Related Experiment Video
Updated: Jul 11, 2025
05:33
High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
Published on: November 9, 2020
9.7K
Targeted Protein Degraders- The Druggability Perspective
Satinder Singh1, Pratima Srivastava1
1Aragen Life Sciences Private Limited, Hyderabad, India.
Journal of Pharmaceutical Sciences
|November 5, 2023
Summary
Targeted protein degraders (TPDs) offer a new way to eliminate disease proteins. Overcoming challenges like solubility is key to developing effective TPD therapeutics.
Area of Science:
- Biochemistry
- Pharmacology
- Drug Discovery
Background:
- Targeted Protein Degraders (TPDs) leverage cellular machinery for protein elimination.
- TPDs offer lasting therapeutic effects, especially for proteins with low turnover.
- Clinical TPD candidates demonstrate promising safety and efficacy profiles.
Purpose of the Study:
- To highlight the therapeutic potential of TPDs.
- To address challenges in TPD development, including physicochemical properties.
- To emphasize the role of in-vitro assays in TPD optimization.
Main Methods:
- Review of existing TPD research and clinical data.
- Analysis of TPD properties concerning drug-likeness (e.g., Lipinski's Rule of Five).
- Discussion of in-vitro assay development for TPD profiling.
Main Results:
- TPDs can target previously undruggable proteins.
- Low protein turnover enhances the lasting therapeutic effect of TPDs.
- Overcoming solubility, permeability, and bioavailability issues is crucial for TPD development.
Conclusions:
- TPDs represent a significant advancement in therapeutic strategies.
- Tailored in-vitro assays are essential for precise TPD profiling and optimization.
- Continued development of TPDs holds promise for diverse therapeutic areas.
Keywords:
Cellular permeabilityIn-vitro assaysPermeabilityScreeningSolubilityTargeted protein degradersMore Related Videos
08:31Biosensor-based High Throughput Biopanning and Bioinformatics Analysis Strategy for the Global Validation of Drug-protein Interactions
Published on: December 1, 2020
5.0K
00:05A Semi-Quantitative Drug Affinity Responsive Target Stability DARTS assay for studying Rapamycin/mTOR interaction
Published on: August 27, 2019
16.4K
Related Concept Videos
01:26Targets for Drug Action: Overview
6.3K
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...
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...
6.3K
01:30Prodrugs
2.6K
Prodrugs are a class of pharmaceutical compounds that undergo a biotransformation process within the body to be converted into a pharmacologically active drug. Prodrugs are designed to improve the therapeutic properties of the parent drug, such as enhancing bioavailability, increasing stability, or reducing toxicity. The concept of prodrugs revolves around modifying the chemical structure of the original drug to make it more effective or convenient for administration.
Prodrugs help overcome...
Prodrugs help overcome...
2.6K
01:24Principles of Drug Action
6.1K
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...
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...
6.1K
01:16Protein-Drug Binding: Mechanism and Kinetics
534
Protein-drug binding refers to the interaction between drugs and proteins within the body. This binding process can occur intracellularly, involving drug interactions with enzymes or receptors within cells, or extracellularly, involving plasma proteins in the blood.
Various forces drive these interactions, including hydrogen bonds, hydrophobic interactions, ionic bonds, electrostatic interactions, and van der Waals forces. These bonds enable drugs to bind to specific sites on proteins,...
Various forces drive these interactions, including hydrogen bonds, hydrophobic interactions, ionic bonds, electrostatic interactions, and van der Waals forces. These bonds enable drugs to bind to specific sites on proteins,...
534
02:58Regulated Protein Degradation
2.5K
2.5K
01:26Drug Discovery: Overview
8.0K
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...
8.0K