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Discovery of 6-(Fluoro-(18)F)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine ([(18)F]-MK-6240): A Positron Emission Tomography (PET) Imaging Agent for Quantification of Neurofibrillary Tangles (NFTs).
Walji AM, Hostetler ED, Selnick H, Zeng Z, Miller P, Bennacef I, Salinas C, Connolly B, Gantert L, Holahan M, O'Malley S, Purcell M, Riffel K, Li J, Balsells J, OBrien JA, Melquist S, Soriano A, Zhang X, Ogawa A, Xu S, Joshi E, Della Rocca J, Hess FJ, Schachter J, Hesk D, Schenk D, Struyk A, Babaoglu K, Lohith TG, Wang Y, Yang K, Fu J, Evelhoch JL, Coleman PJ. Walji AM, et al. Among authors: hesk d. J Med Chem. 2016 May 26;59(10):4778-89. doi: 10.1021/acs.jmedchem.6b00166. Epub 2016 May 5. J Med Chem. 2016. PMID: 27088900
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: hesk d. 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.
Preclinical Characterization of 18F-MK-6240, a Promising PET Tracer for In Vivo Quantification of Human Neurofibrillary Tangles.
Hostetler ED, Walji AM, Zeng Z, Miller P, Bennacef I, Salinas C, Connolly B, Gantert L, Haley H, Holahan M, Purcell M, Riffel K, Lohith TG, Coleman P, Soriano A, Ogawa A, Xu S, Zhang X, Joshi E, Della Rocca J, Hesk D, Schenk DJ, Evelhoch JL. Hostetler ED, et al. Among authors: hesk d. J Nucl Med. 2016 Oct;57(10):1599-1606. doi: 10.2967/jnumed.115.171678. Epub 2016 May 26. J Nucl Med. 2016. PMID: 27230925 Free article.
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: hesk d. Sci Transl Med. 2022 Jan 12;14(627):eabg3684. doi: 10.1126/scitranslmed.abg3684. Epub 2022 Jan 12. Sci Transl Med. 2022. PMID: 35020407
Metallaphotoredox aryl and alkyl radiomethylation for PET ligand discovery.
Pipal RW, Stout KT, Musacchio PZ, Ren S, Graham TJA, Verhoog S, Gantert L, Lohith TG, Schmitz A, Lee HS, Hesk D, Hostetler ED, Davies IW, MacMillan DWC. Pipal RW, et al. Among authors: hesk d. Nature. 2021 Jan;589(7843):542-547. doi: 10.1038/s41586-020-3015-0. Epub 2020 Nov 25. Nature. 2021. PMID: 33238289 Free PMC article.
MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.
Boga SB, Deng Y, Zhu L, Nan Y, Cooper AB, Shipps GW Jr, Doll R, Shih NY, Zhu H, Sun R, Wang T, Paliwal S, Tsui HC, Gao X, Yao X, Desai J, Wang J, Alhassan AB, Kelly J, Patel M, Muppalla K, Gudipati S, Zhang LK, Buevich A, Hesk D, Carr D, Dayananth P, Black S, Mei H, Cox K, Sherborne B, Hruza AW, Xiao L, Jin W, Long B, Liu G, Taylor SA, Kirschmeier P, Windsor WT, Bishop R, Samatar AA. Boga SB, et al. Among authors: hesk d. ACS Med Chem Lett. 2018 Jun 14;9(7):761-767. doi: 10.1021/acsmedchemlett.8b00220. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034615 Free PMC article.
Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology.
Boga SB, Alhassan AB, Cooper AB, Doll R, Shih NY, Shipps G, Deng Y, Zhu H, Nan Y, Sun R, Zhu L, Desai J, Patel M, Muppalla K, Gao X, Wang J, Yao X, Kelly J, Gudipati S, Paliwal S, Tsui HC, Wang T, Sherborne B, Xiao L, Hruza A, Buevich A, Zhang LK, Hesk D, Samatar AA, Carr D, Long B, Black S, Dayananth P, Windsor W, Kirschmeier P, Bishop R. Boga SB, et al. Among authors: hesk d. Bioorg Med Chem Lett. 2018 Jun 15;28(11):2029-2034. doi: 10.1016/j.bmcl.2018.04.063. Epub 2018 Apr 26. Bioorg Med Chem Lett. 2018. PMID: 29748051
54 results