SAR Development of Lysine-Based Irreversible Inhibitors of Transglutaminase 2 for Huntington's Disease

Autor:	Sabine Schaertl, Celia Dominguez, Douglas Macdonald, Maria Beconi, Marie Li, Stephen Martin Courtney, Ignacio Munoz-Sanjuan, Sayeh Erfan, Richard W Marston, Frederick Arthur Brookfield, Darshan Gunvant Vaidya, Anna Pedret-Dunn, Michael Prime, Laura Reed, Peter Johnson, John Wityak, Siw F. Johnsen
Rok vydání:	2012
Předmět:	Dipeptide biology Tissue transglutaminase business.industry Organic Chemistry Lysine Pharmacology medicine.disease Biochemistry In vitro Polar surface area chemistry.chemical_compound chemistry Huntington's disease Acrylamide Drug Discovery biology.protein medicine business ADME
Zdroj:	ACS Medicinal Chemistry Letters. 3:1024-1028
ISSN:	1948-5875
DOI:	10.1021/ml300241m
Popis:	We report a series of irreversible transglutaminase 2 inhibitors starting from a known lysine dipeptide bearing an acrylamide warhead. We established new SARs resulting in compounds demonstrating improved potency and better physical and calculated properties. Transglutaminase selectivity profiling and in vitro ADME properties of selected compounds are also reported.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::876741143e5614a16215dc697c0077d5 https://doi.org/10.1021/ml300241m Zobrazit plný text záznamu