Glucose 6-Phosphate Dehydrogenase from Trypanosomes: Selectivity for Steroids and Chemical Validation in Bloodstream Trypanosoma brucei

Autor: Francesca Moraca, Marc Laverriere, Niall M. Hamilton, Allan M. Jordan, Marcelo A. Comini, Cecilia Ortíz

Publikováno v: Molecules
Volume 26
Issue 2
Molecules, Vol 26, Iss 358, p 358 (2021)

Glucose 6-phosphate dehydrogenase (G6PDH) fulfills an essential role in cell physiology by catalyzing the production of NADPH+ and of a precursor for the de novo synthesis of ribose 5-phosphate. In trypanosomatids, G6PDH is essential for in vitro pro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::df99459684d309ddd9f253be4f533dc9

Cell-active Small Molecule Inhibitors of the DNA-damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides

Autor: Julie A. Tucker, Ben Acton, Ian D. Waddell, Alexandra Stowell, Nicola Hamilton, Niall M. Hamilton, Kate M. Smith, Stuart Donald Jones, James R. Hitchin, Bohdan Waszkowycz, Alison E. McGonagle, Dominic I. James, Allan M. Jordan, Daniel P. Mould, Clifford David Jones, Colin Hutton, Helen F. Small, Emma E. Fairweather, Donald J. Ogilvie, Louise A. Griffiths

Publikováno v: Waszkowycz, B, Smith, K, Mcgonagle, A, Jordan, A, Acton, B, Fairweather, E, Griffiths, L, Hamilton, N M, Hamilton, N, Hitchin, J R, Hutton, C, James, D I, Jones, C D, Jones, S, Mould, D, Small, H F, Stowell, A, Tucker, J, Waddell, I & Ogilvie, D J 2018, ' Cell-active Small Molecule Inhibitors of the DNA-damage Repair Enzyme Poly(ADP-ribose) Glycohydrolase (PARG): Discovery and Optimization of Orally Bioavailable Quinazolinedione Sulfonamides ', Journal of Medicinal Chemistry, vol. 61, no. 23, pp. 10767–10792 . https://doi.org/10.1021/acs.jmedchem.8b01407

DNA damage repair enzymes are promising targets in the development of new therapeutic agents for a wide range of cancers and potentially other diseases. The enzyme poly(ADP-ribose) glycohydrolase (PARG) plays a pivotal role in the regulation of DNA r

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e713bd6a754c7026f2f63ab3b3df4e2
https://doi.org/10.1021/acs.jmedchem.8b01407

Discovery of potent inhibitors of the lysophospholipase autotaxin

Autor: Mar Jimenez Quesada, Ellen Catherine Macdonald, Allan M. Jordan, Caroline Foxton, Huib Ovaa, Pritom Shah, Elisabeth Trivier, Aurore Lejeune, Tony Raynham, Wouter H. Moolenaar, Muddasar Farooq, Martin Stockley, P.J. Owen, James R. Hitchin, Jana Skeete, Michelle Pritchard, Irene Farre Gutierrez, Hamish Ryder, Niall M. Hamilton, Andrew P. Turnbull, Anne Cheasty, Leon Pang, Alexandra Stowell, Susan M. Boyd

Publikováno v: Bioorganic and Medicinal Chemistry Letters, 26(22), 5403-5410

The autotaxin-lysophosphatidic acid (ATX-LPA) axis has been implicated in several disease conditions including inflammation, fibrosis and cancer. This makes ATX an attractive drug target and its inhibition may lead to useful therapeutic agents. Throu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2a7b70a8962d8c311e0ac46deffdc0f8
https://hdl.handle.net/1887/111844

A novel scalable and stereospecific synthesis of 3α- and 3β-amino-5α-androstan-17-ones and 3α- and 3β-amino-5α-pregnan-20-ones

Autor: Allan M. Jordan, James R. Hitchin, Donald J. Ogilvie, Amanda J. Lyons, Niall M. Hamilton

Publikováno v: Tetrahedron Letters. 53:2868-2872

A novel scalable stereoselective synthesis of 3α- and 3β-amino-5α-androstan-17-ones and 3α- and 3β-amino-5α-pregnan-20-ones has been developed using phthalimide based Mitsunobu chemistry. In all four cases, the products were isolated as single

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::11ddd0cbc2d906eb722cfa69b548d509
https://doi.org/10.1016/j.tetlet.2012.03.124

Structural Basis for Agonism and Antagonism for a Set of Chemically Related Progesterone Receptor Modulators

Autor: Ross McGuire, Rolien Bosch, Jacob de Vlieg, Niall M. Hamilton, Olaf Nimz, Koen J. Dechering, Angus R. Brown, Scott J. Lusher, Tsang Wai Lam, Arthur Oubrie, Diep Vu-Pham, Hans C.A. Raaijmakers

Publikováno v: Journal of Biological Chemistry, 286, 35079-35086
Journal of Biological Chemistry, 286, 40, pp. 35079-35086

The progesterone receptor is able to bind to a large number and variety of ligands that elicit a broad range of transcriptional responses ranging from full agonism to full antagonism and numerous mixed profiles inbetween. We describe here two new pro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dfe67a191b82ca4f7414febeccbc79a8
https://doi.org/10.1074/jbc.m111.273029