Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity-Reference-Cited by-同舟云学术

Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity

Published:2018-04-19 Issue:9 Volume:61 Page:3870-3888
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Blaazer Antoni R.¹^ORCID,Singh Abhimanyu K.²,de Heuvel Erik¹,Edink Ewald¹,Orrling Kristina M.¹,Veerman Johan J. N.³,van den Bergh Toine³,Jansen Chimed¹,Balasubramaniam Erin²,Mooij Wouter J.¹,Custers Hans¹,Sijm Maarten¹,Tagoe Daniel N. A.⁴,Kalejaiye Titilola D.⁴,Munday Jane C.⁴,Tenor Hermann⁵,Matheeussen An⁶,Wijtmans Maikel¹^ORCID,Siderius Marco¹,de Graaf Chris¹^ORCID,Maes Louis⁶,de Koning Harry P.⁴,Bailey David S.⁷,Sterk Geert Jan¹,de Esch Iwan J. P.¹,Brown David G.²,Leurs Rob¹^ORCID

Affiliation:

1. Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems, Vrije Universiteit Amsterdam, 1081 HZ Amsterdam, The Netherlands

2. School of Biosciences, University of Kent, Canterbury CT2 7NJ, U.K.

3. Mercachem, 6546 BB Nijmegen, The Netherlands

4. Institute of Infection, Immunity and Inflammation, University of Glasgow, Glasgow G12 8TA, U.K.

5. Topadur Pharma AG, 8952 Schlieren, Switzerland

6. Laboratory for Microbiology, Parasitology and Hygiene, University of Antwerp, 2610 Wilrijk, Belgium

7. IOTA Pharmaceuticals, Cambridge CB4 0WS, U.K.

Funder

FP7 Health

Nederlandse Organisatie voor Wetenschappelijk Onderzoek

Top Institute Pharma

Publisher

American Chemical Society (ACS)