Benzbromarone Analog SAR: Potent hURAT1 (SLC22A12) Inhibitors and Drug Transporter Interaction Studies

These results illustrate that the K<sub>m</sub> for [<sup>14</sup>C]UA uptake was not altered in the presence of <b>2</b> or <b>3</b>, but rather the V<sub>max</sub> was reduced in the presence of inhibitors when added to the uptake solutions. As a result, these data support the notion that <b>2</b> and <b>3</b> inhibit [<sup>14</sup>C]UA uptake by non-competitive inhibition and not at the URAT1 binding site.

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Publication Details

Journal
Drug Design Development and Therapy
Published
2025-02-01
DOI
https://doi.org/10.2147/dddt.s474398
Citations
3
Primary Topic
Gout, Hyperuricemia, Uric Acid
Type
article
Field-Weighted Citation Impact
4.29

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article

Benzbromarone Analog SAR: Potent hURAT1 (SLC22A12) Inhibitors and Drug Transporter Interaction Studies

Janet Lightner, Vijay Kumar, Michael F. Wempe, Peter J. Rice et al.
3 citations
Drug Design Development and Therapy
Gout, Hyperuricemia, Uric Acid
4.29
article

Benzbromarone Analog SAR: Potent hURAT1 (SLC22A12) Inhibitors and Drug Transporter Interaction Studies

Janet Lightner, Vijay Kumar, Michael F. Wempe, Peter J. Rice, Naohiko Anzai, Promsuk Jutabha, Hitoshi Endou
article en
3 citations

Abstract

These results illustrate that the K<sub>m</sub> for [<sup>14</sup>C]UA uptake was not altered in the presence of <b>2</b> or <b>3</b>, but rather the V<sub>max</sub> was reduced in the presence of inhibitors when added to the uptake solutions. As a result, these data support the notion that <b>2</b> and <b>3</b> inhibit [<sup>14</sup>C]UA uptake by non-competitive inhibition and not at the URAT1 binding site.

Drug Design Development and TherapyVol. Volume 19
East Tennessee State University (US), Chiba University (JP), Kyorin University (JP), Mahidol University (TH), University of Colorado Cancer Center (US), Ramathibodi Hospital (TH), University of Colorado Anschutz Medical Campus (US), Dokkyo Medical University (JP), Kentucky State University (US), University of Colorado Denver (US)
East Tennessee State University, Japan Society for the Promotion of Science
Openalex Percentile: Top 7%
Gout, Hyperuricemia, Uric Acid
4.29
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Benzbromarone Analog SAR: Potent hURAT1 (SLC22A12) Inhibitors and Drug Transporter Interaction Studies — Janet Lightner, Vijay Kumar, et al. · Drug Design Development and Therapy (2025) | TGRS Research Map | TGRS