Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

NAMPT (P43490) - Overview - Molecular Target Synopsis

Protein


NAMPT, Nicotinamide phosphoribosyltransferase
Enzyme Classification 2.4.2.12
UniProt P43490

Also Known as NAMPT_HUMAN, NAMPT, PBEF, PBEF1

Catalyzes the condensation of nicotinamide with 5-phosphoribosyl-1-pyrophosphate to yield nicotinamide mononucleotide, an intermediate in the biosynthesis of NAD. It is the rate limiting component in the mammalian NAD biosynthesis pathway. The secreted form behaves both as a cytokine with immunomodulating properties and an adipokine with anti-diabetic properties, it has no enzymatic activity, partly because of lack of activation by ATP, which has a low level in extracellular space and plasma. Plays a role in the modulation of circadian clock function. NAMPT-dependent oscillatory production of NAD regulates oscillation of clock target gene expression by releasing the core clock component: CLOCK-ARNTL/BMAL1 heterodimer from NAD-dependent SIRT1-mediated suppression. Homodimer.

6B75
CRYSTAL STRUCTURE OF HUMAN NAMPT IN COMPLEX WITH NVP-LOQ594
RCSB/PDB
Inspect Structure
See all 3D Structures for NAMPT

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: NAMPT is active in the following subcellular-locations: cytoplasm, nucleus, secreted.
GO terms: NAMPT is active in the following subcellular-locations: cell junction, cytosol, extracellular exosome, nuclear speck, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project NAMPT has gain in 7 cell-lines, loss in 1 cell-lines and no signal in 997 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SR, NCI_H460, A498

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SCC-3, EBC-1, SU-DHL-1

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: NHLF, HMEC, A549

(see details)

3D Structures


For NAMPT there are:
62 structures (133 chains) solved
55 are solved in complex with at least one small molecule ligand
2 are solved with an approved drug

NAMPT is solved in complex with the approved drug(s):

20J/DIAZOXIDE (4LV9_A, 4LV9_B),
NCA/NIACINAMIDE (2E5D_A, 2E5D_B).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


NAMPT has been screened with 2448 compounds (2870 bioactivities), 2122 compounds have bioactivities that show binding affinity of <= 500nM (2423 bioactivities). (see details)