Naval Bajwa - Novel Mcl-1 inhibitors for pancreatic cancer therapy

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  Publication Details (including relevant citation   information):

  Author(s):   Nikolovska-Coleska Z, Bajwa N, Liu   M, et al.

  Conference   Information: 22nd EORTC-NCI-AACR Symposium on Molecular Targets   and Cancer Therapeutics, NOV 16-19, 2010 Berlin,   GERMANY

  Source:   EJC SUPPLEMENTS Volume:   8 Issue: 7 Pages: 94-94  Published: NOV 2010

  Times Cited:   0



  The anti-apoptotic myeloid cell leukemia protein Mcl-1, a member   of the Bcl-2 family proteins, has emerged as a promising   therapeutic target. It was demonstrated that Mcl-1 is an   important survival factor for pancreatic cancer cells; its   down-regulation with siRNA for example, enhances the induction of   apoptosis, chemosenstivity and radiosenstivity of pancreatic   cancer cells. Therefore targeting Mcl-1 to overcome apoptosis   resistance is an important strategy for the development of new   drugs to treat pancreatic cancer. Through high throughput   screening approach we have identified several promising lead   compounds which bind to the BH3 binding site in Mcl-1 selectively   over Bcl-2 and Bcl-xL, and distrupt interactions between   analogues and established initial structure-activity   relationships. Collectively, these findings provide good promise   for further chemical modifications of this compound and further   optimization toward developing a new class of anticancer drugs,   Mcl-1 inhibitors.

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