With the advent of high-throughput, structure-assisted and virtual screening, an argument could be made that every target is now druggable. However, with an estimated 600-1500 possible druggable genes related to disease, the bottleneck is a judicious target choice. Coupled with this is the choice of discovery strategy, target- vs. system-based. This course discusses the pharmacological techniques available to relate targets to therapeutic opportunity, apply new ideas to re-visit mined out or intractable targets, validation beyond targets (pathway-validation) and strategies to improve the 50% efficacy failure rate for new drug candidates.
Who Should Attend • Biologists involved in drug discovery • Medicinal chemists • Pharmacology students • Academic pharmacologists
Course Benefits • Gain new insights into state of the art ideas on drug targets and their association with therapeutic opportunities • Learn new tools to quantitatively assess molecular effects on drug targets • Learn how parameters from these methods can predict activity in all systems • Define new vistas around old targets to better define chemical targets for receptors
Course Topics • Systems- vs. target-based research • Validation examples of CCR5 HIV • Knock outs,Knock ins andDREADs • Drugging Orphans - current methods • Drugability vs. target choice • 50% efficacy failures: reasons why and ways forward • Target vs. pathway validatio andbiased signaling • Single vs. multiple target engagement (CNS multi-target drugs) • Target remits and criteria for new drugs • Prosecuting the genome (single genes vs. ‘nomic’ collections) • Drug re-purposing, mined-ou’ or intractable targets andother shots on goal • Virtual screening and conventional HTS