Jove
Visualize
Contact Us
JoVE
x logofacebook logolinkedin logoyoutube logo
ABOUT JoVE
OverviewLeadershipBlogJoVE Help Center
AUTHORS
Publishing ProcessEditorial BoardScope & PoliciesPeer ReviewFAQSubmit
LIBRARIANS
TestimonialsSubscriptionsAccessResourcesLibrary Advisory BoardFAQ
RESEARCH
JoVE JournalMethods CollectionsJoVE Encyclopedia of ExperimentsArchive
EDUCATION
JoVE CoreJoVE BusinessJoVE Science EducationJoVE Lab ManualFaculty Resource CenterFaculty Site
Terms & Conditions of Use
Privacy Policy
Policies

Related Concept Videos

Regulation of Metabolism01:19

Regulation of Metabolism

9.9K
Cellular needs and conditions vary from cell to cell and change within individual cells over time. For example, the required enzymes and energetic demands of stomach cells are different from those of fat storage cells, skin cells, blood cells, and nerve cells. Furthermore, a digestive cell works much harder to process and break down nutrients during the time that closely follows a meal compared with many hours after a meal. As these cellular demands and conditions vary, so do the amounts and...
9.9K
Allosteric Regulation01:08

Allosteric Regulation

59.3K
Allosteric regulation of enzymes occurs when the binding of an effector molecule to a site that is different from the active site causes a change in the enzymatic activity. This alternate site is called an allosteric site, and an enzyme can contain more than one of these sites. Allosteric regulation can either be positive or negative, resulting in an increase or decrease in enzyme activity. Most enzymes that display allosteric regulation are metabolic enzymes involved in the degradation or...
59.3K
Factors Affecting Drug Biotransformation: Biological01:19

Factors Affecting Drug Biotransformation: Biological

261
Biological factors significantly impact drug metabolism, influencing drug clearance, efficacy, and potential toxicity.
Species differences: Variations in enzyme systems across species can cause disparities in drug metabolism. For instance, humans may metabolize certain drugs faster than rodents, altering therapeutic effects.
Strain differences: Genetic variations within a species can result in differing enzyme activity, impacting drug response and toxicity. For example, some mouse strains may...
261
RNA Editing02:23

RNA Editing

9.2K
RNA editing is a post-transcriptional modification where a precursor mRNA (pre-mRNA) nucleotide sequence is changed by base insertion, deletion, or modification. The extent of RNA editing varies from a few hundred bases, in mitochondrial DNA of trypanosomes, to a just single base, in nuclear genes of mammals. Even a single base change in the pre-mRNA can convert a codon for one amino acid into the codon for another amino acid or a stop codon. This type of re-coding can significantly affect the...
9.2K

You might also read

Related Articles

Articles linked to this work by shared authors, journal, and citation graph.

Sort by
Same author

A 24-Day MicroCycle Journey to Interleukin-17 Inhibitors: From Library Design to Central Core Prioritization and Capping Group Identification.

ChemMedChem·2026
Same author

Acute gastropericardial fistula with cardiac tamponade and septic pericarditis due to <i>Helicobacter pylori</i>-induced gastric ulcer perforation.

JTCVS techniques·2026
Same author

Is splenic artery embolization beneficial when splenic angiography is negative? A multicenter observational study.

The journal of trauma and acute care surgery·2026
Same author

Molecules in Wikipedia: Analysis of Their Chemical Diversity, Functional Roles, and Popularity.

Journal of chemical information and modeling·2025
Same author

Spirocyclopentane as a Novel Scaffold for Potent Ghrelin Receptor Full Agonists.

Journal of medicinal chemistry·2025
Same author

Characterizing Treatment Patterns and Healthcare Use in Patients and Subgroups with Chronic Inflammatory Demyelinating Polyradiculoneuropathy: A Real-World Study.

Neurology and therapy·2025
Same journal

Design, synthesis, and biological evaluation of HSP70-mediated HEMTACs as novel androgen receptor degraders.

European journal of medicinal chemistry·2026
Same journal

Design, synthesis, and anti-SARS-CoV-2 activity of vilazodone derivatives as METTL3 inhibitors.

European journal of medicinal chemistry·2026
Same journal

Fully synthetic arecoline and arecaidine vaccine candidates with α-Galactosylceramide as built-in adjuvant.

