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High Throughput Screening for Novel Anti-Inflammatories pp 165–191Cite as

Birkhäuser

Inhibitors of the MAPK pathway

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Part of the book series: Progress in Inflammation Research ((PIR))

Abstract

The mitogen-activated protein kinase (MAPK) family of protein kinases is a series of three highly conserved protein kinases arrayed in a cascade. Members of this family are proline-directed serine/threonine kinases that are activated by dual-phosphorylation. MAPK belong to the rapidly growing family of mammalian protein kinases. Less than 200 mammalian protein kinases were known in 1994. As of 1998, more than 700 distinct mammalian protein kinases have been identified by genomic technologies and estimates are that the human genome encodes around 2000 protein kinases. MAPK impact many cellular processes such as proliferation, oncogenesis, development and differentiation, cell cycle and cell death [1—4],. Selective inhibition of signal transduction processes has been considered by many pharmaceutical companies as an approach to disease management [5]. Two of the best-characterized anti-inflammatory drugs in patients, rapamycin and cyclosporin, act by directly affecting protein phosphorylation. Multiple clinical trials are underway with specific kinase inhibitors, in particular PKC and tyrosine kinase inhibitors. Therefore, targeting MAPK with therapeutics may be an effective way for treating a large number of diseases. This chapter will review the current field of biological and small molecule inhibitors of MAPKs. The authors recommend as starting point the following reviews on inhibitors of protein kinases [6—15].

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Authors and Affiliations

  1. Signal Pharmaceuticals Inc., 5555 Oberlin Drive, San Diego, CA, 92121, USA

    Brion W. Murray, Yoshitaka Satoh & Bernd Stein

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  1. Brion W. Murray
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  2. Yoshitaka Satoh
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  3. Bernd Stein
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  1. Department of Pathobiology, SC-38, University of Washington, Seattle, WA, 98195, USA

    Michael Kahn

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Murray, B.W., Satoh, Y., Stein, B. (2000). Inhibitors of the MAPK pathway. In: Kahn, M. (eds) High Throughput Screening for Novel Anti-Inflammatories. Progress in Inflammation Research. Birkhäuser, Basel. https://doi.org/10.1007/978-3-0348-8462-4_9

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  • DOI: https://doi.org/10.1007/978-3-0348-8462-4_9

  • Publisher Name: Birkhäuser, Basel

  • Print ISBN: 978-3-0348-9578-1

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