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A GIPR antagonist conjugated to GLP-1 analogues promotes weight loss with improved metabolic parameters in preclinical and phase 1 settings.
Véniant MM, Lu SC, Atangan L, Komorowski R, Stanislaus S, Cheng Y, Wu B, Falsey JR, Hager T, Thomas VA, Ambhaikar M, Sharpsten L, Zhu Y, Kurra V, Jeswani R, Oberoi RK, Parnes JR, Honarpour N, Neutel J, Strande JL. Véniant MM, et al. Among authors: falsey jr. Nat Metab. 2024 Feb;6(2):290-303. doi: 10.1038/s42255-023-00966-w. Epub 2024 Feb 5. Nat Metab. 2024. PMID: 38316982 Free PMC article. Clinical Trial.
GIPR antagonist antibodies conjugated to GLP-1 peptide are bispecific molecules that decrease weight in obese mice and monkeys.
Lu SC, Chen M, Atangan L, Killion EA, Komorowski R, Cheng Y, Netirojjanakul C, Falsey JR, Stolina M, Dwyer D, Hale C, Stanislaus S, Hager T, Thomas VA, Harrold JM, Lloyd DJ, Véniant MM. Lu SC, et al. Among authors: falsey jr. Cell Rep Med. 2021 Apr 30;2(5):100263. doi: 10.1016/j.xcrm.2021.100263. eCollection 2021 May 18. Cell Rep Med. 2021. PMID: 34095876 Free PMC article.
Use of Cryopreserved Hepatocytes as Part of an Integrated Strategy to Characterize In Vivo Clearance for Peptide-Antibody Conjugate Inhibitors of Nav1.7 in Preclinical Species.
Foti RS, Biswas K, Aral J, Be X, Berry L, Cheng Y, Conner K, Falsey JR, Glaus C, Herberich B, Hickman D, Ikotun T, Li H, Long J, Huang L, Miranda LP, Murray J, Moyer B, Netirojjanakul C, Nixey TE, Sham K, Soto M, Tegley CM, Tran L, Wu B, Yin L, Rock DA. Foti RS, et al. Among authors: falsey jr. Drug Metab Dispos. 2019 Oct;47(10):1111-1121. doi: 10.1124/dmd.119.087742. Epub 2019 Aug 6. Drug Metab Dispos. 2019. PMID: 31387871
Engineering NaV1.7 Inhibitory JzTx-V Peptides with a Potency and Basicity Profile Suitable for Antibody Conjugation To Enhance Pharmacokinetics.
Murray JK, Wu B, Tegley CM, Nixey TE, Falsey JR, Herberich B, Yin L, Sham K, Long J, Aral J, Cheng Y, Netirojjanakul C, Doherty L, Glaus C, Ikotun T, Li H, Tran L, Soto M, Salimi-Moosavi H, Ligutti J, Amagasu S, Andrews KL, Be X, Lin MJ, Foti RS, Ilch CP, Youngblood B, Kornecook TJ, Karow M, Walker KW, Moyer BD, Biswas K, Miranda LP. Murray JK, et al. Among authors: falsey jr. ACS Chem Biol. 2019 Apr 19;14(4):806-818. doi: 10.1021/acschembio.9b00183. Epub 2019 Mar 27. ACS Chem Biol. 2019. PMID: 30875193
Engineering Antibody Reactivity for Efficient Derivatization to Generate NaV1.7 Inhibitory GpTx-1 Peptide-Antibody Conjugates.
Biswas K, Nixey TE, Murray JK, Falsey JR, Yin L, Liu H, Gingras J, Hall BE, Herberich B, Holder JR, Li H, Ligutti J, Lin MJ, Liu D, Soriano BD, Soto M, Tran L, Tegley CM, Zou A, Gunasekaran K, Moyer BD, Doherty L, Miranda LP. Biswas K, et al. Among authors: falsey jr. ACS Chem Biol. 2017 Sep 15;12(9):2427-2435. doi: 10.1021/acschembio.7b00542. Epub 2017 Aug 28. ACS Chem Biol. 2017. PMID: 28800217
N-substituted azaindoles as potent inhibitors of Cdc7 kinase.
Bryan MC, Falsey JR, Frohn M, Reichelt A, Yao G, Bartberger MD, Bailis JM, Zalameda L, Miguel TS, Doherty EM, Allen JG. Bryan MC, et al. Among authors: falsey jr. Bioorg Med Chem Lett. 2013 Apr 1;23(7):2056-60. doi: 10.1016/j.bmcl.2013.02.007. Epub 2013 Feb 13. Bioorg Med Chem Lett. 2013. PMID: 23481650
12 results