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

Protein Kinases and Phosphatases02:54

Protein Kinases and Phosphatases

Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
Protein Kinases and Phosphatases02:54

Protein Kinases and Phosphatases

Proteins undergo chemical modifications that trigger changes in the charge, structure, and conformation of the proteins. Phosphorylation, acetylation, glycosylation, nitrosylation, ubiquitination, lipidation, methylation, and proteolysis are various protein modifications that regulate protein activity. Such modifications are usually enzyme-driven.
Protein kinases
Many proteins in the cell are regulated by phosphorylation, the addition of a phosphate group. A family of enzymes called kinases...
Drug Discovery: Overview01:26

Drug Discovery: Overview

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...
PI3K/mTOR/AKT Signaling Pathway01:22

PI3K/mTOR/AKT Signaling Pathway

The mammalian target of rapamycin  (mTOR) is a serine/threonine kinase that regulates growth, proliferation, and cell survival in response to hormones, growth factors, or nutrient availability. This kinase exists in two structurally and functionally distinct forms: mTOR complex 1  (mTORC1) and mTOR complex 2  (mTORC2). The first form (mTORC1) is composed of a rapamycin-sensitive Raptor and proline-rich Akt substrate, PRAS40. In contrast,  mTORC2 consists of a rapamycin-insensitive companion...
Amplifying Signals via Enzymatic Cascade01:22

Amplifying Signals via Enzymatic Cascade

When a ligand binds to a cell-surface receptor, the receptor's intracellular domain changes shape, which may either activate its enzyme function or allow its binding to other molecules. The initial signal is amplified by most signal transduction pathways. This means that a single ligand molecule can activate multiple molecules of a downstream target. Proteins that relay a signal are most commonly phosphorylated at one or more sites, activating or inactivating the protein. Kinases catalyze the...

You might also read

Related Articles

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

Sort by
Same author

BET inhibitor OPN-2853 in advanced solid tumors and lymphoma: results from the phase 1b PLX124-01 trial.

Cancer chemotherapy and pharmacology·2026
Same author

Overcoming the Limits of Inhibition: Mutant-Selective BRAF Degraders.

Cancer research·2026
Same author

Acute Myeloid Leukemia Relapse after Bromodomain Inhibitor Treatment or Chemotherapy is Characterized by Myc-Ras Transcriptional Remodeling.

bioRxiv : the preprint server for biology·2025
Same author

RAF inhibitors activate the integrated stress response by direct activation of GCN2.

Nature communications·2025
Same author

Targeting TAZ-TEAD in minimal residual disease enhances the duration of targeted therapy in melanoma models.

Nature communications·2025
Same author

BET inhibition reforms the immune microenvironment and alleviates T cell dysfunction in chronic lymphocytic leukemia.

JCI insight·2024
Same journal

Resolution Biology in Soft Tissue Joint Disease.

Current topics in microbiology and immunology·2026
Same journal

A 25+ Year Journey on Yeast-Regulated Cell Death Research.

Current topics in microbiology and immunology·2026
Same journal

Adoptive T-Cell Immunotherapy.

Current topics in microbiology and immunology·2026
Same journal

Resolution Pharmacology Targeting the Melanocortin System.

Current topics in microbiology and immunology·2026
Same journal

Resolution of Skeletal Muscle Inflammation: Role of Specialized Pro-resolving Lipid Mediators in the Recovery from Exercise, Injury, and Disease.

Current topics in microbiology and immunology·2026
Same journal

Epstein-Barr Virus: From the Detection of Sequence Polymorphisms to the Recognition of Viral Strains.

Current topics in microbiology and immunology·2026
See all related articles

Related Experiment Video

Updated: May 30, 2026

Identification of Kinase-substrate Pairs Using High Throughput Screening
11:13

Identification of Kinase-substrate Pairs Using High Throughput Screening

Published on: August 29, 2015

Setting up a kinase discovery and development project.

Gideon Bollag1

  • 1Plexxikon Inc, Berkeley, CA 94710, USA. gbollag@plexxikon.com

Current Topics in Microbiology and Immunology
|August 3, 2011
PubMed
Summary
This summary is machine-generated.

Developing selective kinase inhibitors is crucial for drug development. While many current drugs lack target specificity, new technologies promise improved precision, especially for Raf kinases.

More Related Videos

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

Assaying Protein Kinase Activity with Radiolabeled ATP
08:05

Assaying Protein Kinase Activity with Radiolabeled ATP

Published on: May 26, 2017

Related Experiment Videos

Last Updated: May 30, 2026

Identification of Kinase-substrate Pairs Using High Throughput Screening
11:13

Identification of Kinase-substrate Pairs Using High Throughput Screening

Published on: August 29, 2015

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays
13:22

Kinase Inhibitor Screening In Self-assembled Human Protein Microarrays

Published on: October 23, 2019

Assaying Protein Kinase Activity with Radiolabeled ATP
08:05

Assaying Protein Kinase Activity with Radiolabeled ATP

Published on: May 26, 2017

Area of Science:

  • Biochemistry
  • Pharmacology
  • Drug Discovery

Background:

  • Kinase inhibitor development has advanced significantly.
  • Marketed kinase inhibitors often lack target selectivity.
  • Target selectivity is critical for successful kinase inhibitor development.

Purpose of the Study:

  • To discuss key considerations in kinase discovery and development projects.
  • To highlight the importance of target selectivity in kinase inhibitor design.
  • To provide examples focusing on Raf kinase inhibitors.

Main Methods:

  • Review of existing kinase inhibitor development approaches.
  • Analysis of marketed small molecule protein kinase inhibitors.
  • Discussion of emerging technologies for enhancing selectivity.

Main Results:

  • Thirteen small molecule protein kinase inhibitors are currently available.
  • Many existing inhibitors exhibit limited target selectivity.
  • Technological advancements are expected to improve inhibitor selectivity.

Conclusions:

  • Improved kinase inhibitor selectivity is an evolving area.
  • Future kinase inhibitor projects must prioritize target specificity.
  • Raf kinases serve as a relevant case study for selectivity challenges.