| Literature DB >> 10695671 |
A Zhao1, S H Lee, M Mojena, R G Jenkins, D R Patrick, H E Huber, M A Goetz, O D Hensens, D L Zink, D Vilella, A W Dombrowski, R B Lingham, L Huang.
Abstract
A resorcylic acid lactone, L-783,277, isolated from a Phoma sp. (ATCC 74403) which came from the fruitbody of Helvella acetabulum, is a potent and specific inhibitor of MEK (Map kinase kinase). L-783,277 inhibits MEK with an IC50 value of 4 nM. It weakly inhibits Lck and is inactive against Raf, PKA and PKC. L-783,277 is an irreversible inhibitor of MEK and is competitive with respect to ATP. L-783,290, the trans-isomer of L-783,277, was isolated from the same culture and evaluated together with several semi-synthetic resorcylic acid lactone analogs. A preliminary structure-activity relationship is presented. Several independent cell-based assays have been carried out to study the biological activities of these resorcylic acid lactone compounds and a brief result summary from these studies is presented.Entities:
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Year: 1999 PMID： 10695671 DOI： 10.7164/antibiotics.52.1086
Source DB: PubMed Journal: J Antibiot (Tokyo) ISSN： 0021-8820 Impact factor: 2.649