Phenotypic Drug Discovery for Human African Trypanosomiasis: A Powerful Approach

Autor: Frederick S. Buckner, Andriy Buchynskyy, Pendem Nagendar, Donald A. Patrick, J. Robert Gillespie, Zackary Herbst, Richard R. Tidwell, Michael H. Gelb

Publikováno v: Tropical Medicine and Infectious Disease, Vol 5, Iss 1, p 23 (2020)

The work began with the screening of a library of 700,000 small molecules for inhibitors of Trypanosoma brucei growth (a phenotypic screen). The resulting set of 1035 hit compounds was reviewed by a team of medicinal chemists, leading to the nominati

Externí odkaz: https://doaj.org/article/017ace40eccb475fa72c44de9f674162

Structures of Trypanosoma brucei methionyl-tRNA synthetase with urea-based inhibitors provide guidance for drug design against sleeping sickness.

Autor: Cho Yeow Koh, Jessica E Kim, Allan B Wetzel, Will J de van der Schueren, Sayaka Shibata, Ranae M Ranade, Jiyun Liu, Zhongsheng Zhang, J Robert Gillespie, Frederick S Buckner, Christophe L M J Verlinde, Erkang Fan, Wim G J Hol

Publikováno v: PLoS Neglected Tropical Diseases, Vol 8, Iss 4, p e2775 (2014)

Methionyl-tRNA synthetase of Trypanosoma brucei (TbMetRS) is an important target in the development of new antitrypanosomal drugs. The enzyme is essential, highly flexible and displaying a large degree of changes in protein domains and binding pocket

Externí odkaz: https://doaj.org/article/d5d82033472f498782042305c840c109

Synthesis and Structure-Activity Relationships of Imidazopyridine/Pyrimidine- and Furopyridine-Based Anti-infective Agents against Trypanosomiases

Autor: Frederick S. Buckner, An Matheeussen, J. Robert Gillespie, Guy Caljon, Fernando Fumagalli, Anna Junker, Louis Maes, Flavio da Silva Emery, Nora Molasky, Daniel G. Silva, Shaiani Maria Gil de Melo

Publikováno v: Chemmedchem
ChemMedChem

Neglected tropical diseases remain among the most critical public health concerns in Africa and South America. The drug treatments for these diseases are limited, which invariably leads to fatal cases. Hence, there is an urgent need for new antitrypa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e955ddc91a38dd68a24b38d1ea072b63
https://pubmed.ncbi.nlm.nih.gov/33078573

Phenotypic Drug Discovery for Human African Trypanosomiasis: A Powerful Approach

Autor: Zackary M. Herbst, Frederick S. Buckner, Andriy Buchynskyy, Pendem Nagendar, Michael H. Gelb, Richard R. Tidwell, Donald A. Patrick, J. Robert Gillespie

Publikováno v: Tropical Medicine and Infectious Disease, Vol 5, Iss 1, p 23 (2020)
Tropical Medicine and Infectious Disease
Tropical Medicine and Infectious Disease; Volume 5; Issue 1; Pages: 23

The work began with the screening of a library of 700,000 small molecules for inhibitors of Trypanosoma brucei growth (a phenotypic screen). The resulting set of 1035 hit compounds was reviewed by a team of medicinal chemists, leading to the nominati

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dfdf8ceaaff6019c36bdafdccb2409f2
https://www.mdpi.com/2414-6366/5/1/23

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

Autor: Matthew A. Hulverson, Donald A. Patrick, Zackary M. Herbst, Ranae M. Ranade, Michael H. Gelb, Richard R. Tidwell, Joshua McQueen, Sharon A. Creason, J. Robert Gillespie, Frederick S. Buckner

Publikováno v: Journal of Medicinal Chemistry. 60:957-971

A previous publication from this lab (Patrick, et al. Bioorg. Med. Chem. 2016, 24 , 2451 - 2465 ) explored the antitrypanosomal activities of novel derivatives of 2-(2-benzamido)ethyl-4-phenylthiazole (1), which had been identified as a hit against T

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16aa5008d7908a4c4817c116189460d3
https://doi.org/10.1021/acs.jmedchem.6b01163