DC Field | Value | Language |
---|---|---|
dc.contributor.author | Choe, Hyeonjeong | ko |
dc.contributor.author | Kim, Jieun | ko |
dc.contributor.author | Hong, Sungwoo | ko |
dc.date.accessioned | 2013-08-22T02:28:49Z | - |
dc.date.available | 2013-08-22T02:28:49Z | - |
dc.date.created | 2013-08-21 | - |
dc.date.created | 2013-08-21 | - |
dc.date.issued | 2013-08 | - |
dc.identifier.citation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.23, no.15, pp.4324 - 4327 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | http://hdl.handle.net/10203/175554 | - |
dc.description.abstract | The existence of drug resistance caused by mutations in the break-point cluster region-Abelson (BCR-ABL) tyrosine kinase domain remains a clinical challenge due to limited treatment options for effective CML therapies. Here, we report a series of flavone-based common inhibitors equipotent for the wild type and the most drug-resistant T315I mutant of BCR-ABL. The original hit 1 was extensively modified through a structure-based drug design strategy, especially by varying the C7 acetamide appendage of the scaffold to exploit extended interactions with P-loop residues. Structural features relevant to the stabilization of the newly identified inhibitors in the ATP-binding site of ABL are discussed in detail. (C) 2013 Elsevier Ltd. All rights reserved. | - |
dc.language | English | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.subject | CHRONIC MYELOID-LEUKEMIA | - |
dc.subject | BCR-ABL | - |
dc.subject | KINASE | - |
dc.subject | DISCOVERY | - |
dc.subject | POTENT | - |
dc.subject | IDENTIFICATION | - |
dc.subject | RESISTANCE | - |
dc.subject | BIOLOGY | - |
dc.subject | AP24534 | - |
dc.subject | DRUG | - |
dc.title | Structure-based design of flavone-based inhibitors of wild-type and T315I mutant of ABL | - |
dc.type | Article | - |
dc.identifier.wosid | 000321495900008 | - |
dc.identifier.scopusid | 2-s2.0-84879696006 | - |
dc.type.rims | ART | - |
dc.citation.volume | 23 | - |
dc.citation.issue | 15 | - |
dc.citation.beginningpage | 4324 | - |
dc.citation.endingpage | 4327 | - |
dc.citation.publicationname | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.identifier.doi | 10.1016/j.bmcl.2013.05.095 | - |
dc.contributor.localauthor | Hong, Sungwoo | - |
dc.contributor.nonIdAuthor | Choe, Hyeonjeong | - |
dc.contributor.nonIdAuthor | Kim, Jieun | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordAuthor | BCR-ABL | - |
dc.subject.keywordAuthor | Chronic myelogenous leukemia | - |
dc.subject.keywordAuthor | T315I mutant | - |
dc.subject.keywordAuthor | Structure-based design | - |
dc.subject.keywordAuthor | Flavone | - |
dc.subject.keywordPlus | CHRONIC MYELOID-LEUKEMIA | - |
dc.subject.keywordPlus | BCR-ABL | - |
dc.subject.keywordPlus | KINASE | - |
dc.subject.keywordPlus | DISCOVERY | - |
dc.subject.keywordPlus | POTENT | - |
dc.subject.keywordPlus | IDENTIFICATION | - |
dc.subject.keywordPlus | RESISTANCE | - |
dc.subject.keywordPlus | BIOLOGY | - |
dc.subject.keywordPlus | AP24534 | - |
dc.subject.keywordPlus | DRUG | - |
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