Author: Harding, Elijah M. ; Morris, James C. ; Fenwick, Michael K. ; Phan, Isabelle Q. ; Morris, Corbin S. ; Rice, Christopher A. ; Khalifa, Muhammad M. ; Abendroth, Jan ; Golden, Jennifer E. ; Milanes, Jillian E. ; Rozema, Soren D. ; McCord, Hayden T. ; Monaghan, Neil P. ; Wilson, Stevin ; Zigweid, Rachael ; Suryadi, Jimmy

Infection with pathogenic free-living amoebae, including Naegleria fowleri , Acanthamoeba spp., and Balamuthia mandrillaris , can lead to life-threatening illnesses, primarily because of catastrophic central nervous system involvement. Efficacious treatment options for these infections are lacking, and the mortality rate due to infection is high.

01 May 2019·Antimicrobial Agents and ChemotherapyQ2 · MEDICINE

Enzymatic and Structural Characterization of the Naegleria fowleri Glucokinase

Q2 · MEDICINE

Article

Author: Golden, Jennifer E. ; Rozema, Soren D. ; Van Voorhis, Wesley C. ; Phan, Isabelle Q. ; Dranow, David M. ; Milanes, Jillian E. ; Patrick, Stephen L. ; Barrett, Kayleigh F. ; Morris, James C. ; Khalifa, Muhammad M. ; Abendroth, Jan ; Suryadi, Jimmy

Infection with the free-living amoeba Naegleria fowleri leads to life-threatening primary amoebic meningoencephalitis. Efficacious treatment options for these infections are limited, and the mortality rate is very high (∼98%).

07 Dec 2017·ChemMedChemQ3 · MEDICINE

Optimization and Evaluation of Antiparasitic Benzamidobenzoic Acids as Inhibitors of Kinetoplastid Hexokinase 1

Q3 · MEDICINE

Article

Author: Hackler, Amber L. ; Aubé, Jeffrey ; Weiner, Warren S. ; Harris, Michael T. ; Kahney, Elizabeth W. ; Flaherty, Daniel P. ; Morris, James C. ; Khan, Haaris ; Schroeder, Chad E. ; Sharlow, Elizabeth R. ; Patrick, Stephen L. ; Golden, Jennifer E.

AbstractKinetoplastid‐based infections are neglected diseases that represent a significant human health issue. Chemotherapeutic options are limited due to toxicity, parasite susceptibility, and poor patient compliance. In response, we studied a molecular‐target‐directed approach involving intervention of hexokinase activity—a pivotal enzyme in parasite metabolism. A benzamidobenzoic acid hit with modest biochemical inhibition of Trypanosoma brucei hexokinase 1 (TbHK1, IC50=9.1 μm), low mammalian cytotoxicity (IMR90 cells, EC50>25 μm), and no appreciable activity on whole bloodstream‐form (BSF) parasites was optimized to afford a probe with improved TbHK1 potency and, significantly, efficacy against whole BSF parasites (TbHK1, IC50=0.28 μm; BSF, ED50=1.9 μm). Compounds in this series also inhibited the hexokinase enzyme from Leishmania major (LmHK1), albeit with less potency than toward TbHK1, suggesting that inhibition of the glycolytic pathway may be a promising opportunity to target multiple disease‐causing trypanosomatid protozoa.

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Indication	Highest Phase	Country/Location	Organization	Date
Trypanosomiasis, African	Preclinical	United States	University of Pittsburgh	22 Oct 2015

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