Related Experiment Video
Updated: Feb 27, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Small molecules as activators in medicinal chemistry (2000-2016)
Abdul Hameed1, Mariya Al-Rashida2, Rima D Alharthy3
1a H. E. J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences , University of Karachi , Karachi , Pakistan.
This review explores patents on small molecule enzyme activators, highlighting their potential for treating diseases like cancer and Alzheimer's. These compounds offer structural insights for developing more effective therapeutic agents.
Area of Science:
- Medicinal Chemistry
- Drug Discovery
- Enzyme Activation
Background:
- Enhancing enzyme expression is therapeutically beneficial for ailments linked to low enzyme activity.
- Small molecule enzyme activators show potential in treating microbial infections, cancer, diabetes, metabolic disorders, and neurological conditions like Alzheimer's disease.
Purpose of the Study:
- To review patents detailing small molecules as enzyme activators.
- To provide structural leads for designing more potent enzyme activators.
Main Methods:
- Focuses on enzyme activators explored between 2000 and 2016.
- Analysis of patent literature describing small molecule enzyme modulators.
Main Results:
- Identified numerous small molecules investigated as enzyme activators.
- Provided structural insights for the development of novel therapeutic agents.
Conclusions:
- Modulating enzyme activity is a key goal in medicinal chemistry.
- While enzyme inhibitors are common, enzyme activators offer a therapeutic avenue for disorders with suppressed enzyme activity.
More Related Videos
11:44Cellular Membrane Affinity Chromatography Columns to Identify Specialized Plant Metabolites Interacting with Immobilized Tropomyosin Kinase Receptor B
Published on: January 19, 2022
06:26Nano-Differential Scanning Fluorimetry for Screening in Fragment-based Lead Discovery
Published on: May 16, 2021
Related Concept Videos
Structure-Activity Relationships and Drug Design
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...
Drug Discovery: Overview
Principles of Drug Action
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
Targets for Drug Action: Overview
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 Interaction: Agonist
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous...
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...