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Forums Videos Market Live Videos All Blogs My Blogs Friends' Blogs Challenges of Small Molecule Targeted Drug Development Alex Venezuela Phone Number List Brown by Alex Brown 2018-03-03 10 Times Viewed the Classical Mode of Action of Small Molecule Drugs is Occupancy Driven. Since the Approval of the Tumor Targeted Therapy, Tamoxifen Targeting the Estrogen Receptor for the Treatment of Breast Cancer, the Development of Small Molecule Drugs Has Typically.
Focused on The the Screening of High Affinity Inhibitors. Small Molecule Inhibitors Can Bind to Either the Active Site or Allosteric Site of a Protein Thereby Abrogating Its Function. This is a Mode of Action Whereby Occupying a Specific Site on the Target Protein Drives the Loss of Protein Function. Small Molecule Inhibitors Face Two Major Challenges: Drug-resistant Mutations and Difficult-to-drug Targets. On the One Hand, Patients Who Respond to Small Molecule Inhibitors Will Eventually Develop Drug Resistance, Mainly Due to Drug-resistant Mutations. On the Other Hand, the Occupancy-driven Mode of Action Requires Clear Pocket Grooves on the Target Protein.