作者: Ariel Fernandez , Alejandro Crespo
DOI: 10.2741/2338
关键词:
摘要: Molecularly targeted treatment of malignancy requires a careful control drug specificity. We review recent advances in this area focusing on particular marker for ligand-target associations: the poorly wrapped hydrogen bond or dehydron, packing defect protein target. Dehydrons promote their own dehydration and are generally not conserved across homologs. Thus, so-called "wrapping technology" is geared at enhancing specificity by developing ligands that can contribute exogenously to shield dehydrons from water attack. This type design guided an analysis interfaces assessment environmental changes around preformed bonds occurring upon association. Dehydron differences a-priori targets have been exploited redesign drugs order enhance selectivity. Tested wrapping modifications established cancer reviewed. The rationally directed impact prototype compounds points broad applicability technology, ultimately leading molecular therapies with tighter side effects. New perspectives progression using technology outlined. In particular, we discuss future strategy develop highly selective inhibitors targeting signaling complex critical metastasis.