Covalent Inhibition in Drug Discovery.

摘要: Although covalent inhibitors have been used as therapeutics for more than a century, there has general resistance in the pharmaceutical industry against their further development due to safety concerns. This inclination recently reverted after of wide variety address human health conditions along with US Food and Drug Administration (FDA) approval several use humans. Along this exciting resurrection an old drug discovery concept, review surveys enzymes that can be targeted by treatment diseases. We focus on protein kinases, RAS proteins, few other studied extensively targets inhibition, aim challenges designing effective drugs provide suggestions area yet explored.