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Clearance of systemic hematologic tumors by venetoclax (Abt-199) and navitoclax.

Pharmacology research & perspectives

Ackler S, Oleksijew A, Chen J, Chyla BJ, Clarin J, Foster K, McGonigal T, Mishra S, Schlessinger S, Smith ML, Tahir SK, Leverson JD, Souers AJ, Boghaert ER, Hickson J.
PMID: 26516589
Pharmacol Res Perspect. 2015 Oct;3(5):e00178. doi: 10.1002/prp2.178. Epub 2015 Sep 01.

The Bcl-2 family inhibitors venetoclax and navitoclax demonstrated potent antitumor activity in chronic lymphocytic leukemia patients, notably in reducing marrow load and adenopathy. Subsequent trials with venetoclax have been initiated in non-Hodgkin's lymphoma and multiple myeloma patients. Traditional preclinical...

Discovery of a Potent and Selective BCL-XL Inhibitor with in Vivo Activity.

ACS medicinal chemistry letters

Tao ZF, Hasvold L, Wang L, Wang X, Petros AM, Park CH, Boghaert ER, Catron ND, Chen J, Colman PM, Czabotar PE, Deshayes K, Fairbrother WJ, Flygare JA, Hymowitz SG, Jin S, Judge RA, Koehler MF, Kovar PJ, Lessene G, Mitten MJ, Ndubaku CO, Nimmer P, Purkey HE, Oleksijew A, Phillips DC, Sleebs BE, Smith BJ, Smith ML, Tahir SK, Watson KG, Xiao Y, Xue J, Zhang H, Zobel K, Rosenberg SH, Tse C, Leverson JD, Elmore SW, Souers AJ.
PMID: 25313317
ACS Med Chem Lett. 2014 Aug 26;5(10):1088-93. doi: 10.1021/ml5001867. eCollection 2014 Oct 09.

A-1155463, a highly potent and selective BCL-XL inhibitor, was discovered through nuclear magnetic resonance (NMR) fragment screening and structure-based design. This compound is substantially more potent against BCL-XL-dependent cell lines relative to our recently reported inhibitor, WEHI-539, while possessing...

Showing 1 to 2 of 2 entries