domains usually visualized by confocal microscopy and fluorescent antibodies to specific proteins. [GOC:ma, PMID:10330182] |
site of double-strand break | cellular component | A region of a chromosome at which a DNA double-strand break has occurred. DNA damage signaling and repair proteins accumulate at the lesion to respond to the damage and repair the DNA to form a continuous DNA helix. [GOC:bf, GOC:mah, GOC:vw, PMID:20096808, PMID:21035408] |
site of DNA damage | cellular component | A region of a chromosome at which DNA damage has occurred. DNA damage signaling and repair proteins accumulate at the lesion to respond to the damage and repair the DNA to form a continuous DNA helix. [GOC:pg] |
Active In
This protein is active in 6 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
site of double-strand break | cellular component | A region of a chromosome at which a DNA double-strand break has occurred. DNA damage signaling and repair proteins accumulate at the lesion to respond to the damage and repair the DNA to form a continuous DNA helix. [GOC:bf, GOC:mah, GOC:vw, PMID:20096808, PMID:21035408] |
nuclear replication fork | cellular component | The Y-shaped region of a nuclear replicating DNA molecule, resulting from the separation of the DNA strands and in which the synthesis of new strands takes place. Also includes associated protein complexes. [GOC:jl, GOC:mtg_sensu] |
site of DNA damage | cellular component | A region of a chromosome at which DNA damage has occurred. DNA damage signaling and repair proteins accumulate at the lesion to respond to the damage and repair the DNA to form a continuous DNA helix. [GOC:pg] |
nucleolus | cellular component | A small, dense body one or more of which are present in the nucleus of eukaryotic cells. It is rich in RNA and protein, is not bounded by a limiting membrane, and is not seen during mitosis. Its prime function is the transcription of the nucleolar DNA into 45S ribosomal-precursor RNA, the processing of this RNA into 5.8S, 18S, and 28S components of ribosomal RNA, and the association of these components with 5S RNA and proteins synthesized outside the nucleolus. This association results in the formation of ribonucleoprotein precursors; these pass into the cytoplasm and mature into the 40S and 60S subunits of the ribosome. [ISBN:0198506732] |
Part Of
This protein is part of 4 target(s):
Target | Category | Definition |
chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
transcription regulator complex | cellular component | A protein complex that is capable of associating with DNA by direct binding, or via other DNA-binding proteins or complexes, and regulating transcription. [GOC:jl] |
protein-containing complex | cellular component | A stable assembly of two or more macromolecules, i.e. proteins, nucleic acids, carbohydrates or lipids, in which at least one component is a protein and the constituent parts function together. [GOC:dos, GOC:mah] |
protein-DNA complex | cellular component | A macromolecular complex containing both protein and DNA molecules. [GOC:mah] |
Involved In
This protein is involved in 50 target(s):
Target | Category | Definition |
negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
telomere maintenance | biological process | Any process that contributes to the maintenance of proper telomeric length and structure by affecting and monitoring the activity of telomeric proteins, the length of telomeric DNA and the replication and repair of the DNA. These processes includes those that shorten, lengthen, replicate and repair the telomeric DNA sequences. [GOC:BHF, GOC:BHF_telomere, GOC:elh, GOC:rl, PMID:11092831] |
DNA repair | biological process | The process of restoring DNA after damage. Genomes are subject to damage by chemical and physical agents in the environment (e.g. UV and ionizing radiations, chemical mutagens, fungal and bacterial toxins, etc.) and by free radicals or alkylating agents endogenously generated in metabolism. DNA is also damaged because of errors during its replication. A variety of different DNA repair pathways have been reported that include direct reversal, base excision repair, nucleotide excision repair, photoreactivation, bypass, double-strand break repair pathway, and mismatch repair pathway. [PMID:11563486] |
double-strand break repair | biological process | The repair of double-strand breaks in DNA via homologous and nonhomologous mechanisms to reform a continuous DNA helix. [GOC:elh] |
transcription by RNA polymerase II | biological process | The synthesis of RNA from a DNA template by RNA polymerase II (RNAP II), originating at an RNA polymerase II promoter. Includes transcription of messenger RNA (mRNA) and certain small nuclear RNAs (snRNAs). [GOC:jl, GOC:txnOH, ISBN:0321000382] |
