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Page 1
From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9.
Petrilli WL, Adam GC, Erdmann RS, Abeywickrema P, Agnani V, Ai X, Baysarowich J, Byrne N, Caldwell JP, Chang W, DiNunzio E, Feng Z, Ford R, Ha S, Huang Y, Hubbard B, Johnston JM, Kavana M, Lisnock JM, Liang R, Lu J, Lu Z, Meng J, Orth P, Palyha O, Parthasarathy G, Salowe SP, Sharma S, Shipman J, Soisson SM, Strack AM, Youm H, Zhao K, Zink DL, Zokian H, Addona GH, Akinsanya K, Tata JR, Xiong Y, Imbriglio JE. Petrilli WL, et al. Among authors: lisnock jm. Cell Chem Biol. 2020 Jan 16;27(1):32-40.e3. doi: 10.1016/j.chembiol.2019.10.002. Epub 2019 Oct 22. Cell Chem Biol. 2020. PMID: 31653597 Free article.
From Screening to Targeted Degradation: Strategies for the Discovery and Optimization of Small Molecule Ligands for PCSK9.
Petrilli WL, Adam GC, Erdmann RS, Abeywickrema P, Agnani V, Ai X, Baysarowich J, Byrne N, Caldwell JP, Chang W, DiNunzio E, Feng Z, Ford R, Ha S, Huang Y, Hubbard B, Johnston JM, Kavana M, Lisnock JM, Liang R, Lu J, Lu Z, Meng J, Orth P, Palyha O, Parthasarathy G, Salowe SP, Sharma S, Shipman J, Soisson SM, Strack A, Youm H, Zhao K, Zink DL, Zokian H, Addona GH, Akinsanya K, Tata JR, Xiong Y, Imbriglio JE. Petrilli WL, et al. Among authors: lisnock jm. Cell Chem Biol. 2021 Feb 18;28(2):243. doi: 10.1016/j.chembiol.2021.01.019. Cell Chem Biol. 2021. PMID: 33607006 Free article. No abstract available.
A new class of prolylcarboxypeptidase inhibitors, part 1: discovery and evaluation.
Graham TH, Liu W, Verras A, Sebhat IK, Xiong Y, Bleasby K, Bhatt UR, Chen Q, Garcia-Calvo M, Geissler WM, Gorski JN, He H, Lassman ME, Lisnock J, Li X, Shen Z, Tong X, Tung EC, Wiltsie J, Xiao J, Xie D, Xu S, Hale JJ, Pinto S, Shen DM. Graham TH, et al. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2811-7. doi: 10.1016/j.bmcl.2012.02.075. Epub 2012 Mar 1. Bioorg Med Chem Lett. 2012. PMID: 22444683
Discovery and optimization of orally active cyclohexane-based prolylcarboxypeptidase (PrCP) inhibitors.
Debenham JS, Graham TH, Verras A, Zhang Y, Clements MJ, Kuethe JT, Madsen-Duggan C, Liu W, Bhatt UR, Chen D, Chen Q, Garcia-Calvo M, Geissler WM, He H, Li X, Lisnock J, Shen Z, Tong X, Tung EC, Wiltsie J, Xu S, Hale JJ, Pinto S, Shen DM. Debenham JS, et al. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6228-33. doi: 10.1016/j.bmcl.2013.09.094. Epub 2013 Oct 8. Bioorg Med Chem Lett. 2013. PMID: 24157366
Discovery of novel non-steroidal reverse indole mineralocorticoid receptor antagonists.
Ogawa AK, Bunte EV, Mal R, Lan P, Sun Z, Crespo A, Wiltsie J, Clemas J, Gibson J, Contino L, Lisnock J, Zhou G, Garcia-Calvo M, Jochnowitz N, Ma X, Pan Y, Brown P, Zamlynny B, Bateman T, Leung D, Xu L, Tong X, Liu K, Crook M, Sinclair P. Ogawa AK, et al. Bioorg Med Chem Lett. 2016 Jun 15;26(12):2866-2869. doi: 10.1016/j.bmcl.2016.04.052. Epub 2016 Apr 20. Bioorg Med Chem Lett. 2016. PMID: 27161805
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.
Yang C, Balsells J, Chu HD, Cox JM, Crespo A, Ma X, Contino L, Brown P, Gao S, Zamlynny B, Wiltsie J, Clemas J, Lisnock J, Gibson J, Zhou G, Garcia-Calvo M, Bateman TJ, Tong V, Xu L, Crook M, Sinclair P, Shen HC. Yang C, et al. Among authors: lisnock j. ACS Med Chem Lett. 2015 Mar 6;6(4):461-5. doi: 10.1021/acsmedchemlett.5b00010. eCollection 2015 Apr 9. ACS Med Chem Lett. 2015. PMID: 25941555 Free PMC article.
Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety.
He S, Hong Q, Lai Z, Yang DX, Ting PC, Kuethe JT, Cernak TA, Dykstra KD, Sperbeck DM, Wu Z, Yu Y, Yang GX, Jian T, Liu J, Guiadeen D, Krikorian AD, Sonatore LM, Wiltsie J, Liu J, Gorski JN, Chung CC, Gibson JT, Lisnock J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ. He S, et al. Among authors: lisnock j. ACS Med Chem Lett. 2014 Sep 8;5(10):1082-7. doi: 10.1021/ml5003426. eCollection 2014 Oct 9. ACS Med Chem Lett. 2014. PMID: 25349648 Free PMC article.
Mineralocorticoid receptor antagonists: identification of heterocyclic amide replacements in the oxazolidinedione series.
Cox JM, Chu HD, Yang C, Shen HC, Wu Z, Balsells J, Crespo A, Brown P, Zamlynny B, Wiltsie J, Clemas J, Gibson J, Contino L, Lisnock J, Zhou G, Garcia-Calvo M, Bateman T, Xu L, Tong X, Crook M, Sinclair P. Cox JM, et al. Among authors: lisnock j. Bioorg Med Chem Lett. 2014 Apr 1;24(7):1681-4. doi: 10.1016/j.bmcl.2014.02.057. Epub 2014 Mar 1. Bioorg Med Chem Lett. 2014. PMID: 24630411
24 results