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In diesem Kurs gibt es 3 Module
This course covers the stages of drug discovery in which promising compounds (leads) are identified, their optimal and suboptimal characteristics determined, and the suboptimal characteristics optimized to create a candidate suitable for the clinic. The course is built around a case study on the discovery of an antimalarial therapy. Assays useful for screening new compounds are outlined, examples of selection criteria for leads are discussed - such as potency, efficacy, and pharmacokinetics - and the structure activity relationships that contribute to the optimization of a lead series are considered. The phenotypic approach used by the antimalarial program will be briefly contrasted with a target-based program on a different target.
Target audience: This course is suitable for life scientists, clinicians, and individuals from fields that support drug discovery (e.g., patents, finance, licensing, etc.) interested in learning more about the pharmaceutical/biotechnology sector. Advanced undergraduate coursework or practical familiarity/working knowledge in biological sciences and organic chemistry is recommended.
Welcome, by the end of the course students will be able to: Recognize malaria as a neglected tropical disease and understand its significance as an unmet medical need. Identify and describe some of the characteristics an effective small molecule therapeutic should possess, and liabilities to avoid. Describe the principles and common approaches used in defining and optimizing a lead compound's pharmacophore.
Das ist alles enthalten
3 Videos2 Aufgaben
Infos zu Modulinhalt anzeigen
3 Videos•Insgesamt 23 Minuten
Course Welcome•1 Minute
Interview with Juliet Nabakka•16 Minuten
Malaria Life Cycle•6 Minuten
2 Aufgaben•Insgesamt 45 Minuten
Assessment•15 Minuten
Knowledge Check•30 Minuten
Lead Selection & Optimization, part 2
Modul 2•4 Stunden abzuschließen
Moduldetails
Das ist alles enthalten
6 Videos3 Lektüren6 Aufgaben
Infos zu Modulinhalt anzeigen
6 Videos•Insgesamt 30 Minuten
Pharmacophores and Lead Optimization•5 Minuten
Assays for Guiding Lead Optimization•5 Minuten
Hit Criteria and Characterization•4 Minuten
Composite Parameters in Discovery•5 Minuten
SAR of a Compound Series•5 Minuten
Optimization of ADME Properties•7 Minuten
3 Lektüren•Insgesamt 30 Minuten
Lipophilicity•10 Minuten
Homologous series•10 Minuten
Using isosteres to optimize ADME properties•10 Minuten
6 Aufgaben•Insgesamt 200 Minuten
Assessment
•50 Minuten
Knowledge Check•30 Minuten
Knowledge Check•30 Minuten
Knowledge Check•30 Minuten
Knowledge Check•30 Minuten
Knowledge Check•30 Minuten
Lead Selection & Optimization, part 3
Modul 3•3 Stunden abzuschließen
Moduldetails
Das ist alles enthalten
6 Videos1 Lektüre4 Aufgaben
Infos zu Modulinhalt anzeigen
6 Videos•Insgesamt 28 Minuten
In Vivo Pharmacokinetics•6 Minuten
A Target-Based Example - Complement Factor B Inhibitor•5 Minuten
Biomarkers•6 Minuten
In Vivo Pharmacology & Safety•5 Minuten
Discovery Story of KAF156•5 Minuten
Course Farewell•1 Minute
1 Lektüre•Insgesamt 10 Minuten
Using the Protein Data Bank to visualize compound-target cocrystals•10 Minuten
4 Aufgaben•Insgesamt 120 Minuten
Assessment•30 Minuten
Knowledge Check•30 Minuten
Knowledge Check•30 Minuten
Knowledge Check•30 Minuten
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Novartis is committed to empowering the next generation of healthcare leaders. These courses are designed to help learners contribute to healthcare research and community well-being.
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