Literature DB >> 33871981

Early Stages of Drug Discovery in an Academic Institution and Involvement of Pharma for Advancing Promising Leads.

Michael H Gelb, Frederick S Buckner.   

Abstract

In this Viewpoint, we provide a brief description of two efforts to develop drugs to treat diseases caused by tropical parasites (Malaria, human African trypanosomiasis and Chagas disease). These efforts are largely based in a University setting but draw heavily on Pharma for a complete progression from drug hit discovery to advancement toward clinical trials. The first case is the development of protein farnesyltransferase inhibitors, and the second case is a series of benzthiazoles, the target of which is being investigated.

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Year:  2021        PMID: 33871981      PMCID: PMC9323184          DOI: 10.1021/acsinfecdis.1c00091

Source DB:  PubMed          Journal:  ACS Infect Dis        ISSN: 2373-8227            Impact factor:   5.578


  12 in total

1.  Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites.

Authors:  Matthew P Glenn; Sung-Youn Chang; Carrie Hornéy; Kasey Rivas; Kohei Yokoyama; Erin E Pusateri; Steven Fletcher; Christopher G Cummings; Frederick S Buckner; Prakash R Pendyala; Debopam Chakrabarti; Saïd M Sebti; Michael Gelb; Wesley C Van Voorhis; Andrew D Hamilton
Journal:  J Med Chem       Date:  2006-09-21       Impact factor: 7.446

Review 2.  How were new medicines discovered?

Authors:  David C Swinney; Jason Anthony
Journal:  Nat Rev Drug Discov       Date:  2011-06-24       Impact factor: 84.694

Review 3.  Prenyl proteins in eukaryotic cells: a new type of membrane anchor.

Authors:  J A Glomset; M H Gelb; C C Farnsworth
Journal:  Trends Biochem Sci       Date:  1990-04       Impact factor: 13.807

4.  Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.

Authors:  Hari Babu Tatipaka; J Robert Gillespie; Arnab K Chatterjee; Neil R Norcross; Matthew A Hulverson; Ranae M Ranade; Pendem Nagendar; Sharon A Creason; Joshua McQueen; Nicole A Duster; Advait Nagle; Frantisek Supek; Valentina Molteni; Tanja Wenzler; Reto Brun; Richard Glynne; Frederick S Buckner; Michael H Gelb
Journal:  J Med Chem       Date:  2014-01-15       Impact factor: 7.446

Review 5.  Fexinidazole: First Global Approval.

Authors:  Emma D Deeks
Journal:  Drugs       Date:  2019-02       Impact factor: 9.546

6.  Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis.

Authors:  Pendem Nagendar; J Robert Gillespie; Zackary M Herbst; Ranae M Ranade; Nora M R Molasky; Omeed Faghih; Rachael M Turner; Michael H Gelb; Frederick S Buckner
Journal:  ACS Med Chem Lett       Date:  2018-12-04       Impact factor: 4.345

7.  Urea Derivatives of 2-Aryl-benzothiazol-5-amines: A New Class of Potential Drugs for Human African Trypanosomiasis.

Authors:  Donald A Patrick; J Robert Gillespie; Joshua McQueen; Matthew A Hulverson; Ranae M Ranade; Sharon A Creason; Zackary M Herbst; Michael H Gelb; Frederick S Buckner; Richard R Tidwell
Journal:  J Med Chem       Date:  2016-12-19       Impact factor: 7.446

8.  SCYX-7158, an orally-active benzoxaborole for the treatment of stage 2 human African trypanosomiasis.

Authors:  Robert T Jacobs; Bakela Nare; Stephen A Wring; Matthew D Orr; Daitao Chen; Jessica M Sligar; Matthew X Jenks; Robert A Noe; Tana S Bowling; Luke T Mercer; Cindy Rewerts; Eric Gaukel; Jennifer Owens; Robin Parham; Ryan Randolph; Beth Beaudet; Cyrus J Bacchi; Nigel Yarlett; Jacob J Plattner; Yvonne Freund; Charles Ding; Tsutomu Akama; Y-K Zhang; Reto Brun; Marcel Kaiser; Ivan Scandale; Robert Don
Journal:  PLoS Negl Trop Dis       Date:  2011-06-28

9.  1-Benzyl-3-aryl-2-thiohydantoin Derivatives as New Anti-Trypanosoma brucei Agents: SAR and in Vivo Efficacy.

Authors:  Andriy Buchynskyy; J Robert Gillespie; Zackary M Herbst; Ranae M Ranade; Frederick S Buckner; Michael H Gelb
Journal:  ACS Med Chem Lett       Date:  2017-07-10       Impact factor: 4.345

10.  Phenotypic Drug Discovery for Human African Trypanosomiasis: A Powerful Approach.

Authors:  Frederick S Buckner; Andriy Buchynskyy; Pendem Nagendar; Donald A Patrick; J Robert Gillespie; Zackary Herbst; Richard R Tidwell; Michael H Gelb
Journal:  Trop Med Infect Dis       Date:  2020-02-05
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  1 in total

Review 1.  An Updated View of the Trypanosoma cruzi Life Cycle: Intervention Points for an Effective Treatment.

Authors:  Javier Martín-Escolano; Clotilde Marín; María J Rosales; Anastasios D Tsaousis; Encarnación Medina-Carmona; Rubén Martín-Escolano
Journal:  ACS Infect Dis       Date:  2022-06-02       Impact factor: 5.578

  1 in total

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