Lecture

Enzyme Drug Targets

Graph Chat

Chat with Graph Search

Ask any question about EPFL courses, lectures, exercises, research, news, etc. or try the example questions below.

DISCLAIMER: The Graph Chatbot is not programmed to provide explicit or categorical answers to your questions. Rather, it transforms your questions into API requests that are distributed across the various IT services officially administered by EPFL. Its purpose is solely to collect and recommend relevant references to content that you can explore to help you answer your questions.

Description

This lecture covers the importance of enzymes as drug targets, focusing on examples such as cyclooxygenases, dihydrofolate reductase, protein kinase C, tyrosine kinases, GABA transaminase, HIV aspartyl protease, and angiotensin-converting enzyme. It explains the development of molecules targeting these enzymes and the specificity of inhibitors. The lecture also discusses the role of tyrosine kinase inhibitors in cancer treatment, with a spotlight on imatinib. Furthermore, it delves into the control of vascular smooth muscle tone, the renin-angiotensin system, and the synthesis of vasoconstrictor Angiotensin II. The session concludes with insights into the viral life cycle, pharmacological interventions, and the development of ritonavir through structure-based drug design.

Official source

Related concepts (23)

Drug design

Drug design, often referred to as rational drug design or simply rational design, is the inventive process of finding new medications based on the knowledge of a biological target. The drug is most commonly an organic small molecule that activates or inhibits the function of a biomolecule such as a protein, which in turn results in a therapeutic benefit to the patient. In the most basic sense, drug design involves the design of molecules that are complementary in shape and charge to the biomolecular target with which they interact and therefore will bind to it.

Drug development

Drug development is the process of bringing a new pharmaceutical drug to the market once a lead compound has been identified through the process of drug discovery. It includes preclinical research on microorganisms and animals, filing for regulatory status, such as via the United States Food and Drug Administration for an investigational new drug to initiate clinical trials on humans, and may include the step of obtaining regulatory approval with a new drug application to market the drug.

Biological target

A biological target is anything within a living organism to which some other entity (like an endogenous ligand or a drug) is directed and/or binds, resulting in a change in its behavior or function. Examples of common classes of biological targets are proteins and nucleic acids. The definition is contcan refer to the biological target of a pharmacologically active drug compound, the receptor target of a hormone (like insulin), or some other target of an external stimulus.

Tyrosine kinase

A tyrosine kinase is an enzyme that can transfer a phosphate group from ATP to the tyrosine residues of specific proteins inside a cell. It functions as an "on" or "off" switch in many cellular functions. Tyrosine kinases belong to a larger class of enzymes known as protein kinases which also attach phosphates to other amino acids such as serine and threonine. Phosphorylation of proteins by kinases is an important mechanism for communicating signals within a cell (signal transduction) and regulating cellular activity, such as cell division.

Drug delivery

Drug delivery refers to approaches, formulations, manufacturing techniques, storage systems, and technologies involved in transporting a pharmaceutical compound to its target site to achieve a desired therapeutic effect. Principles related to drug preparation, route of administration, site-specific targeting, metabolism, and toxicity are used to optimize efficacy and safety, and to improve patient convenience and compliance. Drug delivery is aimed at altering a drug's pharmacokinetics and specificity by formulating it with different excipients, drug carriers, and medical devices.

Related lectures (37)

Selective Drug Targeting Mechanisms

Explores selective drug targeting mechanisms, resistance development, tuberculosis incidence, BCR-ABL mutations, tyrosine kinase inhibitors, drug toxicity, interactions, and toxicology studies.

Protein-Protein Interaction Networks

Explores protein-protein interaction networks, binding importance, experimental approaches, drug target identification, and network construction.

Pharmacology: Drug Targets and Mechanisms

Discusses ligand-receptor binding, drug targets, insulin physiology, NSAIDs, and tyrosine kinase inhibitors.

Fragment-Based Drug Discovery: Concepts & Technologies

Covers the concepts and technologies of fragment-based drug discovery, exploring hit identification, lead optimization, and screening methods.

Pharmacological Targets and Interventions