Pre-clinical activity of PR-104 as monotherapy and in combination with sorafenib in hepatocellular carcinoma

Phase I/II study of the hypoxia-activated prodrug PR104 in refractory/relapsed acute myeloid leukemia and acute lymphoblastic leukemia

(2015) M. Konopleva et al.   HAEMATOLOGICA

Phase I/II study of the hypoxia-activated prodrug PR104 in refractory/relapsed acute myeloid leukemia and acute lymphoblastic leukemia

(2015) M. Konopleva et al.   HAEMATOLOGICA

A novel fluorometric assay for aldo-keto reductase 1C3 predicts metabolic activation of the nitrogen mustard prodrug PR-104A in human leukaemia cells

(2014) Stephen M.F. Jamieson et al.   BIOCHEMICAL PHARMACOLOGY

Morpholylureas are a new class of potent and selective inhibitors of the type 5 17-β-hydroxysteroid dehydrogenase (AKR1C3)

(2014) Jack U. Flanagan et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Sorafenib-based combination as a first line treatment for advanced hepatocellular carcinoma: A systematic review of the literature

(2014) Omar Abdel-Rahman et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Patient-derived models of acquired resistance can identify effective drug combinations for cancer

(2014) Adam S. Crystal et al.   SCIENCE

Hypoxia-mediated sorafenib resistance can be overcome by EF24 through Von Hippel-Lindau tumor suppressor-dependent HIF-1α inhibition in hepatocellular carcinoma

(2013) Yingjian Liang et al.   HEPATOLOGY

The Nrf2 cell defence pathway: Keap1-dependent and -independent mechanisms of regulation

(2012) Holly K. Bryan et al.   BIOCHEMICAL PHARMACOLOGY

Sorafenib Inhibits Hypoxia-Inducible Factor-1  Synthesis: Implications for Antiangiogenic Activity in Hepatocellular Carcinoma

(2012) L.-p. Liu et al.   CLINICAL CANCER RESEARCH

Evaluation of changes in the tumor microenvironment after sorafenib therapy by sequential histology and 18F-fluoromisonidazole hypoxia imaging in renal cell carcinoma

(2012) MASAHIRO MURAKAMI et al.   INTERNATIONAL JOURNAL OF ONCOLOGY

PR-104 plus sorafenib in patients with advanced hepatocellular carcinoma

(2011) Ghassan K. Abou-Alfa et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Glucuronidation of Anticancer Prodrug PR-104A: Species Differences, Identification of Human UDP-Glucuronosyltransferases, and Implications for Therapy

(2011) Y. Gu et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

A combined pharmacokinetic model for the hypoxia-targeted prodrug PR-104A in humans, dogs, rats and mice predicts species differences in clearance and toxicity

(2010) Kashyap Patel et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

The Bioreductive Prodrug PR-104A Is Activated under Aerobic Conditions by Human Aldo-Keto Reductase 1C3

(2010) C. P. Guise et al.   CANCER RESEARCH

DNA Cross-Links in Human Tumor Cells Exposed to the Prodrug PR-104A: Relationships to Hypoxia, Bioreductive Metabolism, and Cytotoxicity

(2009) R. S. Singleton et al.   CANCER RESEARCH

Characterization of the cancer chemopreventive NRF2-dependent gene battery in human keratinocytes: demonstration that the KEAP1–NRF2 pathway, and not the BACH1–NRF2 pathway, controls cytoprotection against electrophiles as well as redox-cycling compounds

(2009) A.Kenneth MacLeod et al.   CARCINOGENESIS

Metabolism and Excretion of the Novel Bioreductive Prodrug PR-104 in Mice, Rats, Dogs, and Humans

(2009) Y. Gu et al.   DRUG METABOLISM AND DISPOSITION

Rapid and sensitive ultra-high-pressure liquid chromatography–tandem mass spectrometry analysis of the novel anticancer agent PR-104 and its major metabolites in human plasma: Application to a pharmacokinetic study

(2009) Yongchuan Gu et al.   JOURNAL OF CHROMATOGRAPHY B-ANALYTICAL TECHNOLOGIES IN THE BIOMEDICAL AND LIFE SCIENCES

Roles of DNA repair and reductase activity in the cytotoxicity of the hypoxia-activated dinitrobenzamide mustard PR-104A

(2009) Y. Gu et al.   MOLECULAR CANCER THERAPEUTICS

The tumor microenvironment and metastatic disease

(2008) Sarah Jane Lunt et al.   CLINICAL & EXPERIMENTAL METASTASIS

Imaging Induction of Cytoprotective Enzymes in Intact Human Cells: Coumberone, a Metabolic Reporter for Human AKR1C Enzymes Reveals Activation by Panaxytriol, an Active Component of Red Ginseng

(2008) Marlin Halim et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Efficacy and safety of sorafenib in patients in the Asia-Pacific region with advanced hepatocellular carcinoma: a phase III randomised, double-blind, placebo-controlled trial

(2008) Ann-Lii Cheng et al.   LANCET ONCOLOGY

Sorafenib in Advanced Hepatocellular Carcinoma

(2008) Josep M. Llovet et al.   NEW ENGLAND JOURNAL OF MEDICINE