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

Pharmacogenomics: Identification of New Drug Targets01:29

Pharmacogenomics: Identification of New Drug Targets

25
Advances in genomics have profoundly influenced drug discovery by increasing both the speed and accuracy of pharmaceutical development. Pharmacogenomics, which examines how genetic variation influences drug response, facilitates the identification of novel therapeutic targets and enables patient stratification for personalized treatment. These strategies contribute to improved drug efficacy, minimized adverse effects, and more efficient clinical trial design.Mapping genetic differences...
25
Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase01:11

Pharmacogenetics of Drug Targets: β₂-Adrenergic Receptors, Apo E, Thymidylate Synthase

24
Genetic polymorphisms in drug targets have emerged as critical determinants of interindividual variability in drug response and toxicity. Pharmacogenomic investigations increasingly focus on identifying these variations to personalize and optimize therapeutic interventions. A drug target may be a receptor, enzyme, or signaling protein involved in pharmacologic responses or disease-related pathways. While early pharmacogenetic studies focused primarily on drug metabolism, current research...
24
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

9.0K
The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
9.0K
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

10.7K
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...
10.7K
Treatment Resistant Cancers02:56

Treatment Resistant Cancers

3.8K
Cancer is the second leading cause of death in the United States. A cancer cell is genetically unstable and hence can mutate faster. They can also modify their microenvironment and escape immune surveillance. The difficulties in treating cancer are further compounded by the emergence of rapid resistance to anticancer drugs. The most common ways to attain resistance in cancer cells include alteration in drug transport and metabolism, modification of drug target, elevated DNA damage response, or...
3.8K
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

4.3K
Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
Major types that are helpful drug targets include:
4.3K

You might also read

Related Articles

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

Sort by
Same author

A twist in the tale: shifting from covalent targeting of a tyrosine in JAK3 to a lysine in MK2.

RSC medicinal chemistry·2025
Same author

Covalent Targeting Leads to the Development of a LIMK1 Isoform-Selective Inhibitor.

Journal of medicinal chemistry·2025
Same author

Structure-Based Design of PROTACS for the Degradation of Soluble Epoxide Hydrolase.

Journal of medicinal chemistry·2025
Same author

Crystallographic fragment screening reveals ligand hotspots in TRIM21 PRY-SPRY domain.

Communications chemistry·2025
Same author

Type II kinase inhibitors that target Parkinson's disease-associated LRRK2.

Science advances·2025
Same author

Biochemical investigation of LC3/GABARAP-ligand interaction as an important quality measure for LC3/GABARAP-targeting small molecules: addendum to the guidelines (4th edition).

Autophagy·2025

Related Experiment Video

Updated: Feb 19, 2026

Using Human Differentially Expressed Gene Lists to Perform Downstream Pathway Enrichment Analysis and Target Prioritization
03:08

Using Human Differentially Expressed Gene Lists to Perform Downstream Pathway Enrichment Analysis and Target Prioritization

Published on: October 3, 2025

1.0K

Emerging Target Families: Intractable Targets.

Stefan Knapp1,2

  • 1Nuffield Department of Clinical Medicine, Target Discovery Institute, University of Oxford, Oxford, 3 7FZ, UK. knapp@pharmchem.uni-frankfurt.de.

Handbook of Experimental Pharmacology
|November 11, 2015
PubMed
Summary

Druggability assesses if small molecules can modulate targets. This review covers progress in developing inhibitors for challenging drug targets and new protein families.

Keywords:
DruggabilityEpigenetic reader domainsPhosphatasesProtein interaction inhibitorsRASStructure based design

More Related Videos

Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down
08:59

Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down

Published on: December 11, 2017

7.6K
Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
08:46

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms

Published on: December 9, 2015

11.2K

Related Experiment Videos

Last Updated: Feb 19, 2026

Using Human Differentially Expressed Gene Lists to Perform Downstream Pathway Enrichment Analysis and Target Prioritization
03:08

Using Human Differentially Expressed Gene Lists to Perform Downstream Pathway Enrichment Analysis and Target Prioritization

Published on: October 3, 2025

1.0K
Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down
08:59

Looking for Driver Pathways of Acquired Resistance to Targeted Therapy: Drug Resistant Subclone Generation and Sensitivity Restoring by Gene Knock-down

Published on: December 11, 2017

7.6K
Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
08:46

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms

Published on: December 9, 2015

11.2K

Area of Science:

  • Pharmacology and medicinal chemistry
  • Drug discovery and development

Background:

  • Druggability defines a target's amenability to modulation by small molecules.
  • Enzymes have historically been primary drug targets, but some remain intractable.
  • Protein-protein interactions are a growing area for drug development.

Purpose of the Study:

  • To summarize progress in developing inhibitors for challenging drug binding sites.
  • To highlight emerging target families in drug discovery.

Main Methods:

  • Review of literature on small molecule inhibitors.
  • Analysis of historical and recent drug target classes.
  • Discussion of challenges in targeting specific protein families.

Main Results:

  • Enzymes, while historically targeted, present ongoing challenges.
  • Significant advancements have been made in targeting protein-protein interactions.
  • Many high-rationale targets remain difficult to modulate with small molecules.

Conclusions:

  • Despite progress, intractable targets persist in drug discovery.
  • Expanding target space requires innovative approaches for challenging binding sites.
  • Emerging target families offer new opportunities for therapeutic intervention.