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Cyanotriazoles are selective topoisomerase II poisons that rapidly cure trypanosome infections.
Rao SPS, Gould MK, Noeske J, Saldivia M, Jumani RS, Ng PS, René O, Chen YL, Kaiser M, Ritchie R, Francisco AF, Johnson N, Patra D, Cheung H, Deniston C, Schenk AD, Cortopassi WA, Schmidt RS, Wiedemar N, Thomas B, Palkar R, Ghafar NA, Manoharan V, Luu C, Gable JE, Wan KF, Myburgh E, Mottram JC, Barnes W, Walker J, Wartchow C, Aziz N, Osborne C, Wagner J, Sarko C, Kelly JM, Manjunatha UH, Mäser P, Jiricek J, Lakshminarayana SB, Barrett MP, Diagana TT. Rao SPS, et al. Among authors: sarko c. Science. 2023 Jun 30;380(6652):1349-1356. doi: 10.1126/science.adh0614. Epub 2023 Jun 29. Science. 2023. PMID: 37384702 Free article.
Discovery of Novel Quinoline-Based Proteasome Inhibitors for Human African Trypanosomiasis (HAT).
Koester DC, Marx VM, Williams S, Jiricek J, Dauphinais M, René O, Miller SL, Zhang L, Patra D, Chen YL, Cheung H, Gable J, Lakshminarayana SB, Osborne C, Galarneau JR, Kulkarni U, Richmond W, Bretz A, Xiao L, Supek F, Wiesmann C, Honnappa S, Be C, Mäser P, Kaiser M, Ritchie R, Barrett MP, Diagana TT, Sarko C, Rao SPS. Koester DC, et al. Among authors: sarko c. J Med Chem. 2022 Sep 8;65(17):11776-11787. doi: 10.1021/acs.jmedchem.2c00791. Epub 2022 Aug 22. J Med Chem. 2022. PMID: 35993839 Free PMC article.
NITD-688, a pan-serotype inhibitor of the dengue virus NS4B protein, shows favorable pharmacokinetics and efficacy in preclinical animal models.
Moquin SA, Simon O, Karuna R, Lakshminarayana SB, Yokokawa F, Wang F, Saravanan C, Zhang J, Day CW, Chan K, Wang QY, Lu S, Dong H, Wan KF, Lim SP, Liu W, Seh CC, Chen YL, Xu H, Barkan DT, Kounde CS, Sim WLS, Wang G, Yeo HQ, Zou B, Chan WL, Ding M, Song JG, Li M, Osborne C, Blasco F, Sarko C, Beer D, Bonamy GMC, Sasseville VG, Shi PY, Diagana TT, Yeung BKS, Gu F. Moquin SA, et al. Among authors: sarko c. Sci Transl Med. 2021 Feb 3;13(579):eabb2181. doi: 10.1126/scitranslmed.abb2181. Sci Transl Med. 2021. PMID: 33536278
Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria.
Taft BR, Yokokawa F, Kirrane T, Mata AC, Huang R, Blaquiere N, Waldron G, Zou B, Simon O, Vankadara S, Chan WL, Ding M, Sim S, Straimer J, Guiguemde A, Lakshminarayana SB, Jain JP, Bodenreider C, Thompson C, Lanshoeft C, Shu W, Fang E, Qumber J, Chan K, Pei L, Chen YL, Schulz H, Lim J, Abas SN, Ang X, Liu Y, Angulo-Barturen I, Jiménez-Díaz MB, Gamo FJ, Crespo-Fernandez B, Rosenthal PJ, Cooper RA, Tumwebaze P, Aguiar ACC, Campo B, Campbell S, Wagner J, Diagana TT, Sarko C. Taft BR, et al. Among authors: sarko c. J Med Chem. 2022 Mar 10;65(5):3798-3813. doi: 10.1021/acs.jmedchem.1c01995. Epub 2022 Mar 1. J Med Chem. 2022. PMID: 35229610 Free PMC article.
The Novel, Clinical-Stage Soluble Guanylate Cyclase Activator BI 685509 Protects from Disease Progression in Models of Renal Injury and Disease.
Reinhart GA, Harrison PC, Lincoln K, Chen H, Sun P, Hill J, Qian HS, McHugh MC, Clifford H, Ng KJ, Wang H, Fowler D, Gueneva-Boucheva K, Brenneman JB, Bosanac T, Wong D, Fryer RM, Sarko C, Boustany-Kari CM, Pullen SS. Reinhart GA, et al. Among authors: sarko c. J Pharmacol Exp Ther. 2023 Mar;384(3):382-392. doi: 10.1124/jpet.122.001423. Epub 2022 Dec 6. J Pharmacol Exp Ther. 2023. PMID: 36507845
In vivo selective inhibition of TRPC6 by antagonist BI 749327 ameliorates fibrosis and dysfunction in cardiac and renal disease.
