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The PET tracer [11C]MK-6884 quantifies M4 muscarinic receptor in rhesus monkeys and patients with Alzheimer's disease.
Li W, Wang Y, Lohith TG, Zeng Z, Tong L, Mazzola R, Riffel K, Miller P, Purcell M, Holahan M, Haley H, Gantert L, Hesk D, Ren S, Morrow J, Uslaner J, Struyk A, Wai JM, Rudd MT, Tellers DM, McAvoy T, Bormans G, Koole M, Van Laere K, Serdons K, de Hoon J, Declercq R, De Lepeleire I, Pascual MB, Zanotti-Fregonara P, Yu M, Arbones V, Masdeu JC, Cheng A, Hussain A, Bueters T, Anderson MS, Hostetler ED, Basile AS. Li W, et al. Among authors: mazzola r. Sci Transl Med. 2022 Jan 12;14(627):eabg3684. doi: 10.1126/scitranslmed.abg3684. Epub 2022 Jan 12. Sci Transl Med. 2022. PMID: 35020407
Discovery of [11C]MK-6884: A Positron Emission Tomography (PET) Imaging Agent for the Study of M4Muscarinic Receptor Positive Allosteric Modulators (PAMs) in Neurodegenerative Diseases.
Tong L, Li W, Lo MM, Gao X, Wai JM, Rudd M, Tellers D, Joshi A, Zeng Z, Miller P, Salinas C, Riffel K, Haley H, Purcell M, Holahan M, Gantert L, Schubert JW, Jones K, Mulhearn J, Egbertson M, Meng Z, Hanney B, Gomez R, Harrison ST, McQuade P, Bueters T, Uslaner J, Morrow J, Thomson F, Kong J, Liao J, Selyutin O, Bao J, Hastings NB, Agrawal S, Magliaro BC, Monsma FJ Jr, Smith MD, Risso S, Hesk D, Hostetler E, Mazzola R. Tong L, et al. Among authors: mazzola r. J Med Chem. 2020 Mar 12;63(5):2411-2425. doi: 10.1021/acs.jmedchem.9b01406. Epub 2020 Mar 3. J Med Chem. 2020. PMID: 32101422 Free article.
Antinociceptive effects of potent, selective and brain penetrant muscarinic M4 positive allosteric modulators in rodent pain models.
Grauer SM, Sanoja R, Poulin D, Rashid H, Jochnowitz N, Calhoun M, Zwilling D, Varty GB, Rosahl TW, Meziane H, Mittlelhaeuser C, Mazzola R, Morrow J, Smith SM, Henze D, Marcus J. Grauer SM, et al. Among authors: mazzola r. Brain Res. 2020 Jun 15;1737:146814. doi: 10.1016/j.brainres.2020.146814. Epub 2020 Mar 29. Brain Res. 2020. PMID: 32234514
MK-8325: A silyl proline-containing NS5A inhibitor with pan-genotype activity for treatment of HCV.
Nair AG, Zeng Q, Selyutin O, Rosenblum SB, Jiang Y, Yang DY, Keertikar K, Zhou G, Dwyer M, Kim SH, Shankar B, Yu W, Tong L, Chen L, Mazzola R, Caldwell J, Tang H, Agrawal S, Liu R, Kong R, Ingravallo P, Xia E, Zhai Y, Nomeir A, Asante-Appiah E, Kozlowski JA. Nair AG, et al. Among authors: mazzola r. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1954-1957. doi: 10.1016/j.bmcl.2018.03.049. Epub 2018 Mar 20. Bioorg Med Chem Lett. 2018. PMID: 29653894
Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development.
Nair AG, Zeng Q, Selyutin O, Rosenblum SB, Jiang Y, Yang DY, Keertikar K, Zhou G, Dwyer MP, Kim SH, Shankar B, Yu W, Tong L, Chen L, Mazzola R, Caldwell J, Tang H, Allard ML, Buckle RN, Gauuan PJ, Holst CL, Martin GS, Naicker KP, Vellekoop S, Agrawal S, Liu R, Kong R, Ingravallo P, Xia E, Zhai Y, Nomeir A, Kozlowski JA. Nair AG, et al. Among authors: mazzola r. Bioorg Med Chem Lett. 2016 Mar 1;26(5):1475-9. doi: 10.1016/j.bmcl.2016.01.050. Epub 2016 Jan 19. Bioorg Med Chem Lett. 2016. PMID: 26850003
Substituted tetracyclic indole core derivatives of HCV NS5A inhibitor MK-8742.
