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Lecture

Identifying Drug Targets: Safety and Efficacy

In course

CH-332: Medicinal chemistry

Sitting at the crossroad of organic chemistry and medicine, this course outlines how an initial hit compound transitions into a lead candidate, and ultimately a drug, in the modern drug discovery world. Note: the course is held only during 2nd half of spr ...

Description

This lecture focuses on identifying correct drug targets, ensuring efficacy, and maintaining safety in medical chemistry. It covers topics such as the importance of genetic sufficiency tests, leveraging chirality for on-target responses, and the role of stereochemistry in drug action. Case studies, including the discovery of imatinib mesylate, illustrate key concepts. The discussion extends to the challenges of drug resistance, the impact of physicochemical properties on drug development, and the rules of 'drug-likeness' in compounds. Additionally, the lecture addresses safety concerns, structural alerts to avoid in drug design, and the importance of understanding differences between in vitro and in vivo efficacy.

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Instructor

Yimon Aye

Official source

Ontological neighbourhood

Chemistry

Physical chemistry: Stereochemistry

Related concepts (32)

Chirality (chemistry)

In chemistry, a molecule or ion is called chiral (ˈkaɪrəl) if it cannot be superposed on its by any combination of rotations, translations, and some conformational changes. This geometric property is called chirality (kaɪˈrælɪti). The terms are derived from Ancient Greek χείρ (cheir) 'hand'; which is the canonical example of an object with this property. A chiral molecule or ion exists in two stereoisomers that are mirror images of each other, called enantiomers; they are often distinguished as either "right-handed" or "left-handed" by their absolute configuration or some other criterion.

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.

Genetic testing

Genetic testing, also known as DNA testing, is used to identify changes in DNA sequence or chromosome structure. Genetic testing can also include measuring the results of genetic changes, such as RNA analysis as an output of gene expression, or through biochemical analysis to measure specific protein output. In a medical setting, genetic testing can be used to diagnose or rule out suspected genetic disorders, predict risks for specific conditions, or gain information that can be used to customize medical treatments based on an individual's genetic makeup.

Drug discovery

In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which new candidate medications are discovered. Historically, drugs were discovered by identifying the active ingredient from traditional remedies or by serendipitous discovery, as with penicillin. More recently, chemical libraries of synthetic small molecules, natural products or extracts were screened in intact cells or whole organisms to identify substances that had a desirable therapeutic effect in a process known as classical pharmacology.

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.

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