Nuclear receptors as target of new drug therapy
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Nuclear receptors as target of new drug therapy
- 1. NUCLEAR RECEPTORS FOR DEVELOPING NEW DRUG THERAPY By MD. HABIBUR RAHMAN, M.Pharm. Asst. Professor, Dept. of Pharmacology. Anurag Pharmacy College, Kodad, Nalgonda (Dt), A. P
- 6. How does Cell surface Receptor elicits its action: Cell Membrane Unbound Endogenous Activator (Agonist) of Receptor Inactive Cell Surface Receptor Extracellular Compartment Intracellular Compartment N.B : Receptors are Present in equilibrium state of active and inactive conformation. Agonists binds with the active conformations.
- 7. Extracellular Compartment Intracellular Compartment Cell Membrane Bound Endogenous Activator (Agonist) of Receptor Active Cell Surface Receptor Cellular Response
- 8. Cell Membrane Displaced Endogenous Activator (Agonist) of Receptor Inactive Cell Surface Receptor Extracellular Compartment Intracellular Compartment Bound Antagonist of Receptor (Drug) N.B: Antagonist binds to the inactive conformations of the receptor.
- 9. How does Enzyme Receptor elicit its action: Active Enzyme Substrate Product Cellular Function Inactive Enzyme Substrate Bound Enzyme Inhibitor (Drug)
- 11. How does Nuclear Receptor elicit its action: Intracellular Compartment Nucleus DNA Modulation of Transcription Active Nuclear Receptor Bound Endogenous Activator (Agonist) of Nuclear Receptor
- 13. Displaced Endogenous Activator (Agonist) of Nuclear Receptor Intracellular Compartment Nucleus DNA Bound Antagonist of Receptor (Drug) Inactive Nuclear Receptor In Cytosolic Compartment Inactive Nuclear Receptor In Nuclear Compartment
- 26. Gene transcription cartoon showing interactions of ligand/PPAR/RXR heterodimer with cofactors and basal transcription machinery(RNA Polymerase II).
- 40. Pathogenesis: Diet with high fat Bile acid ( Lithocholic acid) poorly reabsorbed A toxic metabolite in enterohepatic circulation High conc. In colon Induce DNA strand breakage, inhibit DNA repair enzyme Colon Cancer
- 41. Pharmacology of VDR in colon cancer Vit-D VDR LCA Catabolism of CYP3A, a target gene Increased detoxification of LCA and elimination Protection against colon cancer.