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The Gatekeeper: Friend or Foe in Identifying the Next Generation of Kinase Inhibitors
Author(s) -
Prien Olaf
Publication year - 2006
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200600163
Subject(s) - kinase , context (archaeology) , small molecule , computational biology , pharmacology , cancer research , biology , medicine , chemistry , genetics , paleontology
Fighting cancer: The next generation of small‐molecule kinase inhibitors might be designed against distinct mutational forms of certain kinases. Current antitumor drugs display remarkable efficacy, but relapse is frequently observed during treatment due to acquired mutation. The gatekeeper plays an important role in this context, and compounds such as 1 that interact with it might be a starting point to design future inhibitors.