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  • https://chem.libretexts.org/Courses/CSU_Chico/CSU_Chico%3A_CHEM_451_-_Biochemistry_I/CHEM_451_Test/08%3A_Transport_and_Kinetics/8.4%3A_Enzyme_Inhibition/C6._Agonist_and_Antagonist_of_Ligand_Binding_to_Receptors_-_An_Extension
    The analysis of competitive, uncompetitive and noncompetitive inhibitors of enzymes can now be extended to understand how the activity of membrane receptors are affected by the binding of drugs. Drugs...The analysis of competitive, uncompetitive and noncompetitive inhibitors of enzymes can now be extended to understand how the activity of membrane receptors are affected by the binding of drugs. Drugs targeted to membrane receptors can have a variety of effects. They may elicit the same biological effects as the natural ligand. If so, they are called agonists. Conversely they may inhibit the biological activity of the receptor. If so they called antagonists
  • https://chem.libretexts.org/Courses/CSU_Chico/CSU_Chico%3A_CHEM_451_-_Biochemistry_I/CHEM_451_Test/07%3A_Binding/7.5%3A_New_Methods_in_Drug_Development/E1._Introduction_to_Drug_Development
    Drugs can be designed to inhibit enzymes or to bind to sites on receptors (either in the membrane or the cytoplasm). When bound to a receptor, the drug ligand may mimic the natural ligand and lead to ...Drugs can be designed to inhibit enzymes or to bind to sites on receptors (either in the membrane or the cytoplasm). When bound to a receptor, the drug ligand may mimic the natural ligand and lead to expression of the biological activity of the receptor. In this case, the drug is an called an agonist of the normal ligand. In general, if the drug inhibits the activity of the bound receptor, the drug is called an antagonist.
  • https://chem.libretexts.org/Bookshelves/Biological_Chemistry/Supplemental_Modules_(Biological_Chemistry)/Pharmaceuticals/Drug_Receptor_Interactions
    Drugs interact with receptor sites localized in macromolecules which have protein-like properties and specific three dimensional shapes. A minimum three point attachment of a drug to a receptor site i...Drugs interact with receptor sites localized in macromolecules which have protein-like properties and specific three dimensional shapes. A minimum three point attachment of a drug to a receptor site is required. In most cases a rather specific chemical structure is required for the receptor site and a complementary drug structure. Slight changes in the molecular structure of the drug may drastically change specificity.

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