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

Noncompartmental Analysis: Mean Residence Time01:05

Noncompartmental Analysis: Mean Residence Time

619
According to statistical moment theory, mean residence time (MRT) is an important measure in pharmacokinetics. MRT can be defined as the expected mean of a probability density function distribution. It provides valuable insights into drug disposition in the body.
After the administration of a drug through intravenous bolus injection, the drug molecules are distributed throughout the body and remain there for varying periods. The MRT represents the average time these drug molecules stay in the...
619
Halogens03:01

Halogens

23.6K
Group 17 elements, known as halogens, are nonmetals. At room temperature, fluorine and chlorine are gases, bromine is a liquid, and iodine a solid. Astatine is a highly unstable radioactive element, so currently, most of its properties are unknown due to its short half-life. Tennessine is a synthetic element also predicted to be in this group. 
23.6K
π Electron Effects on Chemical Shift: Aromatic and Antiaromatic Compounds01:14

π Electron Effects on Chemical Shift: Aromatic and Antiaromatic Compounds

1.9K
In aromatic compounds, such as benzene, the circulation of (4n + 2) π-electrons sets up a diamagnetic or diatropic ring current around the perimeter of the molecule. This current induces a magnetic field that opposes the external field inside the ring and reinforces it on the outside. The protons in benzene are deshielded and exhibit high chemical shifts in the range 6.5–8.5 ppm. The shielding effect at the center of the ring is evident in complex aromatic molecules, such as...
1.9K
Eukaryotic Transcription Inhibitors01:52

Eukaryotic Transcription Inhibitors

11.1K
Certain biochemical processes, such as embryonic development and cell growth regulation, depend on the repression of specific genes. DNA binding proteins known as eukaryotic transcription inhibitors regulate the repression of gene expression in eukaryotes. The presence of these inhibitors at the required location and time in the cell is triggered by the presence of hormones and additional signals from other cells.
Eukaryotic transcription inhibitors usually contain two distinct domains, a...
11.1K
Nucleophilic Aromatic Substitution of Aryldiazonium Salts: Aromatic SN101:14

Nucleophilic Aromatic Substitution of Aryldiazonium Salts: Aromatic SN1

2.8K
Treating arylamines with nitrous acid gives aryldiazonium salts that are effective substrates in nucleophilic aromatic substitution reactions. The diazonio group in these salts can be easily displaced by different nucleophiles, yielding a wide variety of substituted benzenes. The leaving group departs as nitrogen gas, and this easy elimination is the driving force for the substitution reaction.
In the Sandmeyer reaction, for example, the diazonio group is replaced by a chloro, bromo,...
2.8K
π Molecular Orbitals of 1,3-Butadiene01:24

π Molecular Orbitals of 1,3-Butadiene

12.0K
Conjugated dienes have lower heats of hydrogenation than cumulated and isolated dienes, making them more stable. The enhanced stabilization of conjugated systems can be understood from their π molecular orbitals.
The simplest conjugated diene is 1,3-butadiene: a four-carbon system where each carbon is sp2-hybridized and has an unhybridized p orbital that contains an unpaired electron. According to molecular orbital theory, atomic orbitals combine to form molecular orbitals such that the number...
12.0K

You might also read

Related Articles

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

Sort by
Same author

Riding toward Selectivity: Optimization of Covalent 7-Azaindole-Based BMX Kinase Inhibitors.

Journal of medicinal chemistry·2026
Same author

USP22 is a novel vulnerability regulating MEIS1 protein abundance and gene transcription in KMT2Ar acute leukemia.

Blood·2026
Same author

AURORA A interacts with DICER and SETD2 to promote S-phase progression.

EMBO reports·2026
Same author

Mapping the Molecular Universe: Exploring Chemical Compound Space by Multiscale High-Throughput Screening and Machine Learning.

Journal of chemical information and modeling·2026
Same author

On the Scope of DCAF1-Recruiting PROTACs Degrading Protein Kinases.

Journal of medicinal chemistry·2026
Same author

The structural basis for LRRK2's activation and autoinhibition.

bioRxiv : the preprint server for biology·2026

Related Experiment Video

Updated: Feb 12, 2026

From Molecules to Materials: Engineering New Ionic Liquid Crystals Through Halogen Bonding
06:44

From Molecules to Materials: Engineering New Ionic Liquid Crystals Through Halogen Bonding

Published on: March 24, 2018

69.7K

Halogen-Aromatic π Interactions Modulate Inhibitor Residence Times.

Christina Heroven1, Victoria Georgi2, Gaurav K Ganotra3,4

  • 1Nuffield Department of Clinical Medicine, Structural Genomics Consortium, University of Oxford, Oxford, OX3 7DQ, UK.

Angewandte Chemie (International Ed. in English)
|March 31, 2018
PubMed
Summary

Increasing halogen size on drug inhibitors enhances their residence time with target proteins. This strategy can improve drug efficacy and selectivity, aiding drug development.

Keywords:
drug residence timeshalogen-π interactionsiodinekinasesproteins

More Related Videos

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

11.9K
Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions
10:53

Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions

Published on: October 10, 2016

14.6K

Related Experiment Videos

Last Updated: Feb 12, 2026

From Molecules to Materials: Engineering New Ionic Liquid Crystals Through Halogen Bonding
06:44

From Molecules to Materials: Engineering New Ionic Liquid Crystals Through Halogen Bonding

Published on: March 24, 2018

69.7K
Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
10:33

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors

Published on: October 26, 2015

11.9K
Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions
10:53

Anionic Polymerization of an Amphiphilic Copolymer for Preparation of Block Copolymer Micelles Stabilized by π-π Stacking Interactions

Published on: October 10, 2016

14.6K

Area of Science:

  • Medicinal Chemistry
  • Biochemistry
  • Pharmacology

Background:

  • Prolonged drug residence time can enhance drug efficacy and selectivity.
  • Few strategies exist to rationally control drug residence time during development.

Purpose of the Study:

  • To investigate if halogen-protein interactions can modulate inhibitor residence time.
  • To explore the role of halogen size and polarizability in enhancing inhibitor binding.

Main Methods:

  • Utilized serine/threonine kinase haspin and 5-iodotubercidin (5-iTU) derivatives as a model system.
  • Employed kinetic, thermodynamic, and structural analyses.
  • Performed binding-energy calculations.

Main Results:

  • Inhibitor residence times significantly increased with larger, more polarizable halogen atoms.
  • Demonstrated a correlation between halogen size/polarizability and extended residence time.
  • Characterized halogen-aromatic π interactions in haspin-inhibitor complexes.

Conclusions:

  • Halogen-aromatic interactions are a viable strategy to increase inhibitor residence time.
  • Modulating halogen properties offers a rational approach to drug development.
  • This method enhances kinetic selectivity and prolongs drug action.