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Page 1
Bumped Kinase Inhibitors as therapy for apicomplexan parasitic diseases: lessons learned.
Choi R, Hulverson MA, Huang W, Vidadala RSR, Whitman GR, Barrett LK, Schaefer DA, Betzer DP, Riggs MW, Doggett JS, Hemphill A, Ortega-Mora LM, McCloskey MC, Arnold SLM, Hackman RC, Marsh KC, Lynch JJ, Freiberg GM, Leroy BE, Kempf DJ, Choy RKM, de Hostos EL, Maly DJ, Fan E, Ojo KK, Van Voorhis WC. Choi R, et al. Among authors: freiberg gm. Int J Parasitol. 2020 May;50(5):413-422. doi: 10.1016/j.ijpara.2020.01.006. Epub 2020 Mar 26. Int J Parasitol. 2020. PMID: 32224121 Free PMC article. Review.
Development of an Orally Available and Central Nervous System (CNS) Penetrant Toxoplasma gondii Calcium-Dependent Protein Kinase 1 (TgCDPK1) Inhibitor with Minimal Human Ether-a-go-go-Related Gene (hERG) Activity for the Treatment of Toxoplasmosis.
Vidadala RS, Rivas KL, Ojo KK, Hulverson MA, Zambriski JA, Bruzual I, Schultz TL, Huang W, Zhang Z, Scheele S, DeRocher AE, Choi R, Barrett LK, Siddaramaiah LK, Hol WG, Fan E, Merritt EA, Parsons M, Freiberg G, Marsh K, Kempf DJ, Carruthers VB, Isoherranen N, Doggett JS, Van Voorhis WC, Maly DJ. Vidadala RS, et al. J Med Chem. 2016 Jul 14;59(13):6531-46. doi: 10.1021/acs.jmedchem.6b00760. Epub 2016 Jul 1. J Med Chem. 2016. PMID: 27309760 Free PMC article.
Advances in bumped kinase inhibitors for human and animal therapy for cryptosporidiosis.
Hulverson MA, Choi R, Arnold SLM, Schaefer DA, Hemphill A, McCloskey MC, Betzer DP, Müller J, Vidadala RSR, Whitman GR, Rivas KL, Barrett LK, Hackman RC, Love MS, McNamara CW, Shaughnessy TK, Kondratiuk A, Kurnick M, Banfor PN, Lynch JJ, Freiberg GM, Kempf DJ, Maly DJ, Riggs MW, Ojo KK, Van Voorhis WC. Hulverson MA, et al. Among authors: freiberg gm. Int J Parasitol. 2017 Oct;47(12):753-763. doi: 10.1016/j.ijpara.2017.08.006. Epub 2017 Sep 9. Int J Parasitol. 2017. PMID: 28899690 Free PMC article.
SAR Studies of 5-Aminopyrazole-4-carboxamide Analogues as Potent and Selective Inhibitors of Toxoplasma gondii CDPK1.
Huang W, Ojo KK, Zhang Z, Rivas K, Vidadala RS, Scheele S, DeRocher AE, Choi R, Hulverson MA, Barrett LK, Bruzual I, Siddaramaiah LK, Kerchner KM, Kurnick MD, Freiberg GM, Kempf D, Hol WG, Merritt EA, Neckermann G, de Hostos EL, Isoherranen N, Maly DJ, Parsons M, Doggett JS, Van Voorhis WC, Fan E. Huang W, et al. Among authors: freiberg gm. ACS Med Chem Lett. 2015 Oct 22;6(12):1184-1189. doi: 10.1021/acsmedchemlett.5b00319. eCollection 2015 Dec 10. ACS Med Chem Lett. 2015. PMID: 26693272 Free PMC article.
Essential but Not Vulnerable: Indazole Sulfonamides Targeting Inosine Monophosphate Dehydrogenase as Potential Leads against Mycobacterium tuberculosis.
