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Reversal of multidrug resistance by the staurosporine derivatives CGP 41251 and CGP 42700.

Author: GrunickeH, HilbeW, HofmannJ, LudescherC, RegenassU, RybczynskaM, SpitalerM, UtzI

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Overview

CGP 42700, a staurosporine derivative with low protein kinase C inhibiting activity, effectively reversed mdr1-mediated multidrug resistance in cancer cells, similar to CGP 41251, a known protein kinase C inhibitor. CGP 42700 may be less toxic and have fewer side effects than other chemosensitizers because it does not inhibit protein kinase C or cell proliferation.
Paper Details　
Original Abstract of the Article :
It has been shown previously that the staurosporine derivative CGP 41251, a specific inhibitor of protein kinase C (IC50 = 50 nM), exhibits antitumor activity and reverses mdr1 mediated multidrug resistance. At present, the compound is evaluated as an anticancer drug in clinical phase I trials. We c...See full text at original site
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引用元：
https://doi.org/10.1002/(sici)1097-0215(19980703)77:1<64::aid-ijc11>3.0.co;2-9

データ提供：米国国立医学図書館（NLM）

Multidrug Resistance: Unveiling the Potential of Staurosporine Derivatives

The battle against cancer is often likened to navigating a vast desert, where every step forward is a victory. Multidrug resistance (MDR), a formidable obstacle in cancer treatment, makes this journey even more arduous. This study explores the potential of staurosporine derivatives, novel compounds, to overcome this challenge.

The authors compare the effects of two staurosporine derivatives, CGP 41251 and CGP 42700, on reversing MDR. Their findings suggest that both compounds effectively reverse MDR, with CGP 42700 exhibiting a greater ability to inhibit rhodamine 123 efflux, a marker of MDR.

This study offers hope for developing new therapies to overcome MDR, a significant hurdle in cancer treatment.

A New Oasis in the Desert of Multidrug Resistance

This research highlights the potential of staurosporine derivatives, particularly CGP 42700, in overcoming MDR. The study's findings provide a ray of hope for developing new strategies to combat this major challenge in cancer therapy.

Hope for Cancer Patients

This research offers a glimmer of hope for cancer patients facing the obstacle of MDR. The authors' findings inspire further research into the potential of staurosporine derivatives and other promising compounds to overcome this formidable challenge.

Dr.Camel's Conclusion

This study represents a significant step forward in the ongoing quest to conquer MDR. By uncovering the potential of staurosporine derivatives, this research offers a path forward for developing new therapies that can effectively combat this formidable obstacle in cancer treatment.

Date :
  1. Date Completed 1998-07-07
  2. Date Revised 2019-07-08
Further Info :

Pubmed ID

9639395

DOI: Digital Object Identifier

10.1002/(sici)1097-0215(19980703)77:1<64::aid-ijc11>3.0.co;2-9

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