Search results for: UGT OVEREXPRESSION

• Metabolic transformation of antitumor acridinone C-1305 but not C-1311 via selective cellular expression of UGT1A10 increases cytotoxic response: implications for clinical use.

  Publication

  • M. Pawłowska
  • R. Chu
  • B. Fedejko-Kap
  • E. Augustin
  • Z. Mazerska
  • A. Radominska-Pandya
  • T. C. Chambers

  - DRUG METABOLISM AND DISPOSITION - Year 2013

  The acridinone derivates C-1305 and C-1311 are promising antitumor agents with high activity against several experimental cellular and tumor models and which are under evaluation in pre-clinical and early phase clinical trials. Recent evidence from our laboratories has indicated that both compounds were conjugated by several UGT isoforms with the most active being extrahepatic UGT1A10. The present studies were designed to test...

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• The role of glucuronidation in drug resistance

  Publication

  • Z. Mazerska
  • A. Mróz
  • M. Pawłowska
  • E. Augustin

  - PHARMACOLOGY & THERAPEUTICS - Year 2016

  The final therapeutic effect of a drug candidate, which is directed to a specific molecular target strongly depends on its absorption, distribution, metabolism and excretion (ADME). The disruption of at least one element of ADME may result in serious drug resistance. In this work we described the role of one element of this resistance: phase II metabolism with UDP-glucuronosyltransferases (UGTs). UGT function is the transformation...

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