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First-in-human Phase I Trial of TPST-1120, an Inhibitor of PPARα, as Monotherapy or in Combination with Nivolumab, in Patients with Advanced Solid Tumors.
Yarchoan M, Powderly JD, Bastos BR, Karasic TB, Crysler OV, Munster PN, McKean MA, Emens LA, Saenger YM, Ged Y, Stagg R, Smith S, Whiting CC, Moon A, Prasit P, Jenkins Y, Standifer N, Dubensky TW, Whiting SH, Ulahannan SV. Yarchoan M, et al. Among authors: prasit p. Cancer Res Commun. 2024 Apr 18;4(4):1100-1110. doi: 10.1158/2767-9764.CRC-24-0082. Cancer Res Commun. 2024. PMID: 38551394 Free PMC article. Clinical Trial.
Dual Blockade of EP2 and EP4 Signaling is Required for Optimal Immune Activation and Antitumor Activity Against Prostaglandin-Expressing Tumors.
Francica BJ, Holtz A, Lopez J, Freund D, Chen A, Wang D, Powell D, Kipper F, Panigrahy D, Dubois RN, Whiting CC, Prasit P, Dubensky TW. Francica BJ, et al. Among authors: prasit p. Cancer Res Commun. 2023 Aug 8;3(8):1486-1500. doi: 10.1158/2767-9764.CRC-23-0249. eCollection 2023 Aug. Cancer Res Commun. 2023. PMID: 37559947 Free PMC article.
Discovery of potent and selective PPARα/δ dual antagonists and initial biological studies.
Jacintho JD, Baccei CS, Bravo Y, Broadhead A, Chen A, Correa L, Fischer K, Laffitte B, Lee C, Lorrain DS, Messmer D, Prasit P, Stebbins KJ, Stock NS. Jacintho JD, et al. Among authors: prasit p. Bioorg Med Chem Lett. 2019 Feb 1;29(3):503-508. doi: 10.1016/j.bmcl.2018.12.045. Epub 2018 Dec 21. Bioorg Med Chem Lett. 2019. PMID: 30594433
In vitro and in vivo pharmacology of NXT629, a novel and selective PPARα antagonist.
Stebbins KJ, Broadhead AR, Cabrera G, Correa LD, Messmer D, Bundey R, Baccei C, Bravo Y, Chen A, Stock NS, Prasit P, Lorrain DS. Stebbins KJ, et al. Among authors: prasit p. Eur J Pharmacol. 2017 Aug 15;809:130-140. doi: 10.1016/j.ejphar.2017.05.008. Epub 2017 May 5. Eur J Pharmacol. 2017. PMID: 28483457
A Selective Novel Peroxisome Proliferator-Activated Receptor (PPAR)-α Antagonist Induces Apoptosis and Inhibits Proliferation of CLL Cells In Vitro and In Vivo.
Messmer D, Lorrain K, Stebbins K, Bravo Y, Stock N, Cabrera G, Correa L, Chen A, Jacintho J, Chiorazzi N, Yan XJ, Spaner D, Prasit P, Lorrain D. Messmer D, et al. Among authors: prasit p. Mol Med. 2015 Jun 9;21(1):410-9. doi: 10.2119/molmed.2015.00139. Mol Med. 2015. PMID: 26070013 Free PMC article.
Identification of the first potent, selective and bioavailable PPARα antagonist.
Bravo Y, Baccei CS, Broadhead A, Bundey R, Chen A, Clark R, Correa L, Jacintho JD, Lorrain DS, Messmer D, Stebbins K, Prasit P, Stock N. Bravo Y, et al. Among authors: prasit p. Bioorg Med Chem Lett. 2014 May 15;24(10):2267-72. doi: 10.1016/j.bmcl.2014.03.090. Epub 2014 Apr 4. Bioorg Med Chem Lett. 2014. PMID: 24745969
A role for oleoylethanolamide in chronic lymphocytic leukemia.
Masoodi M, Lee E, Eiden M, Bahlo A, Shi Y, Ceddia RB, Baccei C, Prasit P, Spaner DE. Masoodi M, et al. Among authors: prasit p. Leukemia. 2014 Jul;28(7):1381-7. doi: 10.1038/leu.2014.10. Epub 2014 Jan 13. Leukemia. 2014. PMID: 24413323
5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.
Stock NS, Bain G, Zunic J, Li Y, Ziff J, Roppe J, Santini A, Darlington J, Prodanovich P, King CD, Baccei C, Lee C, Rong H, Chapman C, Broadhead A, Lorrain D, Correa L, Hutchinson JH, Evans JF, Prasit P. Stock NS, et al. Among authors: prasit p. J Med Chem. 2011 Dec 8;54(23):8013-29. doi: 10.1021/jm2008369. Epub 2011 Nov 7. J Med Chem. 2011. PMID: 22059882
56 results