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

Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

9.9K
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...
9.9K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

8.6K
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...
8.6K
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

3.7K
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:
3.7K
Protein Kinases and Phosphatases02:54

Protein Kinases and Phosphatases

14.7K
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...
14.7K
Amplifying Signals via Enzymatic Cascade01:22

Amplifying Signals via Enzymatic Cascade

16.8K
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...
16.8K
Principles of Drug Action01:24

Principles of Drug Action

7.8K
Drugs are chemical substances that modify biological responses by interacting with macromolecular targets such as receptors, ion channels, transporters, and enzymes. Pharmacodynamics describes the course of action of drugs leading to the physiological effect at a specific site in the body.
Drugs can be agonists or antagonists. Like the endogenous ligands, agonists always bind and activate the target to produce a cellular response. Agonist binding induces a conformational change which in turn...
7.8K

You might also read

Related Articles

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

Sort by
Same author

MCAK/Kif2C centromeric activity level tunes K-fiber turnover through distinct pathways.

iScience·2026
Same author

MEK interactions tune RAF kinase sensitivity to conformation-selective inhibition.

Nature chemical biology·2026
Same author

Linda Wordeman.

Current biology : CB·2026
Same author

Mitotically Driven Cytoskeletal Reorganization Governs Zebrafish Left-Right Organizer Detachment from EVL and Lumen Morphogenesis.

bioRxiv : the preprint server for biology·2026
Same author

Dominant α-tubulin mutations rescue tauopathy neurodegenerative phenotypes in <i>C. elegans</i>.

bioRxiv : the preprint server for biology·2026
Same author

The β<sub>2</sub>-adrenoceptor agonist formoterol attenuates hallmarks of adrenal Cushing's syndrome.

British journal of pharmacology·2026

Related Experiment Video

Updated: Jan 1, 2026

Subcellular Fractionation for ERK Activation Upon Mitochondrial-derived Peptide Treatment
07:55

Subcellular Fractionation for ERK Activation Upon Mitochondrial-derived Peptide Treatment

Published on: September 25, 2017

8.2K

Subcellular drug targeting illuminates local kinase action.

Paula J Bucko1, Chloe K Lombard2, Lindsay Rathbun3

  • 1Department of Pharmacology, University of Washington, Seattle, United States.

Elife
|December 25, 2019
PubMed
Summary

Researchers developed a new tool, Localized Kinase Inhibition (LoKI), to precisely target kinase inhibitors to specific cell parts. This method reveals organelle-specific kinase functions, impacting cell division and development.

Keywords:
biochemistrycell biologychemical biologykinaseslocal signalingmitosiszebrafish

More Related Videos

Characterization at the Molecular Level using Robust Biochemical Approaches of a New Kinase Protein
11:23

Characterization at the Molecular Level using Robust Biochemical Approaches of a New Kinase Protein

Published on: June 30, 2019

6.6K
An Integrated System to Remotely Trigger Intracellular Signal Transduction by Upconversion Nanoparticle-mediated Kinase Photoactivation
11:20

An Integrated System to Remotely Trigger Intracellular Signal Transduction by Upconversion Nanoparticle-mediated Kinase Photoactivation

Published on: August 30, 2017

7.8K

Related Experiment Videos

Last Updated: Jan 1, 2026

Subcellular Fractionation for ERK Activation Upon Mitochondrial-derived Peptide Treatment
07:55

Subcellular Fractionation for ERK Activation Upon Mitochondrial-derived Peptide Treatment

Published on: September 25, 2017

8.2K
Characterization at the Molecular Level using Robust Biochemical Approaches of a New Kinase Protein
11:23

Characterization at the Molecular Level using Robust Biochemical Approaches of a New Kinase Protein

Published on: June 30, 2019

6.6K
An Integrated System to Remotely Trigger Intracellular Signal Transduction by Upconversion Nanoparticle-mediated Kinase Photoactivation
11:20

An Integrated System to Remotely Trigger Intracellular Signal Transduction by Upconversion Nanoparticle-mediated Kinase Photoactivation

Published on: August 30, 2017

7.8K

Area of Science:

  • Cell Biology
  • Molecular Pharmacology
  • Biochemistry

Background:

  • Understanding enzyme function within specific cellular microenvironments is crucial for biological processes.
  • A-kinase anchoring proteins (AKAPs) regulate protein kinase activity by localizing them to intracellular compartments.
  • Existing kinase inhibitors often lack specificity, affecting multiple cellular locations and functions.

Purpose of the Study:

  • To develop a genetically encoded platform for targeted delivery of kinase inhibitors to specific subcellular locations.
  • To investigate organelle-specific functions of broad-specificity kinases using localized inhibition.
  • To explore the role of localized kinase activity in mitotic processes and embryonic development.

Main Methods:

  • Exploited the AKAP targeting concept to create genetically encoded platforms for kinase inhibitor localization.
  • Utilized chemical genetics, super-resolution microscopy, and live-cell imaging to observe the effects of localized inhibition.
  • Applied the Localized Kinase Inhibition (LoKI) system to study Polo-like kinase 1 (Plk1) and Aurora A (AurA) in cellular and embryonic models.

Main Results:

  • Localized inhibition of Plk1 and AurA at the centrosome attenuated kinase activity, caused spindle defects, and prolonged mitosis.
  • Targeted inhibition of centrosomal Plk1 in zebrafish embryos demonstrated its essential role in mitotic spindle assembly.
  • Inhibition of kinetochore-associated Aurora A blocked phosphorylation of key microtubule-kinetochore components.

Conclusions:

  • The LoKI system provides a versatile tool for precision pharmacology, enabling the investigation of local kinase biology.
  • Localized kinase inhibition can dissect organelle-specific functions of kinases, offering new insights into cell regulation.
  • This approach enhances the study of fundamental biological processes like cell division and development by controlling enzyme activity in specific cellular compartments.