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Updated: Jul 23, 2025

Implementation of In Vitro Drug Resistance Assays: Maximizing the Potential for Uncovering Clinically Relevant Resistance Mechanisms
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Grasping cryptic binding sites to neutralize drug resistance in the field of anticancer

Wei-Cheng Yang1, Dao-Hong Gong1, Hong Wu1

  • 1National Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025, China.

Drug Discovery Today
|July 15, 2023
PubMed

Insights

Targeting cryptic binding sites (CBSs) offers a promising strategy to overcome cancer-related drug resistance (CRDR). This review highlights CBSs

Area of Science:

  • Oncology and Drug Discovery

Background:

  • Drug resistance poses a major challenge in effective cancer therapy.
  • Cryptic binding sites (CBSs) represent underexplored targets for overcoming drug resistance.

Purpose of the Study:

  • To systematically review the application of CBSs in combating cancer-related drug resistance (CRDR).
  • To identify CRDR targets and their associated CBSs, elucidate CBS mechanisms, and showcase successful applications.

Main Methods:

  • Systematic literature review and analysis of CRDR targets and their CBSs.
  • Discussion of the mechanisms by which CBSs can overcome drug resistance.
  • Compilation of successful case studies demonstrating CBS utilization in CRDR.

Main Results:

  • Identification of key cancer-related drug resistance targets and their corresponding cryptic binding sites.
  • Elucidation of the mechanisms through which CBSs can effectively target and overcome drug resistance.
  • Demonstration of successful applications of CBSs in preclinical and clinical settings for CRDR.

Conclusions:

  • Cryptic binding sites offer a viable and promising avenue for developing novel therapeutic strategies against cancer-related drug resistance.
  • This review provides a framework for researchers to leverage CBSs for the design of next-generation anti-cancer drugs.
  • Further exploration of CBSs is crucial for advancing cancer treatment and overcoming therapeutic limitations.
Keywords:
cancercryptic binding sitedrug designdrug resistancetarget drug discovery

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