2 Major Different Mechanisms of Antagonism | Western Sydney University - Edubirdie

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

2024
Views:

251

Pages:

3
Author:

Mariam A. A.

2 major different mechanisms of Antagonism (the same principles apply to enzymes) Competitive antagonist: Antagonist binds to the ligand binding site Non-competitive: Antagonist binds to different site from ligand binding site (but by binding there distorts the receptor shape so that the ligand binding site is blocked) • Reversible vs. irreversible: A reversible antagonist can be "bumped off" the active site (e.g by an excess of agonist) - An irreversible antagonist is a type of antagonist that binds permanently to a receptor, either by forming a covalent bond to the active site, or alternatively just by binding so tightly that the rate of dissociation is effectively zero. Example: Tubocurarine, an antagonists for the nicotinic acetylcholine receptor SAQ Tubocurarine is an antagonist for the nicotinic acetylcholine receptor. What type of agonists is it? What would the physiological effect of exposure be? Why is a good poison? Drugs that Act on Enzymes • Drugs may act on enzymes in form of competitive and non-competitive inhibition - competitive inhibition - a drug acts as a substrate analogue to reversibly block enzyme’s active site and thus inhibit the biochemical process non-competitive inhibition - a drug binds to a site different from the enzyme indirectly blocking its function Competitive vs non-competitive Inhibition (in most cases reversible) Irreversible inhibition (can be competitive or non-competitive) – example: Muscle contraction • • Organic phosphates (poisons like nerve gases) are irreversible inhibitors of acetylcholine esterase Irreversible inhibition occurs by covalent adduct formation to the serine in the active site Other irreversible enzyme inhibitors used in medicine Aspirin, also known as acetylsalicylic acid (ASA), reduces blood clotting, inflammation, fever and pain, is a irreversible inhibitor of cyclooxygenase (COX).

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