Literature DB >> 29541362

Discovery of a Stress-Activated Protein Kinase Inhibitor for Lymphatic Filariasis.

Sreedhar R Tummalapalli1, Rohit Bhat1, Agnieszka Chojnowski1, Monika Prorok1, Tamara Kreiss1, Ronald Goldberg1, Stacie Canan2, Natalie Hawryluk2, Deborah Mortensen2, Vikram Khetani3, Jerome Zeldis3, John J Siekierka1, David P Rotella1.   

Abstract

Lymphatic filariasis infects over 120 million people worldwide and can lead to significant disfigurement and disease. Resistance is emerging with current treatments, and these therapies have dose limiting adverse events; consequently new targets are needed. One approach to achieve this goal is inhibition of parasitic protein kinases involved in circumventing host defense mechanisms. This report describes structure-activity relationships leading to the identification of a potent, orally bioavailable stress activated protein kinase inhibitor that may be used to investigate this hypothesis.

Entities:  

Year:  2018        PMID： 29541362      PMCID： PMC5846038          DOI： 10.1021/acsmedchemlett.7b00477

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  12 in total

1.  Synthesis and biological evaluation of 4-oxycoumarin derivatives as a new class of antifilarial agents.

Authors:  Sweta Misra; Lav Kumar Singh; Jyoti Gupta; Shailja Misra-Bhattacharya; Diksha Katiyar
Journal:  Eur J Med Chem       Date:  2015-02-24       Impact factor: 6.514

Review 2.  Immunopathogenesis of lymphatic filarial disease.

Authors:  Subash Babu; Thomas B Nutman
Journal:  Semin Immunopathol       Date:  2012-10-03       Impact factor: 9.623

3.  The C. elegans p38 MAPK pathway regulates nuclear localization of the transcription factor SKN-1 in oxidative stress response.

Authors:  Hideki Inoue; Naoki Hisamoto; Jae Hyung An; Riva P Oliveira; Eisuke Nishida; T Keith Blackwell; Kunihiro Matsumoto
Journal:  Genes Dev       Date:  2005-09-15       Impact factor: 11.361

4.  Reaction of heterocyclic enamines with nitrile oxide and nitrilimine precursors.

Authors:  Cevher Altuğ; Yasar Dürüst; Mark C Elliott; Benson M Kariuki; Tillique Rorstad; Mark Zaal
Journal:  Org Biomol Chem       Date:  2010-09-01       Impact factor: 3.876

Review 5.  Unresolved issues in anthelmintic pharmacology for helminthiases of humans.

Authors:  Timothy G Geary; Katherine Woo; James S McCarthy; Charles D Mackenzie; John Horton; Roger K Prichard; Nilanthi R de Silva; Piero L Olliaro; Janis K Lazdins-Helds; Dirk A Engels; Donald A Bundy
Journal:  Int J Parasitol       Date:  2009-11-20       Impact factor: 3.981

6.  Draft genome of the filarial nematode parasite Brugia malayi.

Authors:  Elodie Ghedin; Shiliang Wang; David Spiro; Elisabet Caler; Qi Zhao; Jonathan Crabtree; Jonathan E Allen; Arthur L Delcher; David B Guiliano; Diego Miranda-Saavedra; Samuel V Angiuoli; Todd Creasy; Paolo Amedeo; Brian Haas; Najib M El-Sayed; Jennifer R Wortman; Tamara Feldblyum; Luke Tallon; Michael Schatz; Martin Shumway; Hean Koo; Steven L Salzberg; Seth Schobel; Mihaela Pertea; Mihai Pop; Owen White; Geoffrey J Barton; Clotilde K S Carlow; Michael J Crawford; Jennifer Daub; Matthew W Dimmic; Chris F Estes; Jeremy M Foster; Mehul Ganatra; William F Gregory; Nicholas M Johnson; Jinming Jin; Richard Komuniecki; Ian Korf; Sanjay Kumar; Sandra Laney; Ben-Wen Li; Wen Li; Tim H Lindblom; Sara Lustigman; Dong Ma; Claude V Maina; David M A Martin; James P McCarter; Larry McReynolds; Makedonka Mitreva; Thomas B Nutman; John Parkinson; José M Peregrín-Alvarez; Catherine Poole; Qinghu Ren; Lori Saunders; Ann E Sluder; Katherine Smith; Mario Stanke; Thomas R Unnasch; Jenna Ware; Aguan D Wei; Gary Weil; Deryck J Williams; Yinhua Zhang; Steven A Williams; Claire Fraser-Liggett; Barton Slatko; Mark L Blaxter; Alan L Scott
Journal:  Science       Date:  2007-09-21       Impact factor: 47.728

Review 7.  Inflammation and oxidative stress in vertebrate host-parasite systems.

Authors:  Gabriele Sorci; Bruno Faivre
Journal:  Philos Trans R Soc Lond B Biol Sci       Date:  2009-01-12       Impact factor: 6.237

Review 8.  Resistance of filarial nematode parasites to oxidative stress.

Authors:  M E Selkirk; V P Smith; G R Thomas; K Gounaris
Journal:  Int J Parasitol       Date:  1998-09       Impact factor: 3.981

9.  The role of a Brugia malayi p38 MAP kinase ortholog (Bm-MPK1) in parasite anti-oxidative stress responses.

Authors:  Akruti Patel; Agnieszka Nawrocka Chojnowski; Katie Gaskill; William De Martini; Ronald L Goldberg; John J Siekierka
Journal:  Mol Biochem Parasitol       Date:  2010-12-24       Impact factor: 1.759

10.  p38 MAPK regulates expression of immune response genes and contributes to longevity in C. elegans.

Authors:  Emily R Troemel; Stephanie W Chu; Valerie Reinke; Siu Sylvia Lee; Frederick M Ausubel; Dennis H Kim
Journal:  PLoS Genet       Date:  2006-09-11       Impact factor: 5.917
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  2 in total

1.  Discovery of isoxazolyl-based inhibitors of Plasmodium falciparum cGMP-dependent protein kinase.

Authors:  Shams Ul Mahmood; Huimin Cheng; Sreedhar R Tummalapalli; Ramappa Chakrasali; Rammohan R Yadav Bheemanaboina; Tamara Kreiss; Agnieska Chojnowski; Tyler Eck; John J Siekierka; David P Rotella
Journal:  RSC Med Chem       Date:  2019-12-16

2.  Synthesis of 5-(Fluoroalkyl)isoxazole Building Blocks by Regioselective Reactions of Functionalized Halogenoximes.

Authors:  Bohdan A Chalyk; Kateryna V Hrebeniuk; Yulia V Fil; Konstantin S Gavrilenko; Alexander B Rozhenko; Bohdan V Vashchenko; Oleksandr V Borysov; Angelina V Biitseva; Pavlo S Lebed; Iulia Bakanovych; Yurii S Moroz; Oleksandr O Grygorenko
Journal:  J Org Chem       Date:  2019-10-30       Impact factor: 4.354
  2 in total

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