Page last updated: 2024-11-13
pyridostatin
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
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Protein Interactions
Research Growth
Market Indicators
Description
pyridostatin: binds telomeric G-quadruplexes; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 25227847 |
| CHEMBL ID | 2349416 |
| SCHEMBL ID | 24711398 |
| MeSH ID | M0568264 |
Synonyms (21)
| Synonym |
|---|
| 1085412-37-8 |
| 4-(2-aminoethoxy)-n2,n6-bis(4-(2-aminoethoxy)quinolin-2-yl)pyridine-2,6-dicarboxamide |
| pyridostatin |
| CHEMBL2349416 |
| CS-1439 |
| HY-15176 |
| rr-82 |
| AKOS026750251 |
| EX-A869 |
| pyridostain |
| 4-(2-aminoethoxy)-n2,n6-bis[4-(2-aminoethoxy)quinolin-2-yl]pyridine-2,6-dicarboxamide |
| NCGC00357427-06 |
| BCP07688 |
| rr 82 |
| AS-16720 |
| 4-(2-aminoethoxy)-2-n,6-n-bis[4-(2-aminoethoxy)quinolin-2-yl]pyridine-2,6-dicarboxamide |
| NCGC00357427-11 |
| 4-(2-azanylethoxy)-n2,n6-bis[4-(2-azanylethoxy)quinolin-2-yl]pyridine-2,6-dicarboxamide |
| SCHEMBL24711398 |
| 4-(2-aminoethoxy)-n2,n6-bis[4-(2-aminoethoxy)-2-quinolinyl]-2,6-pyridinedicarboxamide, trifluoroacetate salt |
| AC-36193 |
Research Excerpts
Overview
Pyridostatin is a small molecule that binds G4s and is specifically toxic to BRCA1/2-deficient cells in vitro.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Pyridostatin is a small molecule that binds G4s and is specifically toxic to BRCA1/2-deficient cells in vitro." | ( Anti-tumoural activity of the G-quadruplex ligand pyridostatin against BRCA1/2-deficient tumours. Benainous, H; Biroccio, A; Bruna, A; De Visser, Y; Di Vito, S; Groelly, FJ; Kosova, AA; Leonetti, C; Porru, M; Ryan, A; Serra, V; Tarsounas, M; Zimmer, J, 2022) | 1.7 |
| "Pyridostatin (PDS) is a well-known G-quadruplex (G4) inducer and stabilizer, yet its target genes have remained unclear. " | ( G-quadruplex inducer/stabilizer pyridostatin targets SUB1 to promote cytotoxicity of a transplatinum complex. Fang, T; Gan, T; Han, J; Hou, Y; Jia, F; Li, S; Liu, X; Luo, Q; Qi, L; Wang, F; Wang, S; Zhang, Y; Zhao, Y, 2022) | 2.45 |
Bioavailability
| Excerpt | Reference | Relevance |
|---|---|---|
| "The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs." | ( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019) | 0.51 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Bioassays (22)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1473368 | Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for bloodstream form of Trypanosoma brucei brucei | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents. |
| AID1290618 | Ratio of binding affinity to Bcl2 G-quadruplex DNA (unknown origin) to binding affinity to duplex ds26 DNA (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7 | Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog. |
| AID1473363 | Antitrypanosomal activity against bloodstream form of Trypanosoma brucei brucei after 72 hrs by alamar blue assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents. |
| AID1875179 | Cytotoxicity against mouse MNMCA1 cells assessed as cell survival preincubated for 24 hrs with compound further incubated for 48 hrs in drug free medium by MTT assay | 2022 | Journal of medicinal chemistry, 09-22, Volume: 65, Issue:18 | Balancing Affinity, Selectivity, and Cytotoxicity of Hydrazone-Based G-Quadruplex Ligands for Activation of Interferon β Genes in Cancer Cells. |
| AID1290613 | Binding affinity to duplex ds20 DNA (unknown origin) assessed as binding constant at 8 uM by Stern-Volmer plot analysis in the presence of KCl and NaCl | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7 | Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog. |
| AID1473364 | Antileishmanial activity against Leishmania major MHOM/IL/80/Friedlin promastigotes after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents. |
| AID1473365 | Cytotoxicity against human MRC5 cells assessed as cell growth inhibition after 72 hrs by MTT assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents. |
| AID1290614 | Binding affinity to duplex ds26 DNA (unknown origin) assessed as binding constant at 8 uM by Stern-Volmer plot analysis in the presence of KCl and NaCl | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7 | Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog. |
| AID1473369 | Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for erythrocyte stage of Plasmodium falciparum 3D7 | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents. |
| AID1473366 | Antimalarial activity against erythrocyte stage of Plasmodium falciparum 3D7 preincubated for 48 hrs followed by [3H]-hypoxanthine addition measured after 18 hrs by liquid scintillation counting | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents. |
| AID1473367 | Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for Leishmania major MHOM/IL/80/Friedlin promastigotes | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | G-Quadruplex Identification in the Genome of Protozoan Parasites Points to Naphthalene Diimide Ligands as New Antiparasitic Agents. |
| AID737820 | Thermal stabilization of human telomeric G-quadruplex FAM-TTAGGGTTAGGGTTAGGGTTAGGG-TAMRA DNA assessed as change in melting temperature at 1:5 DNA:ligand ratio by FRET assay | 2013 | Journal of medicinal chemistry, Apr-11, Volume: 56, Issue:7 | Guanidino anthrathiophenediones as G-quadruplex binders: uptake, intracellular localization, and anti-Harvey-Ras gene activity in bladder cancer cells. |
| AID1290622 | Ratio of binding affinity to Bcl2 G-quadruplex DNA (unknown origin) to binding affinity to duplex ds20 DNA (unknown origin) | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7 | Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog. |
| AID1290612 | Binding affinity to Bcl2 G-quadraplex DNA (unknown origin) assessed as binding constant at 8 uM by Stern-Volmer plot analysis in the presence of KCl and NaCl | 2016 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7 | Stabilization of G-quadruplex DNA and inhibition of Bcl-2 expression by a pyridostatin analog. |
| AID1347411 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary | 2020 | ACS chemical biology, 07-17, Volume: 15, Issue:7 | High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | |||
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (61)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 35 (57.38) | 24.3611 |
| 2020's | 26 (42.62) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Market Indicators
Research Demand Index: 34.83
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (34.83) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 2 (3.28%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 59 (96.72%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||