Turning promiscuous kinase inhibitors into safer drugs

作者: Xi Zhang , Alejandro Crespo , Ariel Fernández

DOI: 10.1016/J.TIBTECH.2008.02.008

关键词:

摘要: Burgeoning interest in multi-target drugs to treat complex diseases and malignancies has motivated a reassessment of the therapeutic value promiscuity. Although drug efficacy might not correlate with specificity, it would be risky welcome promiscuous compounds without rational strategy control impact. This situation change as novel selectivity filters are incorporated into design. For example, cardiotoxic side effects cancer imatinib curbed by applying such premises. Here, we survey approaches impact cross-reactive kinase inhibitors advocate application filter illustrating its cleaning efficacy. Finally, evaluate possibility turning clinical opportunities through judicious chemical modifications.

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