Four Major Protein Targets for Drugs - Edubirdie

University:
Western Sydney University
Course:
MEDI 2003 | Clinical Sciences 2
Academic year:

2024
Views:

231

Pages:

3
Author:

Mariam A. A.

Four major protein targets for drugs 1. Receptors 2. Carrier molecules (Transporters) 3. Ion channels (bind or move target molecules) 4. Enzymes (convert substrates into products) Four major protein drug targets • • • • • • • • A direct effect Pro drug needs to be converted into an active drug by the enzyme Receptors Receptors are complex macromolecules to which endogenous mediators (e.g., hormones, neurotransmitters) bind and initiate changes in cellular function Most receptors are embedded in cell membranes All receptors that exist in the organism have physiologic roles, and no receptor has been specifically ‘allocated’ for drugs Can be water soluble or fat soluble (fatty acids, vitamin D, steroids etc.) Most are membrane bound but you can find some bound to nucleus and Some drugs can cause adverse effects because they are not very specific can bind to multiple things. Ligand binding to a receptor initiates signals inside the cell Signal Transduction involving Gs -proteins • When bonds causes a confirmational change in the receptor • The a, b and y become stabilised such leads to fragmentation Agonists • • Agonists are chemicals that bind and activate receptors Two types: Endogenous agonists (physiological compounds) - Drug agonists (mimic the action of endogenous agonists) Antagonists • Antagonists are compounds that bind but do NOT activate receptors -> (often called blockers) - Antagonists reduce or block the action of endogenous agonists by preventing their attachment to receptors or by displacing already attached agonists

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