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Pathological angiogenesis in retinopathy engages cellular senescence and is amenable to therapeutic elimination via BCL-xL inhibition.
Crespo-Garcia S, Tsuruda PR, Dejda A, Ryan RD, Fournier F, Chaney SY, Pilon F, Dogan T, Cagnone G, Patel P, Buscarlet M, Dasgupta S, Girouard G, Rao SR, Wilson AM, O'Brien R, Juneau R, Guber V, Dubrac A, Beausejour C, Armstrong S, Mallette FA, Yohn CB, Joyal JS, Marquess D, Beltran PJ, Sapieha P. Crespo-Garcia S, et al. Among authors: marquess d. Cell Metab. 2021 Apr 6;33(4):818-832.e7. doi: 10.1016/j.cmet.2021.01.011. Epub 2021 Feb 5. Cell Metab. 2021. PMID: 33548171 Free article.
Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT(4) receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation.
Long DD, Armstrong SR, Beattie DT, Choi SK, Fatheree PR, Gendron RA, Genov D, Goldblum AA, Humphrey PP, Jiang L, Marquess DG, Shaw JP, Smith JA, Turner SD, Vickery RG. Long DD, et al. Among authors: marquess dg. Bioorg Med Chem Lett. 2012 Oct 1;22(19):6048-52. doi: 10.1016/j.bmcl.2012.08.051. Epub 2012 Aug 21. Bioorg Med Chem Lett. 2012. PMID: 22959244
Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: clinical compound TD-2749.
Long DD, Armstrong SR, Beattie DT, Choi SK, Fatheree PR, Gendron RA, Goldblum AA, Humphrey PP, Marquess DG, Shaw JP, Smith JA, Derek Turner S, Vickery RG. Long DD, et al. Among authors: marquess dg. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4849-53. doi: 10.1016/j.bmcl.2012.05.034. Epub 2012 May 15. Bioorg Med Chem Lett. 2012. PMID: 22683222
Senescent cells: an emerging target for diseases of ageing.
Childs BG, Gluscevic M, Baker DJ, Laberge RM, Marquess D, Dananberg J, van Deursen JM. Childs BG, et al. Among authors: marquess d. Nat Rev Drug Discov. 2017 Oct;16(10):718-735. doi: 10.1038/nrd.2017.116. Epub 2017 Jul 21. Nat Rev Drug Discov. 2017. PMID: 28729727 Free PMC article. Review.
A multivalent approach towards linked dual-pharmacology prostaglandin F receptor agonist/carbonic anhydrase-II inhibitors for the treatment of glaucoma.
Long DD, Frieman B, Hegde SS, Hill CM, Jiang L, Kintz S, Marquess DG, Purkey H, Shaw JP, Steinfeld T, Wilson MS, Wrench K. Long DD, et al. Among authors: marquess dg. Bioorg Med Chem Lett. 2013 Feb 15;23(4):939-43. doi: 10.1016/j.bmcl.2012.12.058. Epub 2012 Dec 22. Bioorg Med Chem Lett. 2013. PMID: 23317571
Discovery of TD-0212, an Orally Active Dual Pharmacology AT1 Antagonist and Neprilysin Inhibitor (ARNI).
McKinnell RM, Fatheree P, Choi SK, Gendron R, Jendza K, Olson Blair B, Budman J, Hill CM, Hegde LG, Yu C, McConn D, Hegde SS, Marquess DG, Klein U. McKinnell RM, et al. Among authors: marquess dg. ACS Med Chem Lett. 2018 Dec 3;10(1):86-91. doi: 10.1021/acsmedchemlett.8b00462. eCollection 2019 Jan 10. ACS Med Chem Lett. 2018. PMID: 30655952 Free PMC article.
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