Discovery of a potent and selective Bcl-2 inhibitor using SAR by NMR

The Bcl-2 family of proteins plays a major role in the regulation of apoptosis, or programmed cell death. Overexpression of the anti-apoptotic members of this family (Bcl-2, Bcl-xL, and Mcl-1) can render cancer cells resistant to chemotherapeutic agents and therefore these proteins are important tar...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-11, Vol.20 (22), p.6587-6591
Hauptverfasser:	Petros, Andrew M., Huth, Jeffrey R., Oost, Thorsten, Park, Cheol-Min, Ding, Hong, Wang, Xilu, Zhang, Haichao, Nimmer, Paul, Mendoza, Renaldo, Sun, Chaohong, Mack, Jamey, Walter, Karl, Dorwin, Sarah, Gramling, Emily, Ladror, Uri, Rosenberg, Saul H., Elmore, Steven W., Fesik, Stephen W., Hajduk, Philip J.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic agents Apoptosis Bcl Biological and medical sciences Fragment General aspects Linking Magnetic Resonance Spectroscopy - methods Medical sciences Models, Molecular NMR Pharmacology. Drug treatments Proto-Oncogene Proteins c-bcl-2 - antagonists & inhibitors Structure-Activity Relationship Structure-based
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