Deep Learning-Driven Anticancer Drug Discovery: Emodepside as a Potential Therapeutic Candidate for Triple-Negative Breast Cancer. [PDF]
J Chem Inf ModelXu Y, Dong T, Li B, Yu J, Wang L.
europepmc +1 more source
Exploiting Metabolic Vulnerabilities in Acute Myeloid Leukemia: Rationale and Evidence for Combining Metabolic Modulators with Conventional Chemotherapy. [PDF]
Pharmaceuticals (Basel)Shams UA +6 more
europepmc +1 more source
High expression of NAMPT in adult T-cell leukemia/lymphoma and anti-tumor activity of a NAMPT inhibitor [PDF]
European Journal of Pharmacology, 2019 ArticleAdult T-cell leukemia/lymphoma (ATL) is a malignancy of mature T lymphocytes induced by human T-cell leukemia virus-1 and has a poor outcome. New molecular targets for the prevention and treatment of ATL are needed urgently. We previously reported
Tomohiro Kozako +2 more
exaly +4 more sources
The NAMPT Inhibitor FK866 Increases Metformin Sensitivity in Pancreatic Cancer Cells [PDF]
Cancers, 2022 Sebastian Igelmann +2 more
exaly +2 more sources
NAMPT Inhibitor and P73 Activator Represses P53 R175H Mutated HNSCC Cell Proliferation in a Synergistic Manner [PDF]
Biomolecules, 2022 Ching-Feng Lien +2 more
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Fragment-based discovery of a potent NAMPT inhibitor
Bioorganic and Medicinal Chemistry Letters, 2018NAMPT expression is elevated in many cancers, making this protein a potential target for anticancer therapy. We have carried out both NMR based and TR-FRET based fragment screens against human NAMPT and identified six novel binders with a range of potencies. Co-crystal structures were obtained for two of the fragments bound to NAMPT while for the other
Diana Raich +2 more
exaly +3 more sources
NAMPT Over-Expression Recapitulates the BRAF Inhibitor Resistant Phenotype Plasticity in Melanoma [PDF]
Cancers, 2020 Serine–threonine protein kinase B-RAF (BRAF)-mutated metastatic melanoma (MM) is a highly aggressive type of skin cancer. Treatment of MM patients using BRAF/MEK inhibitors (BRAFi/MEKi) eventually leads to drug resistance, limiting any clinical benefit ...
Francesca Arruga +2 more
exaly +4 more sources
A Red-Light-Activated Ruthenium-Caged NAMPT Inhibitor Remains Phototoxic in Hypoxic Cancer Cells [PDF]
Angewandte Chemie - International Edition, 2017 Sven H C Askes +2 more
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Crystal structure-based comparison of two NAMPT inhibitors [PDF]
Acta Pharmacologica Sinica, 2017 Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) is a novel strategy for cancer therapy, but only two inhibitors of NAMPT (FK866 and CHS828) have progressed into clinical trials. This study seeks to compare a novel potent NAMPT inhibitor, MS0, with a classical inhibitor FK866 in their biological activity and molecular binding mode, thereby ...
Chao-Yu Miao, Shuo Han, Tian-Ying Xu
exaly +3 more sources
Medicinal Chemistry of Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors
Journal of Medicinal Chemistry, 2013Nicotinamide phoshophoribosyltransferase (NAMPT) plays a key role in the replenishment of the NAD pool in cells. This in turn makes this enzyme an important player in bioenergetics and in the regulation of NAD-using enzymes, such as PARPs and sirtuins. Furthermore, there is now ample evidence that NAMPT is secreted and has a role as a cytokine.
GALLI, Ubaldina +6 more
openaire +5 more sources