| Literature DB >> 9873633 |
J V Duncia1, J B Santella, C A Higley, W J Pitts, J Wityak, W E Frietze, F W Rankin, J H Sun, R A Earl, A C Tabaka, C A Teleha, K F Blom, M F Favata, E J Manos, A J Daulerio, D A Stradley, K Horiuchi, R A Copeland, P A Scherle, J M Trzaskos, R L Magolda, G L Trainor, R R Wexler, F W Hobbs, R E Olson.
Abstract
In search of antiinflammatory drugs with a new mechanism of action, U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with an IC50 of 0.07 microM for MEK 1 and 0.06 microM for MEK 2. U0126 can undergo isomerization and cyclization reactions to form a variety of products, both chemically and in vivo, all of which exhibit less affinity for MEK and lower inhibition of AP-1 activity than parent, U0126.Entities:
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Year: 1998 PMID： 9873633 DOI： 10.1016/s0960-894x(98)00522-8
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823