Yu W, Zhou G, Coburn CA, Zeng Q, Tong L, Dwyer MP, Hu B, Zhong B, Hao J, Ji T, Zan S, Chen L, Mazzola R, Kim JH, Sha D, Selyutin O, Rosenblum SB, Lavey B, Nair AG, Heon Kim S, Keertikar KM, Rokosz L, Agrawal S, Liu R, Xia E, Zhai Y, Curry S, McMonagle P, Ingravallo P, Asante-Appiah E, Chen S, Kozlowski JA. Yu W, et al. Among authors: mazzola r. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4851-4856. doi: 10.1016/j.bmcl.2016.08.002. Epub 2016 Aug 2. Bioorg Med Chem Lett. 2016. PMID: 27568086
The selective phosphodiesterase 9 (PDE9) inhibitor PF-04447943 (6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one) enhances synaptic plasticity and cognitive function in rodents.
Hutson PH, Finger EN, Magliaro BC, Smith SM, Converso A, Sanderson PE, Mullins D, Hyde LA, Eschle BK, Turnbull Z, Sloan H, Guzzi M, Zhang X, Wang A, Rindgen D, Mazzola R, Vivian JA, Eddins D, Uslaner JM, Bednar R, Gambone C, Le-Mair W, Marino MJ, Sachs N, Xu G, Parmentier-Batteur S. Hutson PH, et al. Among authors: mazzola r. Neuropharmacology. 2011 Sep;61(4):665-76. doi: 10.1016/j.neuropharm.2011.05.009. Epub 2011 May 19. Neuropharmacology. 2011. PMID: 21619887
Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms.
Tong L, Yu W, Chen L, Selyutin O, Dwyer MP, Nair AG, Mazzola R, Kim JH, Sha D, Yin J, Ruck RT, Davies IW, Hu B, Zhong B, Hao J, Ji T, Zan S, Liu R, Agrawal S, Xia E, Curry S, McMonagle P, Bystol K, Lahser F, Carr D, Rokosz L, Ingravallo P, Chen S, Feng KI, Cartwright M, Asante-Appiah E, Kozlowski JA. Tong L, et al. Among authors: mazzola r. J Med Chem. 2017 Jan 12;60(1):290-306. doi: 10.1021/acs.jmedchem.6b01310. Epub 2016 Nov 15. J Med Chem. 2017. PMID: 27808515 Free article.
Structure and activity relationships of tartrate-based TACE inhibitors.
Li D, Popovici-Muller J, Belanger DB, Caldwell J, Dai C, David M, Girijavallabhan VM, Lavey BJ, Lee JF, Liu Z, Mazzola R, Rizvi R, Rosner KE, Shankar B, Spitler J, Ting PC, Vaccaro H, Yu W, Zhou G, Zhu Z, Niu X, Sun J, Guo Z, Orth P, Chen S, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Shipps GW Jr, Siddiqui MA, Strickland CO. Li D, et al. Among authors: mazzola r. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4812-5. doi: 10.1016/j.bmcl.2010.06.104. Epub 2010 Jun 25. Bioorg Med Chem Lett. 2010. PMID: 20638281
Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket.
Mazzola RD Jr, Zhu Z, Sinning L, McKittrick B, Lavey B, Spitler J, Kozlowski J, Neng-Yang S, Zhou G, Guo Z, Orth P, Madison V, Sun J, Lundell D, Niu X. Mazzola RD Jr, et al. Bioorg Med Chem Lett. 2008 Nov 1;18(21):5809-14. doi: 10.1016/j.bmcl.2008.09.045. Epub 2008 Sep 13. Bioorg Med Chem Lett. 2008. PMID: 18835710
285 results