alexa Small molecular weight inhibitors of stress-activated and mitogen-activated protein kinases.


Journal of Clinical & Cellular Immunology

Author(s): Malemud CJ

Abstract Share this page

Abstract The stress-activated protein kinase (SAPK) and mitogen-activated protein kinase (MAPK) sub-families are crucial to environmental stress responses and responses to growth factors that cause transcriptional activation of genes required for cell proliferation, differentiation and programmed cell death. Small molecular compounds with specific structure/activity characteristics have been developed that competitively block SAPK/MAPK binding to ATP. Chemically modified compounds based on ATP binding pocket characteristics have improved selectivity and specificity for SAPK/MAPK isoforms. In addition, site-specific mutagenesis of MAPKs has helped identify the MAPK structures required for binding recognition and selectivity of these inhibitors. A group of extracellular-signal regulated protein kinase (ERK) inhibitors has been constructed based almost exclusively on their ability to inhibit the ERK activation cascade. Inhibitors have been employed in vitro to identify protein targets and mechanism of action of SAPKs/MAPKs. The efficacy of SAPK/MAPK inhibitors in animal models of inflammation, arthritis, heart failure, cancer and neurological degeneration has provided the impetus for using them in human studies of inflammation and in clinical trials.
This article was published in Mini Rev Med Chem and referenced in Journal of Clinical & Cellular Immunology

Relevant Expert PPTs

Relevant Speaker PPTs

Recommended Conferences

Relevant Topics

Peer Reviewed Journals
Make the best use of Scientific Research and information from our 700 + peer reviewed, Open Access Journals
International Conferences 2017-18
Meet Inspiring Speakers and Experts at our 3000+ Global Annual Meetings

Contact Us

© 2008-2017 OMICS International - Open Access Publisher. Best viewed in Mozilla Firefox | Google Chrome | Above IE 7.0 version