apoptotic process | biological process | A programmed cell death process which begins when a cell receives an internal (e.g. DNA damage) or external signal (e.g. an extracellular death ligand), and proceeds through a series of biochemical events (signaling pathway phase) which trigger an execution phase. The execution phase is the last step of an apoptotic process, and is typically characterized by rounding-up of the cell, retraction of pseudopodes, reduction of cellular volume (pyknosis), chromatin condensation, nuclear fragmentation (karyorrhexis), plasma membrane blebbing and fragmentation of the cell into apoptotic bodies. When the execution phase is completed, the cell has died. [GOC:cjm, GOC:dhl, GOC:ecd, GOC:go_curators, GOC:mtg_apoptosis, GOC:tb, ISBN:0198506732, PMID:18846107, PMID:21494263] |
DNA damage response | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating damage to its DNA from environmental insults or errors during metabolism. [GOC:go_curators] |
transforming growth factor beta receptor signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a transforming growth factor beta receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:BHF, GOC:mah, GOC:signaling] |
response to gamma radiation | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a gamma radiation stimulus. Gamma radiation is a form of electromagnetic radiation (EMR) or light emission of a specific frequency produced from sub-atomic particle interaction, such as electron-positron annihilation and radioactive decay. Gamma rays are generally characterized as EMR having the highest frequency and energy, and also the shortest wavelength, within the electromagnetic radiation spectrum. [GOC:tair_curators] |
positive regulation of cardiac muscle hypertrophy | biological process | Any process that increases the rate, frequency or extent of the enlargement or overgrowth of all or part of the heart due to an increase in size (not length) of individual cardiac muscle fibers, without cell division. [GOC:BHF, GOC:dph, GOC:tb] |
carbohydrate biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of carbohydrates, any of a group of organic compounds based of the general formula Cx(H2O)y. [ISBN:0198506732] |
protein autoprocessing | biological process | Processing which a protein carries out itself. This involves actions such as the autolytic removal of residues to generate the mature form of the protein. [GOC:ai, PMID:9335337] |
signal transduction involved in regulation of gene expression | biological process | Any process that modulates the frequency, rate or extent of gene expression as a consequence of a process in which a signal is released and/or conveyed from one location to another. [GOC:mtg_signal] |
macrophage differentiation | biological process | The process in which a relatively unspecialized monocyte acquires the specialized features of a macrophage. [GOC:add, ISBN:0781735149] |
DNA ADP-ribosylation | biological process | The covalent attachment of an ADP-ribosyl group to a residue in double-stranded DNA. [PMID:11592983, PMID:27471034, PMID:29361132, PMID:29520010] |
positive regulation of DNA-templated transcription, elongation | biological process | Any process that activates or increases the frequency, rate or extent of transcription elongation, the extension of an RNA molecule after transcription initiation and promoter clearance by the addition of ribonucleotides catalyzed by a DNA-dependent RNA polymerase. [GOC:mah, GOC:txnOH] |
cellular response to insulin stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an insulin stimulus. Insulin is a polypeptide hormone produced by the islets of Langerhans of the pancreas in mammals, and by the homologous organs of other organisms. [GOC:mah, ISBN:0198506732] |
positive regulation of intracellular estrogen receptor signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of the activity of an intracellular estrogen receptor signaling pathway. [GOC:mah] |
negative regulation of transcription elongation by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription elongation, the extension of an RNA molecule after transcription initiation and promoter clearance by the addition of ribonucleotides, catalyzed by RNA polymerase II. [GOC:mah, GOC:txnOH] |
cellular response to UV | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an ultraviolet radiation (UV light) stimulus. Ultraviolet radiation is electromagnetic radiation with a wavelength in the range of 10 to 380 nanometers. [GOC:mah] |
positive regulation of canonical NF-kappaB signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of a canonical NF-kappaB signaling cascade. [GOC:jl] |
innate immune response | biological process | Innate immune responses are defense responses mediated by germline encoded components that directly recognize components of potential pathogens. [GO_REF:0000022, GOC:add, GOC:ebc, GOC:mtg_sensu] |
regulation of circadian sleep/wake cycle, non-REM sleep | biological process | Any process that modulates the frequency, rate or extent of non-rapid eye movement sleep. [GOC:go_curators] |
negative regulation of innate immune response | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the innate immune response. [GOC:go_curators] |
negative regulation of DNA-templated transcription | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
