Drug Discovery, Design and Development

Practice flashcards covering key concepts from the lecture on Drug Discovery, Design and Development.

Drug Discovery

The process by which novel drugs are identified, formulated, and biologically tested before use in human patients.

Key Stages of Drug Discovery

Includes target discovery, validation, assay development, drug screening, and lead optimization.

Target Validation

Demonstrating that targeting a biological component counteracts disease or brings patient relief.

Lead Compound

Bioactive compound resulting from drug screening that shows the desired pharmacological properties.

Preclinical Stage

Involves in vitro and in vivo testing procedures before clinical trials.

Clinical Stage

Testing drug candidates in human subjects to determine efficacy and safety.

Phase I Trials

Study involving healthy human subjects to gather biological and safety data.

Phase II Trials

Pilot studies in small groups of diseased human subjects to establish efficacy and safety profile.

Phase III Trials

Large-scale studies in diseased human subjects to establish overall risk-benefit relationship.

Phase IV Trials

Post-market studies to monitor long-term health outcomes after drug approval.

Structure-Activity Relationship (SAR)

How chemical structures affect biological activity of compounds.

Structure-Property Relationship (SPR)

How drug-like physiochemical properties alter upon structural variation.

Lipinski's Rule of 5

A set of guidelines for predicting drug bioavailability based on chemical structure.

RNA Viruses

Viruses with RNA as genetic material, can be either single-stranded or double-stranded.

Haemagglutinin

A viral glycoprotein crucial for influenza virus adsorption to host cells.

Neuraminidase

An enzyme in the influenza virus that cleaves sialic acid from glycoproteins to release new virions.

Prodrugs

Compounds that become active only after metabolic conversion in the body.

High Throughput Screening (HTS)

An automated process used to evaluate the bioactivity of many compounds against a target.

Target Discovery

The process of identifying biological components involved in a disease for drug targeting.

Assay Development

Development of analytical processes/models for testing compounds.

Lead Optimization

The iterative process of modifying lead compounds to improve drug properties.

Combinatorial Chemistry

A method for synthesizing large libraries of related compounds from chemical building blocks.

Phenotypic Screening

Testing biological responses to compounds without known drug targets.

Target-Based Screening

Screening based on known targets to identify compounds with desired activity.

Drug-Like Properties

Characteristics that enable effective absorption, distribution, metabolism, elimination, and low toxicity.

Isosteres

Atoms/groups with similar properties substituting in a compound without altering its function.

Bioisosteres

Structurally similar groups that impart similar biological properties to a chemical compound.

SAR Studies

Research focused on determining the relationship between chemical structure and biological activity.

Synthetic Feasibility

The practicality and ease of synthesizing a compound or its analogues.

Simplification

The process of making a complex drug structure easier to synthesize and potentially more effective.

Rigidification

The process of restricting the flexibility of a compound to enhance binding interactions.

Natural Product Derivative

A compound derived from natural sources that is chemically modified.

Alkyl Substitution

The replacement of hydrogen in a compound with alkyl groups to enhance properties.

Synthetic Modifications

Chemical changes made to improve the effectiveness or safety of a compound.

Viral Glycoproteins

Proteins on the surface of viruses that play key roles in infection and immune evasion.

Drug Screening

The process of testing compounds against biological targets to identify potential drug candidates.

Medicinal Chemistry

The branch of chemistry focused on the design, synthesis, and development of drugs.

Pharmacophore

The ensemble of steric and electronic features necessary for a drug to interact with its target.

In Vitro Assays

Experiments conducted in a controlled environment outside of a living organism.

In Vivo Assays

Experiments conducted in live organisms to evaluate drug effects.

Dosing Data

Information regarding the amount and frequency of drug administration needed for efficacy.

Modern Drug Development

The contemporary approach involving multi-disciplinary collaboration to create new medications.

Drug Target Interaction

The specific interaction between a drug and its biological target, influencing pharmacological activity.

CYP Enzymes

A family of enzymes involved in drug metabolism, playing a key role in pharmacokinetics.

Accurate Binding Assay

Tests designed to measure the binding interaction between a drug and its target.

Safety Profile

The comprehensive assessment of a drug's safety at various doses in clinical trials.

Efficacy

The ability of a drug to produce a desired therapeutic effect.

Long-Term Safety Studies

Research conducted to establish the lasting effect of drugs post-approval.