Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity.
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| Title: | Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity. |
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| Authors: | Blaazer AR; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands., Singh AK; School of Biosciences , University of Kent , Canterbury CT2 7NJ , U.K., de Heuvel E; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands., Edink E; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands., Orrling KM; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands., Veerman JJN; Mercachem , 6546 BB Nijmegen , The Netherlands., van den Bergh T; Mercachem , 6546 BB Nijmegen , The Netherlands., Jansen C; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands., Balasubramaniam E; School of Biosciences , University of Kent , Canterbury CT2 7NJ , U.K., Mooij WJ; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands., Custers H; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands., Sijm M; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands., Tagoe DNA; Institute of Infection, Immunity and Inflammation , University of Glasgow , Glasgow G12 8TA , U.K., Kalejaiye TD; Institute of Infection, Immunity and Inflammation , University of Glasgow , Glasgow G12 8TA , U.K., Munday JC; Institute of Infection, Immunity and Inflammation , University of Glasgow , Glasgow G12 8TA , U.K., Tenor H; Topadur Pharma AG , 8952 Schlieren , Switzerland., Matheeussen A; Laboratory for Microbiology, Parasitology and Hygiene , University of Antwerp , 2610 Wilrijk , Belgium., Wijtmans M; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands., Siderius M; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands., de Graaf C; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands., Maes L; Laboratory for Microbiology, Parasitology and Hygiene , University of Antwerp , 2610 Wilrijk , Belgium., de Koning HP; Institute of Infection, Immunity and Inflammation , University of Glasgow , Glasgow G12 8TA , U.K., Bailey DS; IOTA Pharmaceuticals , Cambridge CB4 0WS , U.K., Sterk GJ; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands., de Esch IJP; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands., Brown DG; School of Biosciences , University of Kent , Canterbury CT2 7NJ , U.K., Leurs R; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands. |
| Source: | Journal of medicinal chemistry [J Med Chem] 2018 May 10; Vol. 61 (9), pp. 3870-3888. Date of Electronic Publication: 2018 May 01. |
| Publication Type: | Journal Article; Research Support, Non-U.S. Gov't |
| Journal Info: | Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE |
| Database: | MEDLINE Ultimate |
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