Lin BL, Matera D, Doerner JF, Zheng N, Del Camino D, Mishra S, Bian H, Zeveleva S, Zhen X, Blair NT, Chong JA, Hessler DP, Bedja D, Zhu G, Muller GK, Ranek MJ, Pantages L, McFarland M, Netherton MR, Berry A, Wong D, Rast G, Qian HS, Weldon SM, Kuo JJ, Sauer A, Sarko C, Moran MM, Kass DA, Pullen SS. Lin BL, et al. Among authors: sarko c. Proc Natl Acad Sci U S A. 2019 May 14;116(20):10156-10161. doi: 10.1073/pnas.1815354116. Epub 2019 Apr 26. Proc Natl Acad Sci U S A. 2019. PMID: 31028142 Free PMC article.
Discovery and optimization of pyrazole amides as antagonists of CCR1.
Harcken C, Sarko C, Mao C, Lord J, Raudenbush B, Razavi H, Liu P, Swinamer A, Disalvo D, Lee T, Lin S, Kukulka A, Grbic H, Patel M, Patel M, Fletcher K, Joseph D, White D, Amodeo L, Berg K, Brown M, Thomson DS. Harcken C, et al. Among authors: sarko c. Bioorg Med Chem Lett. 2019 Feb 1;29(3):435-440. doi: 10.1016/j.bmcl.2018.11.015. Epub 2018 Nov 9. Bioorg Med Chem Lett. 2019. PMID: 30455146
Abstracts from the 8th International Conference on cGMP Generators, Effectors and Therapeutic Implications : Bamberg, Germany. 23-25 June, 2017.
Todd Milne G; on behalf of the Ironwood team; Sandner P, Lincoln KA, Harrison PC, Chen H, Wang H, Clifford H, Qian HS, Wong D, Sarko C, Fryer R, Richman J, Reinhart GA, Boustany CM, Pullen SS, Andresen H, Moltzau LR, Cataliotti A, Levy FO, Lukowski R, Frankenreiter S, Friebe A, Calamaras T, Baumgartner R, McLaughlin A, Aronovitz M, Baur W, Wang GR, Kapur N, Karas R, Blanton R, Hell S, Waldman SA, Lin JE, Colon-Gonzalez F, Kim GW, Blomain ES, Merlino D, Snook A, Erdmann J, Wobst J, Kessler T, Schunkert H, Walter U, Pagel O, Walter E, Gambaryan S, Smolenski A, Jurk K, Zahedi R, Klinger JR, Benza RL, Corris PA, Langleben D, Naeije R, Simonneau G, Meier C, Colorado P, Chang MK, Busse D, Hoeper MM, Masferrer JL, Jacobson S, Liu G, Sarno R, Bernier S, Zhang P, Todd Milne G, Flores-Costa R, Currie M, Hall K, Möhrle D, Reimann K, Wolter S, Wolters M, Mergia E, Eichert N, Geisler HS, Ruth P, Friebe A, Feil R, Zimmermann U, Koesling D, Knipper M, Rüttiger L, Tanaka Y, Okamoto A, Nojiri T, Kumazoe M, Tokudome T, Miura K, Hino J, Hosoda H, Miyazato M, Kangawa K, Kapil V, Ahluwalia A, Paolocci N, Eaton P, Campbell JC, Henning P, Franz E, Sankaran B, Herberg FW, Kim C, Wittwer M, Luo Q, … See abstract for full author list ➔ Todd Milne G, et al. Among authors: sarko c. BMC Pharmacol Toxicol. 2017 Oct 10;18(Suppl 1):64. doi: 10.1186/s40360-017-0170-5. BMC Pharmacol Toxicol. 2017. PMID: 29035170 Free PMC article. No abstract available.
A Soluble Guanylate Cyclase Activator Inhibits the Progression of Diabetic Nephropathy in the ZSF1 Rat.
Boustany-Kari CM, Harrison PC, Chen H, Lincoln KA, Qian HS, Clifford H, Wang H, Zhang X, Gueneva-Boucheva K, Bosanac T, Wong D, Fryer RM, Richman JG, Sarko C, Pullen SS. Boustany-Kari CM, et al. Among authors: sarko c. J Pharmacol Exp Ther. 2016 Mar;356(3):712-9. doi: 10.1124/jpet.115.230706. Epub 2016 Jan 4. J Pharmacol Exp Ther. 2016. PMID: 26729306
Indole RSK inhibitors. Part 1: discovery and initial SAR.
Boyer SJ, Burke J, Guo X, Kirrane TM, Snow RJ, Zhang Y, Sarko C, Soleymanzadeh L, Swinamer A, Westbrook J, Dicapua F, Padyana A, Cogan D, Gao A, Xiong Z, Madwed JB, Kashem M, Kugler S, O'Neill MM. Boyer SJ, et al. Among authors: sarko c. Bioorg Med Chem Lett. 2012 Jan 1;22(1):733-7. doi: 10.1016/j.bmcl.2011.10.030. Epub 2011 Oct 14. Bioorg Med Chem Lett. 2012. PMID: 22100312
17 results