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THE PROCESS OF DRUG DISCOVERY (TPODD 1)
Answer BOTH parts of the question
Virtual screening against 5-hydroxytryptamine receptor (5-HT2C) resulted in a set of ten small molecules as potential agonists.
a) Discuss the key factors involved in the design and evaluation of CNS drugs and propose a strategy for selection of two compounds for further in vivo experiments. (60% of marks)
b) Propose the use of two commonly used methods for in vivo evaluation of their CNS penetration and provide the justification for this choice. (40% of marks)
Answer ALL parts of the question
A scientist in a biotech company believeshe has discovered a novel cell surface receptor with an important stimulatory role in cell division that might make it a good drug target in the treatment of renal cancer. His discovery was made in a kidney cell culture.
a) When trying to convince his project manager, what sort of properties must he demonstrate that the protein receptor possesses to be a good drug target? (25% of marks)
b) The scientist would like the company geneticist to carry out a Genome Wide Association Study (GWAS). Explain to his project manager what this would involve and what it might show. (25% of marks)
c) The scientist proposes to use his kidney cell culture to validate his receptor as a potential drug target. Explain with molecular detail TWO possible methods that the scientist might use. Highlight any difficulties and how they might be overcome. (50% of marks)