We apologize for Proteopedia being slow to respond. For the past two years, a new implementation of Proteopedia has been being built. Soon, it will replace this 18-year old system. All existing content will be moved to the new system at a date that will be announced here.

1vdv

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
[[Image:1vdv.gif|left|200px]]
+
{{Seed}}
 +
[[Image:1vdv.png|left|200px]]
<!--
<!--
Line 9: Line 10:
{{STRUCTURE_1vdv| PDB=1vdv | SCENE= }}
{{STRUCTURE_1vdv| PDB=1vdv | SCENE= }}
-
'''Bovine Milk Xanthine Dehydrogenase Y-700 Bound Form'''
+
===Bovine Milk Xanthine Dehydrogenase Y-700 Bound Form===
-
==Overview==
+
<!--
-
Y-700 (1-[3-Cyano-4-(2,2-dimethylpropoxy)phenyl]-1H-pyrazole-4-carboxylic acid) is a newly synthesized inhibitor of xanthine oxidoreductase (XOR). Steady-state kinetics with the bovine milk enzyme indicated a mixed type inhibition with K(i) and K(i) ' values of 0.6 and 3.2 nM, respectively. Titration experiments showed that Y-700 bound tightly both to the active sulfo-form and to the inactive desulfo-form of the enzyme with K(d) values of 0.9 and 2.8 nM, respectively. X-ray crystallographic analysis of the enzyme-inhibitor complex revealed that Y-700 closely interacts with the channel leading to the molybdenum-pterin active site but does not directly coordinate to the molybdenum ion. In oxonate-treated rats, orally administered Y-700 (1-10 mg/kg) dose dependently lowered plasma urate levels. At a dose of 10 mg/kg, the hypouricemic action of Y-700 was more potent and of longer duration than that of 4-hydroxypyrazolo(3,4-d)pyrimidine, whereas its action was approximately equivalent to that of 2-(3-cyano-4-isobutoxyphenyl)-4-methyl-5-thiazolecarboxylic acid, a nonpurine inhibitor of XOR. In normal rats, orally administered Y-700 (0.3-3 mg/kg) dose dependently reduced the urinary excretion of urate and allantoin, accompanied by an increase in the excretion of hypoxanthine and xanthine. Y-700 (1 mg/kg) was absorbed rapidly by the oral route with high bioavailability (84.1%). Y-700 was hardly excreted via the kidneys but was mainly cleared via the liver. These results suggest that Y-700 will be a promising candidate for the treatment of hyperuricemia and other diseases in which XOR may be involved.
+
The line below this paragraph, {{ABSTRACT_PUBMED_15190124}}, adds the Publication Abstract to the page
 +
(as it appears on PubMed at http://www.pubmed.gov), where 15190124 is the PubMed ID number.
 +
-->
 +
{{ABSTRACT_PUBMED_15190124}}
==About this Structure==
==About this Structure==
Line 34: Line 38:
[[Category: Xanthine oxidoreductase]]
[[Category: Xanthine oxidoreductase]]
[[Category: Y-700]]
[[Category: Y-700]]
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 12:25:19 2008''
+
 
 +
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 14:56:10 2008''

Revision as of 11:56, 28 July 2008

Image:1vdv.png

Template:STRUCTURE 1vdv

Bovine Milk Xanthine Dehydrogenase Y-700 Bound Form

Template:ABSTRACT PUBMED 15190124

About this Structure

1VDV is a Single protein structure of sequence from Bos taurus. Full crystallographic information is available from OCA.

Reference

Y-700 [1-[3-Cyano-4-(2,2-dimethylpropoxy)phenyl]-1H-pyrazole-4-carboxylic acid]: a potent xanthine oxidoreductase inhibitor with hepatic excretion., Fukunari A, Okamoto K, Nishino T, Eger BT, Pai EF, Kamezawa M, Yamada I, Kato N, J Pharmacol Exp Ther. 2004 Nov;311(2):519-28. Epub 2004 Jun 9. PMID:15190124

Page seeded by OCA on Mon Jul 28 14:56:10 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1vdv"
Personal tools