38585-61-4Relevant articles and documents
Aminooxy analog of histamine is an efficient inhibitor of mammalian l-histidine decarboxylase: Combined in silico and experimental evidence
Castro-Oropeza,Pino-Angeles,Khomutov,Urdiales,Moya-Garcia,Vepsaelaeinen,Persson,Sarabia,Khomutov,Sanchez-Jimenez
, p. 621 - 631 (2014)
Histamine plays highlighted roles in the development of many common, emergent and rare diseases. In mammals, histamine is formed by decarboxylation of l-histidine, which is catalyzed by pyridoxal-5′-phosphate (PLP) dependent histidine decarboxylase (HDC, EC 4.1.1.22). The limited availability and stability of the protein have delayed the characterization of its structure-function relationships. Our previous knowledge on mammalian HDC, derived from both in silico and experimental approaches, indicates that an effective competitive inhibitor should be capable to form an "external aldimine-like structure" and have an imidazole group, or its proper mimetic, which provides additional affinity of PLP-inhibitor adduct to the HDC active center. This is confirmed using HEK-293 cells transfected to express human HDC and the aminooxy analog of histidine, 4(5)-aminooxymethylimidazole (O-IMHA, IC50 ≈ 2 × 10-7M) capable to form a PLP-inhibitor complex (oxime) in the enzyme active center. Taking advantage of the availability of the human HDC X-ray structure, we have also determined the potential interactions that could stabilize this oxime in the active site of mammalian HDC.
THIAZOLOPYRIDINONE DERIVATES AS MCH RECEPTOR ANTAGONISTS
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Page/Page column 99, (2008/06/13)
The present invention relates to a melanin concentrating hormone antagonist compound of formula (I); wherein w, R1, q, p, R2, t, Ar1, L1, R3 and R4 are as defined, or a pharmaceutically acceptable salt, solvate, or enantiomer thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.
Cholecystokinin antagonists
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, (2008/06/13)
Benzodiazepine analogs of the formula: STR1 are disclosed which are antagonists of gastrin and cholecystokinin (CCK).