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

Ligand Binding and Linkage00:49

Ligand Binding and Linkage

3.9K
3.9K
Ligand Binding and Linkage00:49

Ligand Binding and Linkage

5.4K
Allosteric proteins have more than one ligand binding site; the binding of a ligand to any of these sites influences the binding of ligands to the other sites. When a protein is allosteric, its binding sites are called coupled or linked.  In the case of enzymes, the site that binds to the substrate is known as the active site and the other site is known as the regulatory site. When a ligand binds to the regulatory site, this leads to conformational changes in the protein that can influence...
5.4K
Phase II Conjugation Reactions: Overview01:14

Phase II Conjugation Reactions: Overview

728
Conjugation, a key component of phase II biotransformation reactions, is a vital process in drug detoxification. It involves transferring endogenous substances like glucuronic acid, sulfate, and glycine to drugs or their metabolites formed in phase I reactions. These conjugation reactions, often catalyzed by specific enzymes, transform potentially harmful metabolites into inactive, water-soluble forms easily excreted in urine or bile. By enhancing polarity and eliminating pharmacological...
728
Clinical Trials: Overview01:11

Clinical Trials: Overview

4.5K
Clinical development focuses on how the drug will interact with the human body and encompasses four key phases of clinical trials, each serving a specific purpose in assessing the safety and effectiveness of new drugs. These phases overlap and build upon one another. Phase I involves a small group of healthy volunteers (typically 20-80 individuals) or, in cases where significant toxicity is expected, patients with the targeted disease, such as cancer or AIDS. The volunteers are tested for...
4.5K
Preclinical Development: Overview01:28

Preclinical Development: Overview

5.7K
Preclinical development consists of a series of tests that ensure the safety and efficacy of a new therapeutic compound before it is tested in humans. There are four main phases to this process. First, safety pharmacology tests are conducted to ensure the drug does not produce any acutely harmful effects. These tests examine parameters such as bronchoconstriction, cardiac dysrhythmias, blood pressure changes, and ataxia. Next, preliminary toxicological testing is performed to determine the...
5.7K
Clinical Trials01:16

Clinical Trials

10.1K
Clinical trials are prospective experimental studies conducted on humans to determine the safety and efficacy of treatments, drugs, diet methods, and medical devices. Using statistics in clinical trials enables researchers to derive reasonable and accurate conclusions from the collected data, allowing them to make wise decisions in uncertain situations. In medical research, statistical methods are crucial for preventing errors and bias.
There are four phases in a clinical trial. A phase one...
10.1K

You might also read

Related Articles

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

Sort by
Same author

Multifunctional Peroxidase-Mimicking Ag<sub>2</sub>S/NiS/Reduced Graphene Oxide Nanozyme for Hydrogen Peroxide Determination and Dye Degradation.

ChemPlusChem·2026
Same author

Comparative Study of Hyperbaric Bupivacaine Versus Levobupivacaine for Rapid Sequence Spinal Anesthesia in Category 1 and 2 Cesarean Sections.

Cureus·2026
Same author

Discovery of CNS Penetrant SOS1 Inhibitors for the Treatment of KRAS-Dependent Cancers.

Journal of medicinal chemistry·2026
Same author

International Delphi consensus on single-port robotic radical prostatectomy: patient selection, surgical technique, and training.

BJU international·2026
Same author

Hierarchically Nanoporous Carbon Engineered from Wood for Concurrent Dye Remediation and Electrochemical Charge Storage.

ChemPlusChem·2026
Same author

Upper extremity lacrosse injuries presenting to United States emergency departments - 10 year review.

JSES reviews, reports, and techniques·2026

Related Experiment Video

Updated: Jan 8, 2026

Improving Student Outcomes with an Adaptable Molecular Cloning Course-Based Undergraduate Research Experience
10:17

Improving Student Outcomes with an Adaptable Molecular Cloning Course-Based Undergraduate Research Experience

Published on: November 15, 2024

1.6K

Lessons learned in linking PROTACs from discovery to the clinic.

Andy Pike1, Esther C Y Lee2, Iacovos N Michaelides3

  • 1DMPK, Oncology R&D, AstraZeneca, Cambridge, UK. andrew.pike@astrazeneca.com.

Nature Reviews. Chemistry
|December 13, 2025
PubMed
Summary
This summary is machine-generated.

Targeted protein degradation, using proteolysis targeting chimeras (PROTACs), offers new therapeutic potential. Linker optimization is crucial for PROTAC efficacy, oral bioavailability, and clinical success.

More Related Videos

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
08:47

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates

Published on: March 6, 2019

9.9K
Author Spotlight: Evaluating Biophysical Assays for Characterizing PROTACS Ternary Complexes
07:22

Author Spotlight: Evaluating Biophysical Assays for Characterizing PROTACS Ternary Complexes

Published on: January 12, 2024

4.4K

Related Experiment Videos

Last Updated: Jan 8, 2026

Improving Student Outcomes with an Adaptable Molecular Cloning Course-Based Undergraduate Research Experience
10:17

Improving Student Outcomes with an Adaptable Molecular Cloning Course-Based Undergraduate Research Experience

Published on: November 15, 2024

1.6K
Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
08:47

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates

Published on: March 6, 2019

9.9K
Author Spotlight: Evaluating Biophysical Assays for Characterizing PROTACS Ternary Complexes
07:22

Author Spotlight: Evaluating Biophysical Assays for Characterizing PROTACS Ternary Complexes

Published on: January 12, 2024

4.4K

Area of Science:

  • Biochemistry
  • Pharmacology
  • Drug Discovery

Background:

  • Targeted protein degradation offers superior efficacy over conventional inhibitors.
  • It addresses previously undruggable targets, driving interest in novel modalities.
  • Proteolysis targeting chimeras (PROTACs) are a key protein degradation modality.

Purpose of the Study:

  • To review lessons learned in PROTAC optimization.
  • To emphasize the linker region's role in PROTAC development.
  • To discuss PROTACs' evolution into a clinical modality.

Main Methods:

  • Review of preclinical data and clinical trial information.
  • Analysis of PROTAC structure-activity relationships.
  • Focus on linker properties and their impact.

Main Results:

  • Linker optimization significantly impacts PROTAC pharmacology and metabolic fate.
  • Physicochemical challenges, particularly oral bioavailability, are being addressed.
  • PROTACs are transitioning from research tools to clinical therapeutics.

Conclusions:

  • PROTAC technology is advancing rapidly, offering significant therapeutic promise.
  • Understanding linker contributions is vital for successful PROTAC design.
  • Clinical data provides valuable insights for future PROTAC development.