Enzymes and Drug Discovery Overview

Enzymes and Drug Discovery

• Enzymes are crucial components in metabolic pathways.
• Understanding enzyme function and regulation is fundamental in drug development.
• Scientists collaborate to design drugs.

Example Drugs and Their Targets

• Statins reduce cholesterol levels by inhibiting HMG-CoA reductase, the enzyme that synthesizes cholesterol.
• Acetaminophen (Tylenol) inhibits cyclooxygenase, an enzyme involved in fever and inflammation, although its exact mechanism is not fully understood.
• A drug's target is the specific molecule it acts upon.

Drug Discovery Process

• Identifying a drug target is a major challenge in drug discovery.
• Drug targets are identified through laboratory research.
• Understanding how the target acts inside cells and how disease affects reactions is crucial.
• Drug design involves chemists and biologists collaborating to synthesize molecules that either block or activate target reactions.
• Potential drugs undergo numerous tests (in vitro to clinical trials) before FDA approval.

Enzyme Cofactors and Coenzymes

• Many enzymes require specific helper molecules (non-protein) for optimal function.
• Binding can be temporary (ionic/hydrogen bonds) or permanent (covalent bonds).
• Cofactors are inorganic ions (iron, magnesium).
• Coenzymes are organic molecules (carbon and hydrogen based).
• Coenzymes participate in reactions without being changed and are recycled.
• Vitamins are the source of coenzymes. Some are direct coenzymes, while others are precursors.
• Vitamin C is a direct coenzyme for certain enzymes involved in collagen production.
• Enzyme function is influenced by cofactor/coenzyme availability, which can be affected by diet or organismal production.