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Principles of Drug Targets Summary Lecture 1

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Principles of Drug Targets Summary Lecture 1

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  • September 11, 2022
  • 1
  • 2022/2023
  • Class notes
  • R. leurs
  • College 1
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Principles of drug targets
Important matter:
r.leurs@vu.nl (for questions)
Part A and B →1 t/m hoofdstuk 11 + assignments (self-signup) Medicinal chemistry book
↳ presentation Oct. 17h (as a group consisting of 3 students)
↳ online assignments hand in online (bonus point)

Drugs background:
1500 unique drugs at the moment (FDA)
80% Small molecules 20% biologicals
R&D process is long & complex
→ geld wordt niet terug gemaakt
safety & efficacy are the main issues
↳ doesn't translate to humans
quick development: experience, resources, power (around the world)
drug: Chemical substance used to prevent or cure a disease.
aspirine blokkeert cyclo-oxygenase
↳ cyclo-oxygenase usually breaks down
groups to get a more complex molecule
Naming a drug: anti-prostaglandines → like aspirine
drugs interfere with cellular communication
curare: (chemical compound) blocks (gives paralysis) chemical signals between nerve and muscle
cells
acetylcholine → agonist (gives a response)
curare → bonds at receptor, antagonist (no response)
↳ muscle relaxer during surgery
↳ since 1994 Rocuronium
cell membrane, very important is for drug insertation. Because of the hydrophobic and hydrophilic
tendencies. Without the cell membrane it would be hard for drugs to penetrate the cell.

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