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Park, Cheol-Min
Synthetic & Medicinal Chemistry Lab
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  • Organic synthesis, medicinal chemistry, chemical biology

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ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets

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dc.contributor.author Souers, Andrew J. ko
dc.contributor.author Leverson, Joel D. ko
dc.contributor.author Boghaert, Erwin R. ko
dc.contributor.author Ackler, Scott L. ko
dc.contributor.author Catron, Nathaniel D. ko
dc.contributor.author Chen, Jun ko
dc.contributor.author Dayton, Brian D. ko
dc.contributor.author Ding, Hong ko
dc.contributor.author Enschede, Sari H. ko
dc.contributor.author Fairbrother, Wayne J. ko
dc.contributor.author Huang, David C. S. ko
dc.contributor.author Hymowitz, Sarah G. ko
dc.contributor.author Jin, Sha ko
dc.contributor.author Khaw, Seong Lin ko
dc.contributor.author Kovar, Peter J. ko
dc.contributor.author Lam, Lloyd T. ko
dc.contributor.author Lee, Jackie ko
dc.contributor.author Maecker, Heather L. ko
dc.contributor.author Marsh, Kennan C. ko
dc.contributor.author Mason, Kylie D. ko
dc.contributor.author Mitten, Michael J. ko
dc.contributor.author Nimmer, Paul M. ko
dc.contributor.author Oleksijew, Anatol ko
dc.contributor.author Park, Chang H. ko
dc.contributor.author Park, Cheol-Min ko
dc.contributor.author Phillips, Darren C. ko
dc.contributor.author Roberts, Andrew W. ko
dc.contributor.author Sampath, Deepak ko
dc.contributor.author Seymour, John F. ko
dc.contributor.author Smith, Morey L. ko
dc.contributor.author Sullivan, Gerard M. ko
dc.contributor.author Tahir, Stephen K. ko
dc.contributor.author Tse, Chris ko
dc.contributor.author Wendt, Michael D. ko
dc.contributor.author Xiao, Yu ko
dc.contributor.author Xue, John C. ko
dc.contributor.author Zhang, Haichao ko
dc.contributor.author Humerickhouse, Rod A. ko
dc.contributor.author Rosenberg, Saul H. ko
dc.contributor.author Elmore, Steven W. ko
dc.date.available 2014-11-11T00:15:47Z -
dc.date.created 2014-11-10 ko
dc.date.issued 2013-02 -
dc.identifier.citation NATURE MEDICINE, v.19, no.2, pp.202 - 208 ko
dc.identifier.issn 1078-8956 ko
dc.identifier.uri https://scholarworks.unist.ac.kr/handle/201301/8534 -
dc.identifier.uri http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=84873540049 ko
dc.description.abstract Proteins in the B cell CLL/lymphoma 2 (BCL-2) family are key regulators of the apoptotic process. This family comprises proapoptotic and prosurvival proteins, and shifting the balance toward the latter is an established mechanism whereby cancer cells evade apoptosis. The therapeutic potential of directly inhibiting prosurvival proteins was unveiled with the development of navitoclax, a selective inhibitor of both BCL-2 and BCL-2-like 1 (BCL-X L), which has shown clinical efficacy in some BCL-2-dependent hematological cancers. However, concomitant on-target thrombocytopenia caused by BCL-X L inhibition limits the efficacy achievable with this agent. Here we report the re-engineering of navitoclax to create a highly potent, orally bioavailable and BCL-2-selective inhibitor, ABT-199. This compound inhibits the growth of BCL-2-dependent tumors in vivo and spares human platelets. A single dose of ABT-199 in three patients with refractory chronic lymphocytic leukemia resulted in tumor lysis within 24 h. These data indicate that selective pharmacological inhibition of BCL-2 shows promise for the treatment of BCL-2-dependent hematological cancers. ko
dc.description.statementofresponsibility close -
dc.language ENG ko
dc.publisher NATURE PUBLISHING GROUP ko
dc.subject B-CELL LYMPHOMA ko
dc.subject CHRONIC LYMPHOCYTIC-LEUKEMIA ko
dc.subject ACUTE LYMPHOBLASTIC-LEUKEMIA ko
dc.subject NON-HODGKINS-LYMPHOMA ko
dc.subject FAMILY INHIBITOR ko
dc.subject INDUCE APOPTOSIS ko
dc.subject HIGH-AFFINITY ko
dc.subject IN-VIVO ko
dc.subject EXPRESSION ko
dc.subject CANCER ko
dc.title ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets ko
dc.type ARTICLE ko
dc.identifier.scopusid 2-s2.0-84873540049 ko
dc.identifier.wosid 000314675900028 ko
dc.type.rims ART ko
dc.description.wostc 201 *
dc.description.scopustc 136 *
dc.date.tcdate 2015-05-06 *
dc.date.scptcdate 2014-11-10 *
dc.identifier.doi 10.1038/nm.3048 ko
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