decidualization | biological process | The cellular and vascular changes occurring in the endometrium of the pregnant uterus just after the onset of blastocyst implantation. This process involves the proliferation and differentiation of the fibroblast-like endometrial stromal cells into large, polyploid decidual cells that eventually form the maternal component of the placenta. [ISBN:0721662544, PMID:11133685] |
regulation of catalytic activity | biological process | Any process that modulates the activity of an enzyme. [GOC:ai, GOC:ebc, GOC:vw] |
positive regulation of mitochondrial depolarization | biological process | Any process that activates, maintains or increases the frequency, rate or extent of the change in the membrane potential of the mitochondria from negative to positive. [GOC:ai] |
positive regulation of SMAD protein signal transduction | biological process | Any process that increases the rate, frequency or extent of SMAD protein signal transduction. [GOC:BHF, GOC:dph, GOC:tb] |
positive regulation of necroptotic process | biological process | Any process that increases the rate, frequency or extent of a necroptotic process, a necrotic cell death process that results from the activation of endogenous cellular processes, such as signaling involving death domain receptors or Toll-like receptors. [GOC:BHF, GOC:dph, GOC:mtg_apoptosis, GOC:tb] |
protein poly-ADP-ribosylation | biological process | The transfer of multiple ADP-ribose residues from NAD to a protein amino acid, forming a poly(ADP-ribose) chain. [GOC:BHF, GOC:mah, GOC:rl, PMID:25043379] |
protein auto-ADP-ribosylation | biological process | The ADP-ribosylation by a protein of one or more of its own amino acid residues, or residues on an identical protein. [GOC:BHF, GOC:rl] |
protein localization to chromatin | biological process | Any process in which a protein is transported to, or maintained at, a part of a chromosome that is organized into chromatin. [GOC:mah] |
cellular response to zinc ion | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a zinc ion stimulus. [GOC:mah] |
replication fork reversal | biological process | Replication fork processing that involves the unwinding of blocked forks to form four-stranded structures resembling Holliday junctions, which are subsequently resolved. [PMID:19406929] |
negative regulation of cGAS/STING signaling pathway | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of cGAS/STING signaling pathway. [PMID:29875158] |
positive regulation of protein localization to nucleus | biological process | Any process that activates or increases the frequency, rate or extent of protein localization to nucleus. [GOC:TermGenie] |
regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathway | biological process | Any process that modulates the frequency, rate or extent of oxidative stress-induced neuron intrinsic apoptotic signaling pathway. [GO_REF:0000058, GOC:bf, GOC:PARL, GOC:TermGenie] |
positive regulation of single strand break repair | biological process | Any process that activates or increases the frequency, rate or extent of single strand break repair. [GO_REF:0000058, GOC:BHF, GOC:rl, GOC:TermGenie, PMID:17395247] |
response to aldosterone | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of an aldosterone stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:17644563] |
negative regulation of adipose tissue development | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of adipose tissue development. [GO_REF:0000058, GOC:TermGenie, PMID:23081848] |
negative regulation of telomere maintenance via telomere lengthening | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of telomere maintenance via telomere lengthening. [GO_REF:0000058, GOC:BHF, GOC:BHF_telomere, GOC:nc, GOC:TermGenie, PMID:23959892] |
cellular response to amyloid-beta | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a amyloid-beta stimulus. [GO_REF:0000071, GOC:TermGenie, PMID:23555824] |
positive regulation of myofibroblast differentiation | biological process | Any process that activates or increases the frequency, rate or extent of myofibroblast differentiation. [GO_REF:0000058, GOC:BHF, GOC:BHF_miRNA, GOC:rph, GOC:TermGenie, PMID:20533548] |
regulation of base-excision repair | biological process | Any process that modulates the frequency, rate or extent of base-excision repair. [GO_REF:0000058, GOC:ah, GOC:TermGenie, PMID:18973764] |
positive regulation of double-strand break repair via homologous recombination | biological process | Any process that activates or increases the frequency, rate or extent of double-strand break repair via homologous recombination. [GO_REF:0000058, GOC:TermGenie, PMID:12023299] |
cellular response to nerve growth factor stimulus | biological process | A process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a nerve growth factor stimulus. [PMID:22399805, Wikipedia:Nerve_growth_factor] |
ATP generation from poly-ADP-D-ribose | biological process | The process of generating ATP in the nucleus from poly-ADP-D-ribose. Nuclear ATP generation is required for extensive chromatin remodeling events that are energy-consuming. [PMID:27257257] |
negative regulation of ATP biosynthetic process | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of ATP biosynthetic process. [GOC:obol] |