Modern drug discovery Flashcards
(7 cards)
What are the main advances and technologies in modern pharm?
High-throughput screening (HTS) to test thousands of compounds.
Structural biology and bioinformatics for target-based drug design.
Improved preclinical models and computational chemistry
What is target identification, target validation, starting molecule/compound,ligand based discovery and structured based discovery?
Target Identification: Finding a biomolecule linked to disease.
Target Validation: Confirming that modifying the target affects disease.
Starting Molecule/Compound: Initial chemical structure with potential activity.
Ligand-Based Discovery: Designing drugs based on known ligands.
Structure-Based Discovery: Using 3D structures of targets to design drugs.
What is sar cycling , lead compound , lead optimisation and a preclinical development candidate?
SAR Cycling: Modifying structure-activity relationships to improve drug properties.
Lead Compound: Optimised molecule with desired biological activity.
Lead Optimisation: Refining lead compounds for potency, safety, and bioavailability.
Preclinical Development Candidate: Final optimised compound for preclinical testing.
What are the principles of safety and efficacy in preclinical development?
Preclinical Development: Tests for safety, toxicity, and efficacy in animal models.
What are the four stages of clinical trials and what do they test for?
Clinical Trials:
Phase I: Safety in healthy volunteers.
Phase II: Efficacy in small patient groups.
Phase III: Large-scale testing for safety and efficacy.
Post-Market Surveillance: Monitors long-term safety and rare side effects.
what is propanol rational drug design?
Propranolol: First beta-blocker; designed to target β-adrenergic receptors, reducing heart rate and blood pressure.
What is citemetidine rational drug design?
Cimetidine: Histamine H2-receptor antagonist; blocks acid secretion in the stomach, used to treat ulcers.
