The Gatekeeper: Friend or Foe in Identifying the Next Generation of Kinase Inhibitors
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...
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Veröffentlicht in: | ChemMedChem 2006-11, Vol.1 (11), p.1195-1196 |
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description | 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. |
doi_str_mv | 10.1002/cmdc.200600163 |
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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.</description><subject>antitumor agents</subject><subject>drug design</subject><subject>gatekeeper</subject><subject>inhibitors</subject><subject>Models, Molecular</subject><subject>mutation</subject><subject>Protein Kinase Inhibitors - chemistry</subject><subject>Protein Kinase Inhibitors - pharmacology</subject><subject>Protein-Tyrosine Kinases - antagonists & inhibitors</subject><issn>1860-7179</issn><issn>1860-7187</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkMFPIjEUhxujUdfdq0fTk7fB1-nQdrwZFCQqJi5kEy9Np31oFTrYDln57x0Cwb3tqS_p9_sOHyGnDDoMIL-wc2c7OYAAYILvkWOmBGSSKbm_u2V5RH6k9AZQFIqpQ3LEJEDJBRyTyfgV6cA0-I64wHhJ-9FjcLSOtF8j9YEOHYbGT1c-vNCmhUf42dABBoym8XWg9ZTe-WAS0mF49ZVv6ph-koOpmSX8tX1PyKR_M-7dZvePg2Hv6j6zXDGeYa66zFnoVtJJjqyyWDnpmCjb78KBlIXlEiuwhlvrBDPOKCzKSopctTt-Qs433kWsP5aYGj33yeJsZgLWy6SFYjmDcg12NqCNdUoRp3oR_dzElWag1yH1OqTehWwHZ1vzspqj-8a35Vqg3AB__QxX_9Hp3sN17195ttn61ODnbmviuxaSy67-Mxro7sMzH49_3-kn_gXiGI57</recordid><startdate>20061101</startdate><enddate>20061101</enddate><creator>Prien, Olaf</creator><general>WILEY-VCH Verlag</general><general>WILEY‐VCH Verlag</general><scope>BSCLL</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20061101</creationdate><title>The Gatekeeper: Friend or Foe in Identifying the Next Generation of Kinase Inhibitors</title><author>Prien, Olaf</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c3813-e2851dc05b7d73e1bcebd7d1693814d0774c37eb0ca3ccd61ada8e49b7628dc03</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2006</creationdate><topic>antitumor agents</topic><topic>drug design</topic><topic>gatekeeper</topic><topic>inhibitors</topic><topic>Models, Molecular</topic><topic>mutation</topic><topic>Protein Kinase Inhibitors - chemistry</topic><topic>Protein Kinase Inhibitors - pharmacology</topic><topic>Protein-Tyrosine Kinases - antagonists & inhibitors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Prien, Olaf</creatorcontrib><collection>Istex</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>ChemMedChem</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Prien, Olaf</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The Gatekeeper: Friend or Foe in Identifying the Next Generation of Kinase Inhibitors</atitle><jtitle>ChemMedChem</jtitle><addtitle>ChemMedChem</addtitle><date>2006-11-01</date><risdate>2006</risdate><volume>1</volume><issue>11</issue><spage>1195</spage><epage>1196</epage><pages>1195-1196</pages><issn>1860-7179</issn><eissn>1860-7187</eissn><abstract>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.</abstract><cop>Weinheim</cop><pub>WILEY-VCH Verlag</pub><pmid>17009360</pmid><doi>10.1002/cmdc.200600163</doi><tpages>2</tpages></addata></record> |
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source | Wiley-Blackwell Journals; MEDLINE |
subjects | antitumor agents drug design gatekeeper inhibitors Models, Molecular mutation Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Protein-Tyrosine Kinases - antagonists & inhibitors |
title | The Gatekeeper: Friend or Foe in Identifying the Next Generation of Kinase Inhibitors |
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