Proteins > Nicotinamide phosphoribosyltransferase
Page last updated: 2024-08-07 23:31:04
Nicotinamide phosphoribosyltransferase
A nicotinamide phosphoribosyltransferase that is encoded in the genome of human. [PRO:DNx, UniProtKB:P43490]
Synonyms
NAmPRTase;
Nampt;
EC 2.4.2.12;
Pre-B-cell colony-enhancing factor 1;
Pre-B cell-enhancing factor;
Visfatin
Research
Bioassay Publications (21)
Timeframe | Studies on this Protein(%) | 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 | 18 (85.71) | 24.3611 |
2020's | 3 (14.29) | 2.80 |
Compounds (8)
Drugs with Inhibition Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
ci 994 | Homo sapiens (human) | IC50 | 2.0000 | 1 | 1 |
chs 828 | Homo sapiens (human) | IC50 | 0.0037 | 8 | 8 |
chs 828 | Homo sapiens (human) | Ki | 0.0030 | 1 | 1 |
stf-31 | Homo sapiens (human) | IC50 | 0.0215 | 2 | 2 |
fk 866 | Homo sapiens (human) | IC50 | 0.9955 | 15 | 15 |
fk 866 | Homo sapiens (human) | Ki | 0.0024 | 4 | 4 |
chidamide | Homo sapiens (human) | IC50 | 2.1000 | 1 | 1 |
gne-618 | Homo sapiens (human) | IC50 | 0.0054 | 3 | 3 |
gne-617 | Homo sapiens (human) | IC50 | 0.0044 | 5 | 5 |
Drugs with Activation Measurements
Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
diazoxide | Homo sapiens (human) | Kd | 230.0000 | 1 | 1 |
gne-618 | Homo sapiens (human) | EC50 | 0.0012 | 1 | 1 |
gne-617 | Homo sapiens (human) | EC50 | 0.0011 | 1 | 1 |
SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT).Bioorganic & medicinal chemistry letters, , 08-01, Volume: 27, Issue:15, 2017
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.Journal of medicinal chemistry, , 09-22, Volume: 59, Issue:18, 2016
Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Structural and biochemical analyses of the catalysis and potency impact of inhibitor phosphoribosylation by human nicotinamide phosphoribosyltransferase.Chembiochem : a European journal of chemical biology, , May-26, Volume: 15, Issue:8, 2014
Nicotinamide phosphoribosyltransferase inhibitors, design, preparation, and structure-activity relationship.Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Structure-based identification of ureas as novel nicotinamide phosphoribosyltransferase (Nampt) inhibitors.Journal of medicinal chemistry, , Jun-27, Volume: 56, Issue:12, 2013
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Chemical proteomics identifies Nampt as the target of CB30865, an orphan cytotoxic compound.Chemistry & biology, , Jun-25, Volume: 17, Issue:6, 2010
[no title available]Journal of medicinal chemistry, , 06-09, Volume: 65, Issue:11, 2022
Dual nicotinamide phosphoribosyltransferase and epidermal growth factor receptor inhibitors for the treatment of cancer.European journal of medicinal chemistry, , Feb-05, Volume: 211, 2021
Discovery of trans-3-(pyridin-3-yl)acrylamide-derived sulfamides as potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitors for the potential treatment of cancer.Bioorganic & medicinal chemistry letters, , 06-15, Volume: 29, Issue:12, 2019
Controlling cellular distribution of drugs with permeability modifying moieties.MedChemComm, , Jun-01, Volume: 10, Issue:6, 2019
Fragment-based discovery of a potent NAMPT inhibitor.Bioorganic & medicinal chemistry letters, , 02-01, Volume: 28, Issue:3, 2018
Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.ACS medicinal chemistry letters, , Jan-11, Volume: 9, Issue:1, 2018
SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT).Bioorganic & medicinal chemistry letters, , 08-01, Volume: 27, Issue:15, 2017
Small Molecule Inhibitors Simultaneously Targeting Cancer Metabolism and Epigenetics: Discovery of Novel Nicotinamide Phosphoribosyltransferase (NAMPT) and Histone Deacetylase (HDAC) Dual Inhibitors.Journal of medicinal chemistry, , 10-12, Volume: 60, Issue:19, 2017
Structure-Based Design of Potent Nicotinamide Phosphoribosyltransferase Inhibitors with Promising in Vitro and in Vivo Antitumor Activities.Journal of medicinal chemistry, , 06-23, Volume: 59, Issue:12, 2016
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.Journal of medicinal chemistry, , 09-22, Volume: 59, Issue:18, 2016
Fragment-based identification of amides derived from trans-2-(pyridin-3-yl)cyclopropanecarboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Nicotinamide phosphoribosyltransferase inhibitors, design, preparation, and structure-activity relationship.Journal of medicinal chemistry, , Nov-27, Volume: 56, Issue:22, 2013
Medicinal chemistry of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Structure-based identification of ureas as novel nicotinamide phosphoribosyltransferase (Nampt) inhibitors.Journal of medicinal chemistry, , Jun-27, Volume: 56, Issue:12, 2013
