Discover Community Create You

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Article

Structural basis for resistance to diverse classes of NAMPT inhibitors.

PloS one - 1 Jan 2014

Wang Weiru, Elkins Kristi, Oh Angela, Ho Yen-Ching, Wu Jiansheng, Li Hong, Xiao Yang, Kwong Mandy, Coons Mary, Brillantes Bobby, Cheng Eric, Crocker Lisa, Dragovich Peter S, Sampath Deepak, Zheng Xiaozhang, Bair Kenneth W, O'Brien Thomas, Belmont Lisa D

Abstract excerpt

Inhibiting NAD biosynthesis by blocking the function of nicotinamide phosphoribosyl transferase (NAMPT) is an attractive therapeutic strategy for targeting tumor metabolism. However, the development of drug resistance commonly limits the efficacy of cancer therapeutics. This study identifies mutations in NAMPT that confer resistance to a novel NAMPT inhibitor, GNE-618, in cell culture and in vivo, thus...

Read the complete abstract on PubMed

Topics

Share this publication in a Topic to start or enrich a Post.

Share to Enzyme Inhibitors
Share to Antineoplastic Agents

Methodology Data sources Editorial policy Privacy About Contact Helena Bioinformatics

Share to Catalytic Domain

Share to Cell Line, Tumor

Share to Cytokines

Share to Drug Resistance, Neoplasm

Share to Models, Molecular

Share to Nicotinamide Phosphoribosyltransferase

Source

Open in PubMed Open full text

Identifiers

PMID: 25285661
DOI: 10.1371/journal.pone.0109366
PMCID: PMC4186856

Genes

NAMPT
GNE

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

Related research

Semantic proximity does not establish scientific evidence.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

Structural basis for resistance to diverse classes of NAMPT inhibitors.PMID 25285661Read ↗

Identification of novel resistance mechanisms to NAMPT inhibition via the de novo NAD+ biosynthesis pathway and NAMPT mutation.Semantic proximity Read ↗

Mechanisms of resistance to NAMPT inhibitors in cancerSemantic proximity Read ↗

Target enzyme mutations are the molecular basis for resistance towards pharmacological inhibition of nicotinamide phosphoribosyltransferase.Semantic proximity Read ↗

Discovery of a Highly Selective NAMPT Inhibitor That Demonstrates Robust Efficacy and Improved Retinal Toxicity with Nicotinic Acid CoadministrationSemantic proximity Read ↗

Identification of NAPRT Inhibitors with Anti-Cancer Properties by In Silico Drug DiscoverySemantic proximity Read ↗

Discovery and characterization of novel small-molecule inhibitors targeting nicotinamide phosphoribosyltransferaseSemantic proximity Read ↗

Next-generation NAMPT inhibitors identified by sequential high-throughput phenotypic chemical and functional genomic screens.Semantic proximity Read ↗

Nicotinic Acid Phosphoribosyltransferase Regulates Cancer Cell Metabolism, Susceptibility to NAMPT Inhibitors, and DNA RepairSemantic proximity Read ↗

Loss of NAPRT1 Expression by Tumor-Specific Promoter Methylation Provides a Novel Predictive Biomarker for NAMPT InhibitorsSemantic proximity Read ↗

NAMPT Is the Cellular Target of STF-31-Like Small-Molecule ProbesSemantic proximity Read ↗

Advances in NAD-Lowering Agents for Cancer TreatmentSemantic proximity Read ↗

NNMT-driven metabolic reprogramming creates a NAMPT druggable vulnerability and reveals liquid biopsy biomarkers for TKI resistance in EGFR-mutant NSCLC.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.