15174-02-4Relevant articles and documents
Photochemical nucleophile mapping: Identification of Tyr311 within the catalytic domain of rabbit muscle glyceraldehyde-3-phosphate dehydrogenase
Hatanaka, Yasumaru,Kaneda, Masaki,Tomohiro, Takenori
, p. 213 - 217 (2007)
Photochemical mapping of nucleophiles in close proximity to the active site Cys149 of rabbit glyceraldehyde-3-phosphate dehydrogenase (GAPDH) was demonstrated based on the nucleophilic aromatic photosubstitution reaction using two regioisomers of alkoxy-fluoro-nitro-substituted benzenes. Two photophores were covalently attached to the active site SH group of GAPDH and the protein was subjected to photolysis then to the cyanogen bromide cleavage reaction. The advantage of this method is the capability to chase labeled products by monitoring absorption at 380 nm because of the chromogenic property of photophore. HPLC separation identified a large labeled peptide fragment that was further digested by V8 protease for Edman sequence analysis. From the recent X-ray crystallography of rabbit GAPDH, Tyr311, His176, Ser238 and Lys183 are closely located to catalytic Cys149. Among these nucleophiles, Tyr311 was preferentially labeled with 2-fluoro-4-nitrophenoxy photophore and no label was identified with the isomeric 4-fluoro-2-nitrophenoxy photophore. The result clearly reflects the distance between Cys149 and nucleophiles to distinguish the nearest Tyr311. As photophores show great reactivity even with water under neutral conditions, the distance between nucleophiles and photophores is important for photo-induced nucleophilic aromatic substitution. The method will provide a useful technique to survey nucleophiles within the catalytic domain.
NOVEL ARYL-CYANOGUANIDINE COMPOUNDS
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, (2016/07/05)
The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory substituted cyanoguanidine-pyrazolines of general formula (I) wherein R1, R2/s
METABOLITES OF 1-{3-4`4-(2-METHOXYPHENYL) PIPERAZIN-1-YL!-PROPYL}-PIPERIDINE-2, 6-DIONE FOR USE IN THE TREATMENT OF BENIGN PROSTATIC HYPERPLASIA
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Page/Page column 18-19, (2010/02/11)
The present invention relates to the metabolites of 1-{3-[4-(2-Methoxyphenyl) piperazin-1-yl]-propyl}-piperidine-2, 6-dione of Formula (I). The disclosed compounds can function as α1a-adrenceptor antagonists and thus can be used for the treatme
2, 4- DI (PHENYLAMINO) PYRIMIDINES USEFUL IN THE TREATMENT OF NEOPLASTIC DISEASES, INFLAMMATORY AND IMMUNE SYSTEM DISORDERS
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Page 136, (2010/02/08)
Novel pyrimidine derivatives of formula (I), to processes for their production, their use as pharmaceuticals in the treatment of neoplastic diseases, inflammatory and immune system disorders and to pharmaceutical compositions comprising them.
9-(P-phenylazoanilino)-7-methyl-1H-imidazo[4,5-f]quinolines
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, (2008/06/13)
A series of 9-(substituted amino)imidazo[4,5-f]quinolines are effective anthelmintic agents; particularly in respect to the tapeworm Hymenolepis nana.