Helicobacter pylori Xanthine–Guanine–Hypoxanthine Phosphoribosyltransferase—A Putative Target for Drug Discovery against Gastrointestinal Tract Infections

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61388963%3A_____%2F21%3A00542267" target="_blank" >RIV/61388963:_____/21:00542267 - isvavai.cz</a>
Result on the web
<a href="https://doi.org/10.1021/acs.jmedchem.0c02184" target="_blank" >https://doi.org/10.1021/acs.jmedchem.0c02184</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1021/acs.jmedchem.0c02184" target="_blank" >10.1021/acs.jmedchem.0c02184</a>

Result language
angličtina
Original language name
Helicobacter pylori Xanthine–Guanine–Hypoxanthine Phosphoribosyltransferase—A Putative Target for Drug Discovery against Gastrointestinal Tract Infections
Original language description
Helicobacter pylori (Hp) is a human pathogen that lives in the gastric mucosa of approximately 50% of the world’s population causing gastritis, peptic ulcers, and gastric cancer. An increase in resistance to current drugs has sparked the search for new Hp drug targets and therapeutics. One target is the disruption of nucleic acid production, which can be achieved by impeding the synthesis of 6-oxopurine nucleoside monophosphates, the precursors of DNA and RNA. These metabolites are synthesized by Hp xanthine–guanine–hypoxanthine phosphoribosyltransferase (XGHPRT). Here, nucleoside phosphonates have been evaluated, which inhibit the activity of this enzyme with Ki values as low as 200 nM. The prodrugs of these compounds arrest the growth of Hp at a concentration of 50 μM in cell-based assays. The kinetic properties of HpXGHPRT have been determined together with its X-ray crystal structure in the absence and presence of 9-[(N-3-phosphonopropyl)-aminomethyl-9-deazahypoxanthine, providing a basis for new antibiotic development.
Czech name
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Czech description
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Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
10401 - Organic chemistry

Project
<a href="/en/project/GA19-07707S" target="_blank" >GA19-07707S: Acyclic nucleoside phosphonates as potential inhibitors of adenine phosphoribosyltransferases in human trypanosomatid parasites</a><br>
Continuities
I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year
2021
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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