ArticleChemistry & biology2013
Next-generation NAMPT inhibitors identified by sequential high-throughput phenotypic chemical and functional genomic screens.
Article in Chemistry & biology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 49 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
49 citing papers in PubMed.
- Article
- Phenotypic drug discovery: recent successes, lessons learned and new directions.Nature reviews. Drug discovery · 2022Review
- Functional characterization of the PI3K/AKT/MTOR signaling pathway for targeted therapy in B-precursor acute lymphoblastic leukemia.Cancer gene therapy · 2022Article
- NAD/NAMPT and mTOR Pathways in Melanoma: Drivers of Drug Resistance and Prospective Therapeutic Targets.International journal of molecular sciences · 2022Review
- Review
- NAMPT Inhibition Induces Neuroblastoma Cell Death and Blocks Tumor Growth.Frontiers in oncology · 2022Article
- PAK4 and NAMPT as Novel Therapeutic Targets in Diffuse Large B-Cell Lymphoma, Follicular Lymphoma, and Mantle Cell Lymphoma.Cancers · 2021Article
- Functional annotation of lncRNA in high-throughput screening.Essays in biochemistry · 2021Review
- Advances in NAD-Lowering Agents for Cancer Treatment.Nutrients · 2021Review
- From Phenotypic Hit to Chemical Probe: Chemical Biology Approaches to Elucidate Small Molecule Action in Complex Biological Systems.Molecules (Basel, Switzerland) · 2020Review
- Nampt-mediated spindle sizing secures a post-anaphase increase in spindle speed required for extreme asymmetry.Nature communications · 2020Article
- OT-82, a novel anticancer drug candidate that targets the strong dependence of hematological malignancies on NAD biosynthesis.Leukemia · 2020Article
- Effective targeting of NAMPT in patient-derived xenograft models of high-risk pediatric acute lymphoblastic leukemia.Leukemia · 2020Article
- A genome-wide analysis of targets of macrolide antibiotics in mammalian cells.The Journal of biological chemistry · 2020Article
- Tryptophan scanning mutagenesis as a way to mimic the compound-bound state and probe the selectivity of allosteric inhibitors in cells.Chemical science · 2020Article
- Metabolomic profiles of induced pluripotent stem cells derived from patients with rheumatoid arthritis and osteoarthritis.Stem cell research & therapy · 2019Article
- Article
- LMO2 activation by deacetylation is indispensable for hematopoiesis and T-ALL leukemogenesis.Blood · 2019Article
- Metabolomic profiling identifies pathways associated with minimal residual disease in childhood acute lymphoblastic leukaemia.EBioMedicine · 2019Article
- Chemogenetic interactions in human cancer cells.Computational and structural biotechnology journal · 2019Review
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14 authors.
Funding
Abstract
Phenotypic high-throughput chemical screens allow for discovery of small molecules that modulate complex phenotypes and provide lead compounds for novel therapies; however, identification of the mechanistically relevant targets remains a major experimental challenge. We report the application of sequential unbiased high-throughput chemical and ultracomplex small hairpin RNA (shRNA) screens to identify a distinctive class of inhibitors that target nicotinamide phosphoribosyl transferase (NAMPT), a rate-limiting enzyme in the biosynthesis of nicotinamide adenine dinucleotide, a crucial cofactor in many biochemical processes. The lead compound STF-118804 is a highly specific NAMPT inhibitor, improves survival in an orthotopic xenotransplant model of high-risk acute lymphoblastic leukemia, and targets leukemia stem cells. Tandem high-throughput screening using chemical and ultracomplex shRNA libraries, therefore, provides a rapid chemical genetics approach for seamless progression from small-molecule lead identification to target discovery and validation.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.