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Once a person understands the ideas of drug efficacy, potency, pharmacokinetics, and safety, original research articles can be readily understood. The Journal of Medicinal Chemistry of the American Chemical Society regularly publishes a series of articles called Drug Annotations. These articles summaries a drug discovery program from a pharmaceutical company. The article covers everything from the indication of the drug, key pathways and promising drug targets within the pathways, library screening, lead selection, lead optimization, and both preclinical safety and PK/ADME studies. The articles are excellent articles for students who are testing their knowledge of drug discovery.
In this course about drug discovery case studies, students will read five different Drug Annotations articles. Each article will require approximately two hours to read thoroughly and fully process. Including assessment questions based on the articles, the full course should require no more than 15 hours of effort.
Students in the course should understand lead selection, lead optimization, pharmacodynamics, drug activity, pharmacokinetics, and preclinical safety. A fundamental understanding of the structure of organic molecules and their functional groups is also required. The course has no structure beyond having a module for each case study article. A handful of 10-15-minute videos with discussions of other Drug Annotation articles are provided for reference. Each module provides a link to the open access article on the Journal of Medicinal Chemistry website.
Students signed up for the Audit Track have access to the links to the case studies and the sample Drug Annotation article videos. Students enrolled through the Verified Track also have access to assessment questions.
Students will learn about several drug programs in the pharmaceutical industry…
AZD4831 – a compound that reduces incidence of heart failure
MRTX0902 – a compound with anti-tumor activity
pritelivir – a compound that treats herpes simplex virus infections
reldesemitiv -a compound that treats impaired muscle function
sebetralstat – a compound that treats hereditary angioedema
case study 1: Discovery of AZD4831, a mechanism-based irreversible inhibitor of myeloperoxidase, as a potential treatment for heart failure with preserved ejection fraction
case study 2: Design and discovery of MRTX0902, a potent, selective, brain-penetrant, and orally bioavailable inhibitor of the SOS1:KRAS protein−protein interaction
case study 3: Discovery, chemistry, and preclinical development of pritelivir, a novel treatment option for acyclovir-resistant herpes simplex virus infections
case study 4: Discovery of reldesemtiv, a fast skeletal muscle troponin activator for the treatment of impaired muscle function
case study 5: Sebetralstat (KVD900): a potent and selective small molecule plasma kallikrein inhibitor featuring a novel P1 group as a potential oral on-demand treatment for hereditary angioedema
