Identification and Structure-Guided Development of Pyrimidinone Based USP7 Inhibitors

Autor: Eamon Cassidy, Peter Hewitt, Elias Arkoudis, Natalie Page, Gerald Gavory, Hugues Miel, J. S. Shane Rountree, Caroline Hughes, Ewa Odrzywol, Keeva McClelland, Matthew Helm, Colin O'Dowd, Scarlett Dvorkin, Tim Harrison, Linda Jordan, Oliver Barker, Stephanie Feutren-Burton, Ewelina Rozycka, Jakub T. Flasz

Publikováno v: O'Dowd, C R, Helm, M D, Rountree, J S S, Flasz, J T, Arkoudis, E, Miel, H, Hewitt, P R, Jordan, L, Barker, O, Hughes, C, Rozycka, E, Cassidy, E, McClelland, K, Odrzywol, E, Page, N, Fuetren-Burton, S, Dvorkin, S, Gavory, G & Harrison, T 2018, ' Identification and structure-guided development of pyrimidinone based USP7 inhibitors ', ACS Medicinal Chemistry Letters, vol. 9, no. 3, pp. 238-243 . https://doi.org/10.1021/acsmedchemlett.7b00512

[Image: see text] Ubiquitin specific protease 7 (USP7, HAUSP) has become an attractive target in drug discovery due to the role it plays in modulating Mdm2 levels and consequently p53. Increasing interest in USP7 is emerging due to its potential invo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::92f42201b193e5dbba8db4243fe20048
https://pubmed.ncbi.nlm.nih.gov/29541367

Abstract 4869: Discovery and characterization of highly potent and selective USP7 inhibitors and benchmarking against clinical MDM2 antagonists

Autor: Matt Helm, Elias Arkoudis, Caroline Hughes, Jakub T. Flasz, Ewa Odrzywol, Colin O'Dowd, Gerald Gavory, Natalie Page, Eamon Cassidy, Keeva McClelland, Hugues Miel, Oliver Barker, Tim Harrison, Anthony Dossang

Publikováno v: Cancer Research. 78:4869-4869

Given the importance of USP7 in known oncogenic pathways and its emerging role in immuno-oncology, the identification of USP7 inhibitors has attracted considerable interest in the scientific community. However, despite substantial efforts over the pa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::369e45d6c4c01955b51cd4bbf0a0f259
https://doi.org/10.1158/1538-7445.am2018-4869

Zeolite NaY‐Promoted Monocyclization of Epoxy Polyene Terpenes: A Unique Route for the Direct Synthesis of Incompletely Cyclized Naturally Occurring Terpenols

Autor: Constantinos Tsangarakis, Elias Arkoudis, Christos Raptis, Manolis Stratakis

Publikováno v: Advanced Synthesis & Catalysis. 350:1587-1600

A variety of epoxy polyene terpenes cyclize readily by confinement within zeolite NaY to form primarily products of monocyclization. The monocyclization pathway is highly predominant, irrespectively of the side chain of the epoxy terpene, while the m

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7408f3e049ecde6fca627affa0d4fc89
https://doi.org/10.1002/adsc.200800180

ChemInform Abstract: Synthesis of Cordiaquinones B, C, J, and K on the Basis of a Bioinspired Approach and the Revision of the Relative Stereochemistry of Cordiaquinone C

Autor: Manolis Stratakis, Elias Arkoudis

Publikováno v: ChemInform. 39

Four members of the cordiaquinone family (cordiaquinones B, C, J, and K) were synthesized on the basis of a bioinspired scenario in five to six steps from trans,trans-farnesol. As key reactions we used the acid-catalyzed cyclization of a suitable epo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c41f69ed8a94528089385a3eefe230d1
https://doi.org/10.1002/chin.200843181

Selective Monocyclization of Epoxy Terpenoids Promoted by Zeolite NaY. A Short Biomimetic Synthesis of Elegansidiol (IV) and Farnesiferols B—D (V)—(VII)

Autor: Christos Raptis, Constantinos Tsangarakis, Elias Arkoudis, Manolis Stratakis

Publikováno v: ChemInform. 38

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::6fd413ec5f06bf6e73f34f7287e23b89
https://doi.org/10.1002/chin.200726153