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Drug Discovery: Overview

Drug Discovery: Overview

Drug discovery is a multifaceted process involving extensive screening, testing, and optimization of lead compounds to identify potential new drugs for therapeutic use. It combines several approaches, including screening large numbers of natural products, chemical modification of known active molecules, identification of new drug targets, and rational design based on biological mechanisms and drug-receptor structure. These approaches are carried out in both academic research laboratories and...

Structure-Activity Relationships and Drug Design

Structure-Activity Relationships and Drug Design

Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
SAR studies the intricate relationship between a drug's chemical structure and biological activity. It focuses on understanding how modifications to a drug's structure can influence its...

Drug Biotransformation: Overview

Drug Biotransformation: Overview

Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...

Targets for Drug Action: Overview

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...

Drug-Receptor Interactions

Drug-Receptor Interactions

Drug-receptor interaction describes the binding of receptors by drugs, but not all drug-receptor interactions result in activation and tissue response. For instance, the binding of agonists activates the receptor to generate a cellular reaction, while antagonists bind to receptors without causing their activation.
Several parameters, such as the drug's affinity for its receptor and its efficacy, which is its ability to activate the receptor, determine the drug's effect on the tissue.

Quantitative Aspects of Drug-Receptor Interaction

Quantitative Aspects of Drug-Receptor Interaction

The receptor occupancy theory connects a drug's response to the number of occupied receptors. With higher drug concentrations, more receptors are occupied, leading to increased responses. The formation of drug-receptor complexes involves association and dissociation rates, which reach equilibrium when the forward and backward reactions are equal. The equilibrium association constant (Ka) and its inverse, the equilibrium dissociation constant (Kd), indicate drug affinity. Higher Ka and lower Kd...

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Related Experiment Video

Updated: Jun 21, 2026

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

Published on: December 1, 2020

Text-based information systems for drug discovery.

R Hull¹, A Jenkins, M Zweerink

¹RY86-205 Merck & Co Inc, Rahway, NJ 0706, USA.

Current Opinion in Drug Discovery & Development

|August 4, 2009

Summary

This summary is machine-generated.

Scientific breakthroughs can be lost if not effectively communicated. This highlights the risk of important research being overlooked amidst a flood of less significant publications, hindering scientific progress.

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A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English

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Last Updated: Jun 21, 2026

Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions

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Published on: December 1, 2020

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English

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Area of Science:

Genetics
Scientific Communication
History of Science

Background:

Gregor Mendel's foundational work on genetics was initially overlooked.
The loss of Mendel's research for a generation illustrates a recurring problem in science.

Purpose of the Study:

To analyze the historical impact of lost scientific publications.
To underscore the importance of effective dissemination of significant research findings.

Main Methods:

Historical analysis of Gregor Mendel's publication and its reception.
Conceptual framework for understanding the loss of scientific information.

Main Results:

Mendel's laws of inheritance remained undiscovered by the scientific community for decades.
Significant scientific advancements risk being lost due to poor visibility.

Conclusions:

The scientific community must develop better mechanisms for identifying and promoting crucial research.
Preventing the loss of significant scientific attainments is vital for continued progress.