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Abstract P3-07-15: Preliminary data from a Phase 1b dose escalation study of OP-1250, an oral CERAN, in combination with palbociclib in patients with advanced and/or metastatic estrogen receptor (ER)-positive, HER2-negative breast cancer

Autor: Arlene Chan, Daphne Day, Rina Hui, Nicole McCarthy, Rosalind Wilson, Demiana Faltaos, Morena Shaw, Caitlin Murphy

Publikováno v: Cancer Research. 83:P3-07

Background: OP-1250 is a small molecule oral complete estrogen receptor antagonist (CERAN) that binds the ligand binding domain of the ER and completely blocks ER-driven transcriptional activity. CDK4/6 inhibitors in combination with endocrine therap

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0d41f285d79aeb774c3a994db453fd47
https://doi.org/10.1158/1538-7445.sabcs22-p3-07-15

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State-Dependent Allosteric Inhibition of the Human SLC13A5 Citrate Transporter by Hydroxysuccinic Acids, PF-06649298 and PF-06761281

Autor: Simon A. Hinke, Marie-Laure Rives, Bin Zhu, Morena Shaw, Alan D. Wickenden

Publikováno v: Molecular pharmacology. 90(6)

In the liver, citrate is a key metabolic intermediate involved in the regulation of glycolysis and lipid synthesis and reduced expression of the hepatic citrate SLC13A5 transporter has been shown to improve metabolic outcomes in various animal models

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fd31bed4ec7b92331db936ca5cee0814
https://pubmed.ncbi.nlm.nih.gov/27754898

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Akademický článek

ASCPT News.

Publikováno v: Clinical Pharmacology & Therapeutics; Mar2020, Vol. 107 Issue 3, p486-491, 6p

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