التفاصيل البيبلوغرافية
العنوان:
MEK inhibitors: The chemistry and biological activity of U0126, its analogs, and cyclization products
المؤلفون:
Santella Joseph B , John Wityak , Ruth R. Wexler , Robert A. Copeland , Pitts William J , Deborah A. Stradley , Frank W. Hobbs , Peggy Scherle , Elizabeth J. Manos , A. Christine Tabaka , Jung-Hui Sun , Kurumi Y. Horiuchi , James M. Trzaskos , William Eric Frietze , Ronald L. Magolda , Duncia John , Andrea J. Daulerio , Richard E. Olson , C. Anne Higley , Christopher A. Teleha , Richard A. Earl , F.Wayne Rankin , Margaret F. Favata , Karl F. Blom , George L. Trainor
المصدر:
Bioorganic & Medicinal Chemistry Letters . 8:2839-2844
بيانات النشر:
Elsevier BV, 1998.
سنة النشر:
1998
مصطلحات موضوعية:
Stereochemistry , Clinical Biochemistry , Anti-Inflammatory Agents , Pharmaceutical Science , Protein Serine-Threonine Kinases , Biochemistry , Non-competitive inhibition , In vivo , Nitriles , Drug Discovery , Butadienes , medicine , Animals , Enzyme Inhibitors , Molecular Biology , IC50 , Biotransformation , Transcriptional activity , Chemistry , Organic Chemistry , NF-kappa B , Dual-specificity kinase , Biological activity , Rats , Transcription Factor AP-1 , Mechanism of action , Cyclization , Molecular Medicine , medicine.symptom , Isomerization
الوصف:
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.
تدمد:
0960-894X
DOI:
10.1016/s0960-894x(98)00522-8
URL الوصول:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e6e7239bbbcdbe88ce04a2dcd87efb1e https://doi.org/10.1016/s0960-894x (98)00522-8
Rights:
CLOSED
رقم الانضمام:
edsair.doi.dedup.....e6e7239bbbcdbe88ce04a2dcd87efb1e
قاعدة البيانات:
OpenAIRE