Related Experiment Video
Updated: Nov 21, 2025
12:08
Diagonal Method to Measure Synergy Among Any Number of Drugs
Published on: June 21, 2018
19.2K
Glycorandomization: A promising diversification strategy for the drug development.
Bharat Goel1, Nancy Tripathi1, Debaraj Mukherjee2
1Department of Pharmaceutical Engineering and Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi, 221005, Uttar Pradesh, India.
European Journal of Medicinal Chemistry
|January 18, 2021
Summary
Glycorandomization modifies natural products by attaching diverse sugars to enhance drug properties like solubility and efficacy. This versatile technique, using synthetic or chemoenzymatic methods, aids in discovering new therapeutics for various diseases.
Area of Science:
- Natural Product Chemistry
- Drug Discovery
- Glycoscience
Background:
- Glycosylation significantly impacts natural product properties, including solubility, mechanism of action, target recognition, and toxicity.
- Modifying sugar moieties offers a strategy to fine-tune these properties for therapeutic benefit.
Purpose of the Study:
- To review glycorandomization strategies as a tool in drug discovery and development.
- To discuss the fundamentals, types, and applications of glycorandomization in creating diverse natural product and small molecule libraries.
Main Methods:
- Glycorandomization involves attaching different sugar moieties to the aglycone of natural glycosides.
- Approaches include synthetic neoglycorandomization and chemoenzymatic methods (in vitro and in vivo).
- Enzymatic approaches leverage substrate flexibility of glycosyltransferases, with potential for genetic engineering.
Main Results:
- Glycorandomization improves pharmacokinetic (solubility) and pharmacodynamic profiles (mechanism of action, toxicity, target recognition) of parent compounds.
- The technique is versatile due to enzyme flexibility towards various sugar and aglycone substrates.
- Genetic engineering of enzymes can expand the diversity of glycorandomized libraries.
Conclusions:
- Glycorandomization is a promising technology for drug discovery, enhancing the therapeutic potential of natural products.
- It enables the creation of novel compounds with improved properties to address challenging disease states.
- This review highlights glycorandomization's role in developing advanced glycorandomized libraries for drug development.
Related Concept Videos
01:13Randomized Experiments
8.6K
The randomization process involves assigning study participants randomly to experimental or control groups based on their probability of being equally assigned. Randomization is meant to eliminate selection bias and balance known and unknown confounding factors so that the control group is similar to the treatment group as much as possible. A computer program and a random number generator can be used to assign participants to groups in a way that minimizes bias.
Simple randomization
Simple...
Simple randomization
Simple...
8.6K
01:24Dosage Regimen: Individualization
71
Individualization in dosing regimens is the customization of medication doses for individual patients. Its necessity arises from the goal of maximizing therapeutic benefits while minimizing risks. This approach is pivotal because human responses to drugs can vary widely; what is effective for one person may be inadequate or excessive for another. Interpatient (intersubject) variability refers to differences in drug responses between individuals, while intrapatient (intrasubject) variability...
71
01:26Drug Discovery: Overview
10.5K
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...
10.5K
01:27Pharmaceutical Alternatives: Polymorphic Form-Related and Particle Size-Related Therapeutic Nonequivalence
75
Changes in polymorphic forms can significantly influence the bioavailability of poorly soluble drugs. Although the FDA defines pharmaceutical equivalence based on having the same active ingredient, dosage form, and route of administration, it does not automatically disqualify products with different polymorphic forms. This means two products with different polymorphs can still be deemed pharmaceutically equivalent. However, polymorphic differences can affect properties like wettability,...
75
01:20Bioequivalence Experimental Study Designs: Completely Randomized and Randomized Block Designs
90
Body:Bioequivalence experimental study designs are crucial methodologies used in evaluating and comparing the bioavailability of different drug products. These designs are categorized into various types: completely randomized, randomized block, repeated measures, cross and carry-over, and Latin square designs.Completely randomized designs involve randomly allocating treatments to all subjects participating in the experiment. This allocation is achieved by assigning unique random numbers to...
90
01:28Structure-Activity Relationships and Drug Design
1.4K
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...
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...
1.4K