Title : Discovery of marinopyrrole A (maritoclax) as a selective Mcl-1 antagonist that overcomes ABT-737 resistance by binding to and targeting Mcl-1 for proteasomal degradation.

Pub. Date : 2012 Mar 23

PMID : 22311987






3 Functional Relationships(s)
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1 While ABT-737 and its orally active analog ABT-263 are the most potent and specific inhibitors to date that bind Bcl-2 and Bcl-X(L) with high affinity but have a much lower affinity for Mcl-1, they are not very effective as single agents in certain cancer types because of elevated levels of Mcl-1. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid MCL1 apoptosis regulator, BCL2 family member Homo sapiens
2 While ABT-737 and its orally active analog ABT-263 are the most potent and specific inhibitors to date that bind Bcl-2 and Bcl-X(L) with high affinity but have a much lower affinity for Mcl-1, they are not very effective as single agents in certain cancer types because of elevated levels of Mcl-1. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid MCL1 apoptosis regulator, BCL2 family member Homo sapiens
3 While ABT-737 and its orally active analog ABT-263 are the most potent and specific inhibitors to date that bind Bcl-2 and Bcl-X(L) with high affinity but have a much lower affinity for Mcl-1, they are not very effective as single agents in certain cancer types because of elevated levels of Mcl-1. 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid MCL1 apoptosis regulator, BCL2 family member Homo sapiens