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Nav1.7 target modulation and efficacy can be measured in nonhuman primate assays.
Kraus RL, Zhao F, Pall PS, Zhou D, Vardigan JD, Danziger A, Li Y, Daley C, Ballard JE, Clements MK, Klein RM, Holahan MA, Greshock TJ, Kim RM, Layton ME, Burgey CS, Serra J, Henze DA, Houghton AK. Kraus RL, et al. Among authors: greshock tj. Sci Transl Med. 2021 May 19;13(594):eaay1050. doi: 10.1126/scitranslmed.aay1050. Sci Transl Med. 2021. PMID: 34011626
Association of respiratory failure with inhibition of NaV1.6 in the phrenic nerve.
Klein RM, Layton ME, Regan H, Regan CP, Li Y, Filzen T, Cato M, Clements MK, Wang J, Sanoja R, Greshock TJ, Roecker AJ, Pero JE, Kim R, Burgey C, John CT, Wang YH, Bhandari N, Struyk A, Kraus RL, Henze DA, Houghton AK. Klein RM, et al. Among authors: greshock tj. Channels (Austin). 2022 Dec;16(1):230-243. doi: 10.1080/19336950.2022.2122309. Channels (Austin). 2022. PMID: 36239534 Free PMC article.
Discovery of Arylsulfonamide Nav1.7 Inhibitors: IVIVC, MPO Methods, and Optimization of Selectivity Profile.
Roecker AJ, Layton ME, Pero JE, Kelly MJ 3rd, Greshock TJ, Kraus RL, Li Y, Klein R, Clements M, Daley C, Jovanovska A, Ballard JE, Wang D, Zhao F, Brunskill APJ, Peng X, Wang X, Sun H, Houghton AK, Burgey CS. Roecker AJ, et al. Among authors: greshock tj. ACS Med Chem Lett. 2021 Jun 1;12(6):1038-1049. doi: 10.1021/acsmedchemlett.1c00218. eCollection 2021 Jun 10. ACS Med Chem Lett. 2021. PMID: 34141090 Free PMC article.
Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group.
Bungard CJ, Williams PD, Ballard JE, Bennett DJ, Beaulieu C, Bahnck-Teets C, Carroll SS, Chang RK, Dubost DC, Fay JF, Diamond TL, Greshock TJ, Hao L, Holloway MK, Felock PJ, Gesell JJ, Su HP, Manikowski JJ, McKay DJ, Miller M, Min X, Molinaro C, Moradei OM, Nantermet PG, Nadeau C, Sanchez RI, Satyanarayana T, Shipe WD, Singh SK, Truong VL, Vijayasaradhi S, Wiscount CM, Vacca JP, Crane SN, McCauley JA. Bungard CJ, et al. Among authors: greshock tj. ACS Med Chem Lett. 2016 May 9;7(7):702-7. doi: 10.1021/acsmedchemlett.6b00135. eCollection 2016 Jul 14. ACS Med Chem Lett. 2016. PMID: 27437081 Free PMC article.
Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity.
Scott JD, DeMong DE, Greshock TJ, Basu K, Dai X, Harris J, Hruza A, Li SW, Lin SI, Liu H, Macala MK, Hu Z, Mei H, Zhang H, Walsh P, Poirier M, Shi ZC, Xiao L, Agnihotri G, Baptista MA, Columbus J, Fell MJ, Hyde LA, Kuvelkar R, Lin Y, Mirescu C, Morrow JA, Yin Z, Zhang X, Zhou X, Chang RK, Embrey MW, Sanders JM, Tiscia HE, Drolet RE, Kern JT, Sur SM, Renger JJ, Bilodeau MT, Kennedy ME, Parker EM, Stamford AW, Nargund R, McCauley JA, Miller MW. Scott JD, et al. Among authors: greshock tj. J Med Chem. 2017 Apr 13;60(7):2983-2992. doi: 10.1021/acs.jmedchem.7b00045. Epub 2017 Mar 16. J Med Chem. 2017. PMID: 28245354
Potent, selective and orally bioavailable leucine-rich repeat kinase 2 (LRRK2) inhibitors.
Greshock TJ, Sanders JM, Drolet RE, Rajapakse HA, Chang RK, Kim B, Rada VL, Tiscia HE, Su H, Lai MT, Sur SM, Sanchez RI, Bilodeau MT, Renger JJ, Kern JT, McCauley JA. Greshock TJ, et al. Bioorg Med Chem Lett. 2016 Jun 1;26(11):2631-5. doi: 10.1016/j.bmcl.2016.04.021. Epub 2016 Apr 9. Bioorg Med Chem Lett. 2016. PMID: 27106707
MK-7622: A First-in-Class M1 Positive Allosteric Modulator Development Candidate.
Beshore DC, N Di Marco C, Chang RK, Greshock TJ, Ma L, Wittmann M, Seager MA, Koeplinger KA, Thompson CD, Fuerst J, Hartman GD, Bilodeau MT, Ray WJ, Kuduk SD. Beshore DC, et al. Among authors: greshock tj. ACS Med Chem Lett. 2018 Apr 30;9(7):652-656. doi: 10.1021/acsmedchemlett.8b00095. eCollection 2018 Jul 12. ACS Med Chem Lett. 2018. PMID: 30034595 Free PMC article.
35 results