Chemistry:Padnarsertib

From HandWiki

Padnarsertib (KPT-9274), is a drug which acts as a dual inhibitor of the enzymes p21-activated kinase 4 (PAK4) and nicotinamide phosphoribosyltransferase (NAMPT). It has potential applications in the treatment of some forms of cancer.[1][2][3][4][5][6][7]

References

  1. "Dual and Specific Inhibition of NAMPT and PAK4 By KPT-9274 Decreases Kidney Cancer Growth". Molecular Cancer Therapeutics 15 (9): 2119–2129. September 2016. doi:10.1158/1535-7163.MCT-16-0197. PMID 27390344. 
  2. "Targeting the vulnerability to NAD+ depletion in B-cell acute lymphoblastic leukemia". Leukemia 32 (3): 616–625. March 2018. doi:10.1038/leu.2017.281. PMID 28904384. 
  3. "PAK4-NAMPT Dual Inhibition as a Novel Strategy for Therapy Resistant Pancreatic Neuroendocrine Tumors". Cancers 11 (12): 1902. November 2019. doi:10.3390/cancers11121902. PMID 31795447. 
  4. "KPT-9274, an Inhibitor of PAK4 and NAMPT, Leads to Downregulation of mTORC2 in Triple Negative Breast Cancer Cells". Chemical Research in Toxicology 33 (2): 482–491. February 2020. doi:10.1021/acs.chemrestox.9b00376. PMID 31876149. 
  5. "Recent advances on development of p21-activated kinase 4 inhibitors as anti-tumor agents". Frontiers in Pharmacology 13. 2022. doi:10.3389/fphar.2022.956220. PMID 36105226. 
  6. "Targeting NAD+ Metabolism: Preclinical Insights into Potential Cancer Therapy Strategies". Endocrinology 165 (5). March 2024. doi:10.1210/endocr/bqae043. PMID 38565429. 
  7. "Inhibition of NAMPT by PAK4 Inhibitors". International Journal of Molecular Sciences 25 (18). September 2024. doi:10.3390/ijms251810138. PMID 39337621.