Study of the interaction surface for the c-Src-imatinib complex by a molecular dicing technique.
With the beginning of the new millennium, a new and exciting era for cancer therapy has begun with the appearance of molecular targeted drugs. Imatinib is a clinically well-tolerated small molecule that exerts selective, dual inhibition of the transforming growth factor beta (TGFbeta) and platelet-derived growth factor (PDGF) pathways. Imatinib is also suggested as a chemopreventive for recurrent and metastatic malignancies. An interesting point to be clarified regarding the mechanism of imatinib is its interaction with c-Src. Fortunately, complexing of c-Src and imatinib has recently reported, which provides a basis for further study of the interactions between the two molecules. In the present study, the author used the technique named molecular dicing to study the interaction surface between the two molecules. Accordingly, the interaction surface in c-Scr and imatinib could be identified.
Wiwanitkit
Viroj
V
Department of Clinical Laboratory Medicine, Faculty of Medicine, Chulalongkorn University, Bangkok, Thailand 10330. wviroj@yahoo.com
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D001549:Benzamides; D019295:Computational Biology / Q000379:methods; D016391:Genes, src / Q000187:drug effects*; D006801:Humans; D000068877:Imatinib Mesylate; D010879:Piperazines / Q000737:chemistry / Q000494:pharmacology*; D025941:Protein Interaction Mapping; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D001549:Benzamides; D010879:Piperazines; D011743:Pyrimidines; D000068877:Imatinib Mesylate