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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: cheng y. 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: cheng y. 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: cheng y. 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: cheng y. 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
Development of 2-aminooxazoline 3-azaxanthene β-amyloid cleaving enzyme (BACE) inhibitors with improved selectivity against Cathepsin D.
Low JD, Bartberger MD, Chen K, Cheng Y, Fielden MR, Gore V, Hickman D, Liu Q, Allen Sickmier E, Vargas HM, Werner J, White RD, Whittington DA, Wood S, Minatti AE. Low JD, et al. Among authors: cheng y. Medchemcomm. 2017 Apr 27;8(6):1196-1206. doi: 10.1039/c7md00106a. eCollection 2017 Jun 1. Medchemcomm. 2017. PMID: 30108829 Free PMC article.
An Orally Available BACE1 Inhibitor That Affords Robust CNS Aβ Reduction without Cardiovascular Liabilities.
Cheng Y, Brown J, Judd TC, Lopez P, Qian W, Powers TS, Chen JJ, Bartberger MD, Chen K, Dunn RT 2nd, Epstein O, Fremeau RT Jr, Harried S, Hickman D, Hitchcock SA, Luo Y, Minatti AE, Patel VF, Vargas HM, Wahl RC, Weiss MM, Wen PH, White RD, Whittington DA, Zheng XM, Wood S. Cheng Y, et al. ACS Med Chem Lett. 2014 Dec 29;6(2):210-5. doi: 10.1021/ml500458t. eCollection 2015 Feb 12. ACS Med Chem Lett. 2014. PMID: 25699151 Free PMC article.
From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1).
Cheng Y, Judd TC, Bartberger MD, Brown J, Chen K, Fremeau RT Jr, Hickman D, Hitchcock SA, Jordan B, Li V, Lopez P, Louie SW, Luo Y, Michelsen K, Nixey T, Powers TS, Rattan C, Sickmier EA, St Jean DJ Jr, Wahl RC, Wen PH, Wood S. Cheng Y, et al. J Med Chem. 2011 Aug 25;54(16):5836-57. doi: 10.1021/jm200544q. Epub 2011 Jul 29. J Med Chem. 2011. PMID: 21707077
Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer's disease.
Chen JJ, Liu Q, Yuan C, Gore V, Lopez P, Ma V, Amegadzie A, Qian W, Judd TC, Minatti AE, Brown J, Cheng Y, Xue M, Zhong W, Dineen TA, Epstein O, Human J, Kreiman C, Marx I, Weiss MM, Hitchcock SA, Powers TS, Chen K, Wen PH, Whittington DA, Cheng AC, Bartberger MD, Hickman D, Werner JA, Vargas HM, Everds NE, Vonderfecht SL, Dunn RT 2nd, Wood S, Fremeau RT Jr, White RD, Patel VF. Chen JJ, et al. Among authors: cheng y, cheng ac. Bioorg Med Chem Lett. 2015 Feb 15;25(4):767-74. doi: 10.1016/j.bmcl.2014.12.092. Epub 2015 Jan 8. Bioorg Med Chem Lett. 2015. PMID: 25613679
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