This course describes the conversion of ‘descriptive’ (what we see) data in test systems to ‘predictive’ scales that are system independent and can be used to predict therapeutic activity.
Because drugs interact with ongoing physiology in the body, activity can be difficult to predict in therapeutic situations from single estimates of activity in test systems. The main (50%) reason for new drug candidate failure is lack of efficacy. The premise of this course is that pharmacology can now be used to yield more detailed and accurate profiles of drug efficacy that can be used to link activity in the clinic and also provide a better roadmap for follow-up candidates should molecules fail in the clinic.
Medicinal and synthetic organic chemists, biologists involved in drug development, any scientist involved in process of drug discovery, production and approval.
Lecture 1: The four (4) critical parameters needed to describe all drug action: Affinity, efficacies, Allosteric vs Orthosteric interaction, kinetics target offset.
Lecture 2: Receptors: Cell response activation (agonists), concept of efficacy, predicting agonism in all tissues, biased signaling
Lecture 3: Receptors: Antagonists: measurement of equilibrium dissociation constants for antagonist-receptor interaction, inverse agonism
Lecture 4: Allosterism and alteration of large Protein-protein interactions: quantification of cooperativity for affinity (a effect) and efficacy (b effect)
Lecture 5: Kinetics: measurement of real time kinetics and prediction of target coverage in vivo
Lecture 6: Enzyme inhibition: Measurement of competitive, non-competitive, uncompetitive and mixed enzyme inhibition; differentiation of mechanism
Five for four! Register five people for one course, one person for five courses, or any combination in between and your fifth registration is free. The free registration will be the course of the lowest price. Please note: This discount cannot be combined with any other discount offered.
Each person attending must register individually for this course.
Course fee includes electronic access to the course materials and session recordings.
Dr. Terry Kenakin is Professor of Pharmacology at the University of North Carolina School of Medicine. He is the author of 11 books on Pharmacology.