structural elucidation of the dfg-asp in and dfg-asp out states of tam kinases and insight into the selectivity of their inhibitors
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ID: 213590
2014
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Abstract
Structural elucidation of the active (DFG-Asp in) and inactive (DFG-Asp out) states of the TAM family of receptor tyrosine kinases is required for future development of TAM inhibitors as drugs. Herein we report a computational study on each of the three TAM members Tyro-3, Axl and Mer. DFG-Asp in and DFG-Asp out homology models of each one were built based on the X-ray structure of c-Met kinase, an enzyme with a closely related sequence. Structural validation and in silico screening enabled identification of critical amino acids for ligand binding within the active site of each DFG-Asp in and DFG-Asp out model. The position and nature of amino acids that differ among Tyro-3, Axl and Mer, and the potential role of these residues in the design of selective TAM ligands, are discussed.
| Reference Key |
messoussi2014moleculesstructural
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| Authors | ;Abdellah Messoussi;Lucile Peyronnet;Clémence Feneyrolles;Gwénaël Chevé;Khalid Bougrin;Aziz Yasri |
| Journal | Journal of ethnopharmacology |
| Year | 2014 |
| DOI |
10.3390/molecules191016223
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