Design, synthesis and X-ray crystallographic study of NAmPRTase inhibitors as anti-cancer agents.European journal of medicinal chemistry, , Volume: 46, Issue:4, 2011
Chemical proteomics identifies Nampt as the target of CB30865, an orphan cytotoxic compound.Chemistry & biology, , Jun-25, Volume: 17, Issue:6, 2010
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.Journal of medicinal chemistry, , 09-22, Volume: 59, Issue:18, 2016
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 23, Issue:20, 2013
Minimizing CYP2C9 Inhibition of Exposed-Pyridine NAMPT (Nicotinamide Phosphoribosyltransferase) Inhibitors.Journal of medicinal chemistry, , 09-22, Volume: 59, Issue:18, 2016
Structural and biochemical analyses of the catalysis and potency impact of inhibitor phosphoribosylation by human nicotinamide phosphoribosyltransferase.Chembiochem : a European journal of chemical biology, , May-26, Volume: 15, Issue:8, 2014
Structure-based discovery of novel amide-containing nicotinamide phosphoribosyltransferase (nampt) inhibitors.Journal of medicinal chemistry, , Aug-22, Volume: 56, Issue:16, 2013
Identification of amides derived from 1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid as potent inhibitors of human nicotinamide phosphoribosyltransferase (NAMPT).Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 23, Issue:20, 2013
Enables
This protein enables 4 target(s):
Target | Category | Definition |
cytokine activity | molecular function | The activity of a soluble extracellular gene product that interacts with a receptor to effect a change in the activity of the receptor to control the survival, growth, differentiation and effector function of tissues and cells. [ISBN:0198599471, PMID:11530802] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
nicotinamide phosphoribosyltransferase activity | molecular function | Catalysis of the reaction: diphosphate + nicotinamide mononucleotide = 5-phospho-alpha-D-ribose 1-diphosphate + H+ + nicotinamide. [RHEA:16149] |
Located In
This protein is located in 4 target(s):
Target | Category | Definition |
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] |
nuclear speck | cellular component | A discrete extra-nucleolar subnuclear domain, 20-50 in number, in which splicing factors are seen to be localized by immunofluorescence microscopy. [http://www.cellnucleus.com/] |
cell junction | cellular component | A cellular component that forms a specialized region of connection between two or more cells, or between a cell and the extracellular matrix, or between two membrane-bound components of a cell, such as flagella. [GOC:aruk, GOC:bc, GOC:mah, http://www.vivo.colostate.edu/hbooks/cmb/cells/pmemb/junctions_a.html, ISBN:0198506732, PMID:26820516, PMID:28096264] |
extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
Involved In
This protein is involved in 8 target(s):
Target | Category | Definition |
signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
cell-cell signaling | biological process | Any process that mediates the transfer of information from one cell to another. This process includes signal transduction in the receiving cell and, where applicable, release of a ligand and any processes that actively facilitate its transport and presentation to the receiving cell. Examples include signaling via soluble ligands, via cell adhesion molecules and via gap junctions. [GOC:dos, GOC:mah] |
positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
circadian regulation of gene expression | biological process | Any process that modulates the frequency, rate or extent of gene expression such that an expression pattern recurs with a regularity of approximately 24 hours. [GOC:mah] |
NAD biosynthesis via nicotinamide riboside salvage pathway | biological process | The chemical reactions and pathways resulting in the formation of nicotinamide adenine dinucleotide (NAD) from the vitamin precursor nicotinamide riboside. [PMID:17482543] |
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] |
positive regulation of nitric-oxide synthase biosynthetic process | biological process | Any process that activates or increases the frequency, rate or extent of the chemical reactions and pathways resulting in the formation of a nitric oxide synthase enzyme. [GOC:ai] |
NAD biosynthetic process | biological process | The chemical reactions and pathways resulting in the formation of nicotinamide adenine dinucleotide, a coenzyme present in most living cells and derived from the B vitamin nicotinic acid; biosynthesis may be of either the oxidized form, NAD, or the reduced form, NADH. [GOC:jl, ISBN:0618254153] |