Drug Mimicry: Promiscuous Receptors PXR and AhR, and Microbial Metabolite Interactions in the Intestine
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F20%3A73602178" target="_blank" >RIV/61989592:15310/20:73602178 - isvavai.cz</a>
Result on the web
<a href="https://www.sciencedirect.com/science/article/pii/S0165614720302200" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0165614720302200</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1016/j.tips.2020.09.013" target="_blank" >10.1016/j.tips.2020.09.013</a>
Alternative languages
Result language
angličtina
Original language name
Drug Mimicry: Promiscuous Receptors PXR and AhR, and Microbial Metabolite Interactions in the Intestine
Original language description
Significant attrition limits drug discovery. The available chemical entities present with drug-like features contribute to this limitation. Using specific examples of promiscuous receptor-ligand interactions, a case is made for expanding the chemical space for drug-like molecules. These ligand-receptor interactions are poor candidates for the drug discovery process. However, provided herein are specific examples of ligand-receptor or transcription-factor interactions, namely, the pregnane X receptor (PXR) and the aryl hydrocarbon receptor (AhR), and its interactions with microbial metabolites. Discrete examples of microbial metabolite mimicry are shown to yield more potent and non-toxic therapeutic leads for pathophysiological conditions regulated by PXR and AhR. These examples underscore the opinion that microbial metabolite mimicry of promiscuous ligand-receptor interactions is warranted, and will likely expand the existing chemical space of drugs.
Czech name
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Czech description
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Classification
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
30104 - Pharmacology and pharmacy
Result continuities
Project
<a href="/en/project/NV19-05-00220" target="_blank" >NV19-05-00220: ACTIVATORS OF HUMAN ARYL HYDROCARBON RECEPTOR (AHR) IN THE THERAPY OF INFLAMMATORY BOWEL DISEASE</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2020
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
TRENDS IN PHARMACOLOGICAL SCIENCES
ISSN
0165-6147
e-ISSN
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Volume of the periodical
41
Issue of the periodical within the volume
12
Country of publishing house
GB - UNITED KINGDOM
Number of pages
9
Pages from-to
900-908
UT code for WoS article
000591072300002
EID of the result in the Scopus database
2-s2.0-85093646327