Park Y, Pacitto A, Bayliss T, Cleghorn LA, Wang Z, Hartman T, Arora K, Ioerger TR, Sacchettini J, Rizzi M, Donini S, Blundell TL, Ascher DB, Rhee K, Breda A, Zhou N, Dartois V, Jonnala SR, Via LE, Mizrahi V, Epemolu O, Stojanovski L, Simeons F, Osuna-Cabello M, Ellis L, MacKenzie CJ, Smith AR, Davis SH, Murugesan D, Buchanan KI, Turner PA, Huggett M, Zuccotto F, Rebollo-Lopez MJ, Lafuente-Monasterio MJ, Sanz O, Diaz GS, Lelièvre J, Ballell L, Selenski C, Axtman M, Ghidelli-Disse S, Pflaumer H, Bösche M, Drewes G, Freiberg GM, Kurnick MD, Srikumaran M, Kempf DJ, Green SR, Ray PC, Read K, Wyatt P, Barry CE 3rd, Boshoff HI. Park Y, et al. Among authors: freiberg gm. ACS Infect Dis. 2017 Jan 13;3(1):18-33. doi: 10.1021/acsinfecdis.6b00103. Epub 2016 Oct 17. ACS Infect Dis. 2017. PMID: 27704782 Free PMC article.
Spirocycle MmpL3 Inhibitors with Improved hERG and Cytotoxicity Profiles as Inhibitors of Mycobacterium tuberculosis Growth.
Ray PC, Huggett M, Turner PA, Taylor M, Cleghorn LAT, Early J, Kumar A, Bonnett SA, Flint L, Joerss D, Johnson J, Korkegian A, Mullen S, Moure AL, Davis SH, Murugesan D, Mathieson M, Caldwell N, Engelhart CA, Schnappinger D, Epemolu O, Zuccotto F, Riley J, Scullion P, Stojanovski L, Massoudi L, Robertson GT, Lenaerts AJ, Freiberg G, Kempf DJ, Masquelin T, Hipskind PA, Odingo J, Read KD, Green SR, Wyatt PG, Parish T. Ray PC, et al. ACS Omega. 2021 Jan 13;6(3):2284-2311. doi: 10.1021/acsomega.0c05589. eCollection 2021 Jan 26. ACS Omega. 2021. PMID: 33521468 Free PMC article.
Identification of Selective Dual ROCK1 and ROCK2 Inhibitors Using Structure-Based Drug Design.
Hobson AD, Judge RA, Aguirre AL, Brown BS, Cui Y, Ding P, Dominguez E, DiGiammarino E, Egan DA, Freiberg GM, Gopalakrishnan SM, Harris CM, Honore MP, Kage KL, Kapecki NJ, Ling C, Ma J, Mack H, Mamo M, Maurus S, McRae B, Moore NS, Mueller BK, Mueller R, Namovic MT, Patel K, Pratt SD, Putman CB, Queeney KL, Sarris KK, Schaffter LM, Stoll V, Vasudevan A, Wang L, Wang L, Wirthl W, Yach K. Hobson AD, et al. Among authors: freiberg gm. J Med Chem. 2018 Dec 27;61(24):11074-11100. doi: 10.1021/acs.jmedchem.8b01098. Epub 2018 Dec 12. J Med Chem. 2018. PMID: 30384606
Antimalarial Inhibitors Targeting Serine Hydroxymethyltransferase (SHMT) with in Vivo Efficacy and Analysis of their Binding Mode Based on X-ray Cocrystal Structures.
Schwertz G, Witschel MC, Rottmann M, Bonnert R, Leartsakulpanich U, Chitnumsub P, Jaruwat A, Ittarat W, Schäfer A, Aponte RA, Charman SA, White KL, Kundu A, Sadhukhan S, Lloyd M, Freiberg GM, Srikumaran M, Siggel M, Zwyssig A, Chaiyen P, Diederich F. Schwertz G, et al. Among authors: freiberg gm. J Med Chem. 2017 Jun 22;60(12):4840-4860. doi: 10.1021/acs.jmedchem.7b00008. Epub 2017 Jun 13. J Med Chem. 2017. PMID: 28537728
14 results