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One health therapeutics: Target-Based drug development for cryptosporidiosis and other apicomplexa diseases.
Van Voorhis WC, Hulverson MA, Choi R, Huang W, Arnold SLM, Schaefer DA, Betzer DP, Vidadala RSR, Lee S, Whitman GR, Barrett LK, Maly DJ, Riggs MW, Fan E, Kennedy TJ, Tzipori S, Doggett JS, Winzer P, Anghel N, Imhof D, Müller J, Hemphill A, Ferre I, Sanchez-Sanchez R, Ortega-Mora LM, Ojo KK. Van Voorhis WC, et al. Among authors: huang w. Vet Parasitol. 2021 Jan;289:109336. doi: 10.1016/j.vetpar.2020.109336. Epub 2020 Dec 15. Vet Parasitol. 2021. PMID: 33418437 Free PMC article. Review.
Potent and selective inhibitors of CDPK1 from T. gondii and C. parvum based on a 5-aminopyrazole-4-carboxamide scaffold.
Zhang Z, Ojo KK, Vidadala R, Huang W, Geiger JA, Scheele S, Choi R, Reid MC, Keyloun KR, Rivas K, Siddaramaiah LK, Comess KM, Robinson KP, Merta PJ, Kifle L, Hol WG, Parsons M, Merritt EA, Maly DJ, Verlinde CL, Van Voorhis WC, Fan E. Zhang Z, et al. Among authors: huang w. ACS Med Chem Lett. 2014 Jan 9;5(1):40-44. doi: 10.1021/ml400315s. ACS Med Chem Lett. 2014. PMID: 24494061 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. 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.
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. Among authors: huang w. 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.
5-Fluoroimidazo[4,5-b]pyridine Is a Privileged Fragment That Conveys Bioavailability to Potent Trypanosomal Methionyl-tRNA Synthetase Inhibitors.
Zhang Z, Koh CY, Ranade RM, Shibata S, Gillespie JR, Hulverson MA, Huang W, Nguyen J, Pendem N, Gelb MH, Verlinde CL, Hol WG, Buckner FS, Fan E. Zhang Z, et al. Among authors: huang w. ACS Infect Dis. 2016 Jun 10;2(6):399-404. doi: 10.1021/acsinfecdis.6b00036. Epub 2016 Apr 11. ACS Infect Dis. 2016. PMID: 27627628 Free PMC article.
A Novel Calcium-Dependent Kinase Inhibitor, Bumped Kinase Inhibitor 1517, Cures Cryptosporidiosis in Immunosuppressed Mice.
Castellanos-Gonzalez A, Sparks H, Nava S, Huang W, Zhang Z, Rivas K, Hulverson MA, Barrett LK, Ojo KK, Fan E, Van Voorhis WC, White AC Jr. Castellanos-Gonzalez A, et al. Among authors: huang w. J Infect Dis. 2016 Dec 15;214(12):1850-1855. doi: 10.1093/infdis/jiw481. Epub 2016 Oct 12. J Infect Dis. 2016. PMID: 27738055 Free PMC article.
5-Aminopyrazole-4-carboxamide analogues are selective inhibitors of Plasmodium falciparum microgametocyte exflagellation and potential malaria transmission blocking agents.
Huang W, Hulverson MA, Zhang Z, Choi R, Hart KJ, Kennedy M, Vidadala RSR, Maly DJ, Van Voorhis WC, Lindner SE, Fan E, Ojo KK. Huang W, et al. Bioorg Med Chem Lett. 2016 Nov 15;26(22):5487-5491. doi: 10.1016/j.bmcl.2016.10.014. Epub 2016 Oct 10. Bioorg Med Chem Lett. 2016. PMID: 27780638 Free PMC article.
Novel Bumped Kinase Inhibitors Are Safe and Effective Therapeutics in the Calf Clinical Model for Cryptosporidiosis.
Schaefer DA, Betzer DP, Smith KD, Millman ZG, Michalski HC, Menchaca SE, Zambriski JA, Ojo KK, Hulverson MA, Arnold SL, Rivas KL, Vidadala RS, Huang W, Barrett LK, Maly DJ, Fan E, Van Voorhis WC, Riggs MW. Schaefer DA, et al. Among authors: huang w. J Infect Dis. 2016 Dec 15;214(12):1856-1864. doi: 10.1093/infdis/jiw488. Epub 2016 Oct 17. J Infect Dis. 2016. PMID: 27923949 Free PMC article.
5-Aminopyrazole-4-Carboxamide-Based Compounds Prevent the Growth of Cryptosporidium parvum.
Huang W, Choi R, Hulverson MA, Zhang Z, McCloskey MC, Schaefer DA, Whitman GR, Barrett LK, Vidadala RSR, Riggs MW, Maly DJ, Van Voorhis WC, Ojo KK, Fan E. Huang W, et al. Antimicrob Agents Chemother. 2017 Jul 25;61(8):e00020-17. doi: 10.1128/AAC.00020-17. Print 2017 Aug. Antimicrob Agents Chemother. 2017. PMID: 28533246 Free PMC article.
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