Discovery and characterisation of hydrazines as inhibitors of the immune suppressive enzyme, indoleamine 2,3-dioxygenase 1 (IDO1)

Autor: Sai Parng S Fung, Sofian M. Tijono, Jack U. Flanagan, Joanne F. Jamie, Brian D. Palmer, Lai-Ming Ching, Christopher J. Squire, Haiyan Wang, Petr Tomek, David J. A. Bridewell

Publikováno v: Bioorganic & Medicinal Chemistry. 21:7595-7603

Screening of a fragment library identified 2-hydrazinobenzothiazole as a potent inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), an enzyme expressed by tumours that suppresses the immune system. Spectroscopic studies indicated that 2-hydrazinobenzo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2065a06b0acbc8f2edfeab7365d6c2e1
https://doi.org/10.1016/j.bmc.2013.10.037

Identification of human reductases that activate the dinitrobenzamide mustard prodrug PR-104A: A role for NADPH:cytochrome P450 oxidoreductase under hypoxia

Autor: Christopher P. Guise, William R. Wilson, Anke Theil, Anderson T. Wang, Adam V. Patterson, David J. A. Bridewell

Publikováno v: Biochemical Pharmacology. 74:810-820

Hypoxia is a common trait found in many solid tumours and thus represents a therapeutic target with considerable potential. PR-104, a hypoxia-activated prodrug currently in clinical trial, is a water-soluble phosphate ester which is converted in vivo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::aa8c17473c47cd18d5e2ec2bb9f2bac7
https://doi.org/10.1016/j.bcp.2007.06.014

Labeling of oxidizable proteins with a photoactivatable analog of the antitumor agent DMXAA: evidence for redox signaling in its mode of action

Autor: Brian D. Palmer, Liang-Chuan S. Wang, See-Tarn Woon, David J. A. Bridewell, Stefanie N. Vogel, Dieter Malinger, Romy Brauer, Lai-Ming Ching, Sofian M. Tijono, Kimiora Henare, Claudine Kieda

Publikováno v: Neoplasia
Neoplasia, Elsevier, 2010, 12 (9), pp.755-65
Neoplasia: An International Journal for Oncology Research, Vol 12, Iss 9, Pp 755-765 (2010)

International audience; The signaling pathway(s) and molecular target(s) for 5,6-dimethylxanthenone-4-acetic acid (DMXAA), a tumor vascular disrupting agent in late stages of clinical development, are still undefined. As an approach toward identifyin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58a75c8dc54c8b619aced6f756327c48
https://hal.science/hal-00591656

Mechanism of cytotoxicity of N-[2-(dimethylamino)ethyl] acridine-4-carboxamide and of its 7-chloro derivative: the roles of topoisomerases I and II

Autor: David J. A. Bridewell, Bruce C. Baguley, Graeme J. Finlay

Publikováno v: Cancer chemotherapy and pharmacology. 43(4)

DACA [N-[2-(dimethylamino)ethyl]acridine-4-carboxamide], an acridine derivative that is highly active against solid tumours in mice, is currently in clinical trial. The ability of DACA to overcome "atypical" (topoisomerase II-mediated) multidrug resi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ecf700f8b0a8f1ec2b034973b80f799a
https://pubmed.ncbi.nlm.nih.gov/10071981

Abstract 24: Labeling of oxidizable proteins with a photoactivatable analog of the antitumor agent DMXAA and evidence for redox signaling in its mode of action

Autor: Lai-Ming Ching, Romy Brauer, David J. A. Bridewell, Liang-Chuan S. Wang, Kimiora Henare, Brian D. Palmer

Publikováno v: Cancer Research. 70:24-24

DMXAA (5,6-dimethylxanthenone-4-acetic acid) is in late stages of clinical development as a tumor vascular disrupting agent. The signalling pathway(s) and molecular target(s) for this drug are still undefined. As an approach towards identifying poten

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::bb90fe7fbc8f0b5e8693676ecee9c656
https://doi.org/10.1158/1538-7445.am10-24