European journal of medicinal chemistry·2026
Same journal

GPR120/free fatty acid receptor 4 (FFAR-4) agonists, antagonists, allosteric modulators: Computational drug design and discovery review.

European journal of medicinal chemistry·2026
Same journal

The development of novel ferrocenyl quinoline-benzimidazole molecular hybrids against cutaneous leishmaniasis.

European journal of medicinal chemistry·2026
Same journal

2-Pyridone as privileged scaffold: Advances in drug design and structural modification.

European journal of medicinal chemistry·2026
See all related articles

Related Experiment Video

Updated: Sep 21, 2025

In Ovo Feeding of Commercial Broiler Eggs: An Accurate and Reproducible Method to Affect Muscle Development and Growth
06:38

In Ovo Feeding of Commercial Broiler Eggs: An Accurate and Reproducible Method to Affect Muscle Development and Growth

Published on: September 20, 2021

2.5K

Ring replacement recommender: Ring modifications for improving biological activity.

Peter Ertl1, Eva Altmann1, Sophie Racine1

  • 1Global Discovery Chemistry, Novartis Institutes for BioMedical Research, CH-4056, Basel, Switzerland.

European Journal of Medicinal Chemistry
|May 31, 2022
PubMed
Summary
This summary is machine-generated.

Medicinal chemists can improve drug discovery by using novel heterocyclic ring replacements. A database and web tool suggest 80 diverse substitutions for optimizing biological activity and exploring structure-activity relationships.

Keywords:
Bioisosteric replacementBuilding blocksCheminformaticsHeterocyclic ringsHit to lead optimizationLibrary designSubstituents

More Related Videos

Author Spotlight: In Silico Creation and Impact of Carbonylated Amino Acids on Protein Structure and Function
05:57

Author Spotlight: In Silico Creation and Impact of Carbonylated Amino Acids on Protein Structure and Function

Published on: April 26, 2024

508
Rapid Synthesis and Screening of Chemically Activated Transcription Factors with GFP-based Reporters
09:22

Rapid Synthesis and Screening of Chemically Activated Transcription Factors with GFP-based Reporters

Published on: November 26, 2013

14.7K

Related Experiment Videos

Last Updated: Sep 21, 2025

In Ovo Feeding of Commercial Broiler Eggs: An Accurate and Reproducible Method to Affect Muscle Development and Growth
06:38

In Ovo Feeding of Commercial Broiler Eggs: An Accurate and Reproducible Method to Affect Muscle Development and Growth

Published on: September 20, 2021

2.5K
Author Spotlight: In Silico Creation and Impact of Carbonylated Amino Acids on Protein Structure and Function
05:57

Author Spotlight: In Silico Creation and Impact of Carbonylated Amino Acids on Protein Structure and Function

Published on: April 26, 2024

508
Rapid Synthesis and Screening of Chemically Activated Transcription Factors with GFP-based Reporters
09:22

Rapid Synthesis and Screening of Chemically Activated Transcription Factors with GFP-based Reporters

Published on: November 26, 2013

14.7K

Area of Science:

  • Medicinal Chemistry
  • Drug Discovery
  • Computational Chemistry

Background:

  • Structure-activity relationships (SAR) are crucial for drug development.
  • Identifying novel heterocyclic scaffolds can enhance biological activity.
  • Large-scale literature analysis is a powerful tool for SAR insights.

Purpose of the Study:

  • To identify and database heterocyclic ring replacements that improve biological activity.
  • To provide medicinal chemists with data-driven suggestions for hit optimization.
  • To facilitate the design of focused libraries for efficient SAR exploration.

Main Methods:

  • Analysis of structure-activity data from extensive medicinal chemistry literature.
  • Development of a database cataloging replacements for 245 common heterocyclic rings.
  • Creation of a web-based tool for interactive exploration of ring substitutions.

Main Results:

  • A curated set of heterocyclic ring replacements with high potential for improved biological activity was identified.
  • A database containing these replacements for 245 common heterocyclic rings is now available.
  • 80 diverse substituted rings are recommended for early-stage hit optimization and focused library design.

Conclusions:

  • The identified ring replacements offer a strategic approach to enhance biological activity in drug discovery programs.
  • The provided database and recommender tool streamline the process of SAR exploration and lead optimization.
  • This resource empowers medicinal chemists to accelerate the discovery of novel therapeutics.