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USP7 inhibits Wnt/β-catenin signaling through promoting stabilization of Axin.
Ji L, Lu B, Zamponi R, Charlat O, Aversa R, Yang Z, Sigoillot F, Zhu X, Hu T, Reece-Hoyes JS, Russ C, Michaud G, Tchorz JS, Jiang X, Cong F. Ji L, et al. Among authors: aversa r. Nat Commun. 2019 Sep 13;10(1):4184. doi: 10.1038/s41467-019-12143-3. Nat Commun. 2019. PMID: 31519875 Free PMC article.
Design and Discovery of N-(2-Methyl-5'-morpholino-6'-((tetrahydro-2H-pyran-4-yl)oxy)-[3,3'-bipyridin]-5-yl)-3-(trifluoromethyl)benzamide (RAF709): A Potent, Selective, and Efficacious RAF Inhibitor Targeting RAS Mutant Cancers.
Nishiguchi GA, Rico A, Tanner H, Aversa RJ, Taft BR, Subramanian S, Setti L, Burger MT, Wan L, Tamez V, Smith A, Lou Y, Barsanti PA, Appleton BA, Mamo M, Tandeske L, Dix I, Tellew JE, Huang S, Mathews Griner LA, Cooke VG, Van Abbema A, Merritt H, Ma S, Gampa K, Feng F, Yuan J, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Jansen JM, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Lees E, Shao W, Stuart DD, Dillon MP, Ramurthy S. Nishiguchi GA, et al. Among authors: aversa rj. J Med Chem. 2017 Jun 22;60(12):4869-4881. doi: 10.1021/acs.jmedchem.6b01862. Epub 2017 Jun 8. J Med Chem. 2017. PMID: 28557458
Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF.
Shao W, Mishina YM, Feng Y, Caponigro G, Cooke VG, Rivera S, Wang Y, Shen F, Korn JM, Mathews Griner LA, Nishiguchi G, Rico A, Tellew J, Haling JR, Aversa R, Polyakov V, Zang R, Hekmat-Nejad M, Amiri P, Singh M, Keen N, Dillon MP, Lees E, Ramurthy S, Sellers WR, Stuart DD. Shao W, et al. Among authors: aversa r. Cancer Res. 2018 Mar 15;78(6):1537-1548. doi: 10.1158/0008-5472.CAN-17-2033. Epub 2018 Jan 17. Cancer Res. 2018. PMID: 29343524
Design and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic.
Ramurthy S, Taft BR, Aversa RJ, Barsanti PA, Burger MT, Lou Y, Nishiguchi GA, Rico A, Setti L, Smith A, Subramanian S, Tamez V, Tanner H, Wan L, Hu C, Appleton BA, Mamo M, Tandeske L, Tellew JE, Huang S, Yue Q, Chaudhary A, Tian H, Iyer R, Hassan AQ, Mathews Griner LA, La Bonte LR, Cooke VG, Van Abbema A, Merritt H, Gampa K, Feng F, Yuan J, Mishina Y, Wang Y, Haling JR, Vaziri S, Hekmat-Nejad M, Polyakov V, Zang R, Sethuraman V, Amiri P, Singh M, Sellers WR, Lees E, Shao W, Dillon MP, Stuart DD. Ramurthy S, et al. Among authors: aversa rj. J Med Chem. 2020 Mar 12;63(5):2013-2027. doi: 10.1021/acs.jmedchem.9b00161. Epub 2019 May 16. J Med Chem. 2020. PMID: 31059256
Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling, downstream of activated RAS, and the poor overall kinase selectivity of putative RAF inhibitors. Herein, we describe 15 (LXH …
Direct pharmacological inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of …
Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.
Barsanti PA, Pan Y, Lu Y, Jain R, Cox M, Aversa RJ, Dillon MP, Elling R, Hu C, Jin X, Knapp M, Lan J, Ramurthy S, Rudewicz P, Setti L, Subramanian S, Mathur M, Taricani L, Thomas G, Xiao L, Yue Q. Barsanti PA, et al. Among authors: aversa rj. ACS Med Chem Lett. 2014 Oct 30;6(1):42-6. doi: 10.1021/ml500352s. eCollection 2015 Jan 8. ACS Med Chem Lett. 2014. PMID: 25589928 Free PMC article.
Maitotoxin: An Inspiration for Synthesis.
Nicolaou KC, Aversa RJ. Nicolaou KC, et al. Isr J Chem. 2011 Apr;51(3-4):359-377. doi: 10.1002/ijch.201100003. Isr J Chem. 2011. PMID: 21709816 Free PMC article.
Chemical Synthesis of the GHIJKLMNO Ring System of Maitotoxin.
Nicolaou KC, Frederick MO, Burtoloso AC, Denton RM, Rivas F, Cole KP, Aversa RJ, Gibe R, Umezawa T, Suzuki T. Nicolaou KC, et al. Among authors: aversa rj. J Am Chem Soc. 2008 Jun 11;130(23):7466-76. doi: 10.1021/ja801139f. Epub 2008 May 16. J Am Chem Soc. 2008. PMID: 18481856
Synthesis of the ABCDEFG ring system of maitotoxin.
Nicolaou KC, Aversa RJ, Jin J, Rivas F. Nicolaou KC, et al. J Am Chem Soc. 2010 May 19;132(19):6855-61. doi: 10.1021/ja102260q. J Am Chem Soc. 2010. PMID: 20415445 Free PMC article.
Synthesis of the C'D'E'F' domain of maitotoxin.
Nicolaou KC, Seo JH, Nakamura T, Aversa RJ. Nicolaou KC, et al. J Am Chem Soc. 2011 Jan 19;133(2):214-9. doi: 10.1021/ja109531d. Epub 2010 Dec 17. J Am Chem Soc. 2011. PMID: 21166429 Free PMC article.
48 results