2009
DOI: 10.1002/dta.24
|View full text |Cite
|
Sign up to set email alerts
|

Synthesis of labeled BCX‐4208, a potent inhibitor of purine nucleoside phosphorylase

Abstract: BCX-4208, a novel inhibitor of the enzyme purine nucleoside phosphorylase, mimics the charged ribosyl oxocarbenium ion formed during the transition state of the enzyme-catalyzed C-N bond cleavage of nucleosides. A slow-onset, tight-binding inhibitor with a Ki(*) of 16 +/- 1.4 pM, BCX-4208 is one of the most potent inhibitors known for the enzyme. In support of our BCX-4208 clinical program, a mass spectrometric assay has been developed that required labeled BCX-4208 as an internal standard. The synthesis of [(… Show more

Help me understand this report

Search citation statements

Order By: Relevance

Paper Sections

Select...
1

Citation Types

0
0
0

Year Published

2010
2010
2024
2024

Publication Types

Select...
3
1

Relationship

0
4

Authors

Journals

citations
Cited by 4 publications
(1 citation statement)
references
References 6 publications
0
0
0
Order By: Relevance
“…Besides, topiroxostat, known as a novel XOD inhibitor, was under preclinical study [14] . In addition, purine nucleoside phosphorylase (PNP) was a new clinical target for uric acid management, and its inhibitor BCX4208 is in early clinical investigation in gout treatment [15] (Table 1). The biosynthesis, reabsorption and excretion of uric acid in human.…”
Section: Inhibition Of Uric Acid Biosynthesismentioning
confidence: 99%
“…Besides, topiroxostat, known as a novel XOD inhibitor, was under preclinical study [14] . In addition, purine nucleoside phosphorylase (PNP) was a new clinical target for uric acid management, and its inhibitor BCX4208 is in early clinical investigation in gout treatment [15] (Table 1). The biosynthesis, reabsorption and excretion of uric acid in human.…”
Section: Inhibition Of Uric Acid Biosynthesismentioning
confidence: 99%