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Related Concept Videos

Drug Metabolism: Phase II Reactions01:14

Drug Metabolism: Phase II Reactions

Phase II reactions are essential for the detoxification and elimination of drugs from the body. These reactions involve the conjugation of parent drugs or their phase I metabolites with endogenous molecules, resulting in more hydrophilic drug conjugates. The primary conjugation reactions in this phase are sulfation and glucuronidation. Both sulfation and glucuronidation typically produce biologically inactive metabolites. However, in some cases involving prodrugs, active metabolites may be...
Phase II Conjugation Reactions: Overview01:14

Phase II Conjugation Reactions: Overview

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...
Modified-Release Drug Delivery Systems: Classification01:23

Modified-Release Drug Delivery Systems: Classification

Modified-release drug delivery systems improve drug efficacy and minimize side effects by controlling the rate and location of drug release. These systems fall into three categories: rate-programmed, stimuli-activated, and site-targeted.Rate-programmed systems release drugs at a predetermined rate, maintaining consistent therapeutic levels and reducing fluctuations that could lead to toxicity or subtherapeutic effects. These systems use polymeric matrices, reservoir-based designs, or osmotic...
Drug Biotransformation: Overview01:16

Drug Biotransformation: Overview

Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
Drug Biotransformation: Overview01:28

Drug Biotransformation: Overview

Biotransformation, also known as drug metabolism, is a vital physiological process that chemically alters drugs, facilitating their elimination from the body and terminating their action. This process involves two main phases: phase I and phase II reactions. Phase I reactions, including oxidation, reduction, and hydrolysis, introduce or unmask polar functional groups on the drug molecule, thereby increasing its water solubility. By enhancing water solubility, the drug becomes more hydrophilic...
Modified-Release Drug Delivery Systems: Overview01:19

Modified-Release Drug Delivery Systems: Overview

Modified-release dosage forms are designed to address the limitations of drugs with short biological half-lives. These forms maintain stable therapeutic drug concentrations over extended periods, reducing the need for frequent dosing. A consistent drug level helps minimize peak-trough fluctuations, which can reduce adverse effects, lower the risk of drug resistance, and improve overall treatment effectiveness.One common type of modified-release form is the extended-release (ER) formulation. ER...

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Updated: May 17, 2026

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English
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A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English

Published on: April 3, 2026

A Plug-and-Play Platform for Customizing Multivalent Degraders and Degrader-Drug Conjugates.

Mengqing Zhao1, Yan Deng2, Jianjian Han1

  • 1State Key Laboratory of Biocatalysis and Enzyme Engineering, Hubei Province Key Laboratory of Industrial Biotechnology, School of Life Sciences, Hubei University, Wuhan, China.

Advanced Science (Weinheim, Baden-Wurttemberg, Germany)
|May 15, 2026
PubMed
Summary

We developed a novel UPTAB platform for targeted protein degradation of membrane proteins, achieving high degradation efficiency and significant tumor growth inhibition. This platform also enables potent degrader-drug conjugates for enhanced cancer therapy.

Keywords:
LYTACdegrader‐drug conjugatesmultivalencyplug‐and‐playprotein pairs

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High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
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High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

Published on: November 9, 2020

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Last Updated: May 17, 2026

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English
14:34

A Bilingual Computational Workflow for Identifying Potential PLK1 Inhibitors in American Sign Language and English

Published on: April 3, 2026

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines
05:33

High-Throughput Cellular Profiling of Targeted Protein Degradation Compounds Using HiBiT CRISPR Cell Lines

Published on: November 9, 2020

Area of Science:

  • Biochemistry
  • Molecular Biology
  • Oncology

Background:

  • Membrane proteins are crucial drug targets but challenging for traditional targeted protein degradation (TPD).
  • Over 60% of drug targets are membrane proteins, necessitating new TPD strategies.
  • Existing TPD methods show limited efficacy against these targets.

Purpose of the Study:

  • To develop a versatile platform for targeted membrane protein degradation.
  • To engineer modular TPD systems with high affinity and specificity.
  • To create novel degrader-drug conjugates for enhanced cancer therapeutics.

Main Methods:

  • Engineered a modular "plug-and-play" UPTAB (Ultrahigh-affinity Protein pairs fused to Targeting Binders) platform.
  • Utilized orthogonal ultrahigh-affinity Im/CL protein pairs for complex assembly.
  • Developed Type-I (mono), Type-II (dual), and Type-III (tri-targeted) UPTAB configurations.
  • Validated degradation efficacy in vitro and in vivo (breast cancer xenograft model).
  • Created degrader-drug conjugates (DDCs) via site-specific conjugation of MMAE payload.

Main Results:

  • UPTAB achieved near-complete degradation of EGFR and PD-L1 in cancer cell lines.
  • Type-II and Type-III UPTAB enabled simultaneous degradation of multiple targets (e.g., EGFR/c-MET).
  • Type-I UPTAB showed ~80% tumor growth inhibition, reduced EGFR levels, and extended survival in vivo.
  • DDCs retained degradation ability and demonstrated enhanced anti-proliferative activity.

Conclusions:

  • The UPTAB platform offers a modular and efficient approach for membrane protein degradation.
  • UPTAB is a versatile tool with potential for developing next-generation cancer therapeutics.
  • The platform's bioconjugation capability facilitates the creation of potent degrader-drug conjugates.