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 |
| FullText | Text: Availability: 0 |
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| Header | DbId: mdl DbLabel: MEDLINE Ultimate An: 29672041 AccessLevel: 2 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 0 |
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| Items | – Name: Title Label: Title Group: Ti Data: Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AU" term="%22Blaazer+AR%22">Blaazer AR</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands.<br /><searchLink fieldCode="AU" term="%22Singh+AK%22">Singh AK</searchLink>; School of Biosciences , University of Kent , Canterbury CT2 7NJ , U.K.<br /><searchLink fieldCode="AU" term="%22de+Heuvel+E%22">de Heuvel E</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands.<br /><searchLink fieldCode="AU" term="%22Edink+E%22">Edink E</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands.<br /><searchLink fieldCode="AU" term="%22Orrling+KM%22">Orrling KM</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands.<br /><searchLink fieldCode="AU" term="%22Veerman+JJN%22">Veerman JJN</searchLink>; Mercachem , 6546 BB Nijmegen , The Netherlands.<br /><searchLink fieldCode="AU" term="%22van+den+Bergh+T%22">van den Bergh T</searchLink>; Mercachem , 6546 BB Nijmegen , The Netherlands.<br /><searchLink fieldCode="AU" term="%22Jansen+C%22">Jansen C</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands.<br /><searchLink fieldCode="AU" term="%22Balasubramaniam+E%22">Balasubramaniam E</searchLink>; School of Biosciences , University of Kent , Canterbury CT2 7NJ , U.K.<br /><searchLink fieldCode="AU" term="%22Mooij+WJ%22">Mooij WJ</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands.<br /><searchLink fieldCode="AU" term="%22Custers+H%22">Custers H</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands.<br /><searchLink fieldCode="AU" term="%22Sijm+M%22">Sijm M</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands.<br /><searchLink fieldCode="AU" term="%22Tagoe+DNA%22">Tagoe DNA</searchLink>; Institute of Infection, Immunity and Inflammation , University of Glasgow , Glasgow G12 8TA , U.K.<br /><searchLink fieldCode="AU" term="%22Kalejaiye+TD%22">Kalejaiye TD</searchLink>; Institute of Infection, Immunity and Inflammation , University of Glasgow , Glasgow G12 8TA , U.K.<br /><searchLink fieldCode="AU" term="%22Munday+JC%22">Munday JC</searchLink>; Institute of Infection, Immunity and Inflammation , University of Glasgow , Glasgow G12 8TA , U.K.<br /><searchLink fieldCode="AU" term="%22Tenor+H%22">Tenor H</searchLink>; Topadur Pharma AG , 8952 Schlieren , Switzerland.<br /><searchLink fieldCode="AU" term="%22Matheeussen+A%22">Matheeussen A</searchLink>; Laboratory for Microbiology, Parasitology and Hygiene , University of Antwerp , 2610 Wilrijk , Belgium.<br /><searchLink fieldCode="AU" term="%22Wijtmans+M%22">Wijtmans M</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands.<br /><searchLink fieldCode="AU" term="%22Siderius+M%22">Siderius M</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands.<br /><searchLink fieldCode="AU" term="%22de+Graaf+C%22">de Graaf C</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands.<br /><searchLink fieldCode="AU" term="%22Maes+L%22">Maes L</searchLink>; Laboratory for Microbiology, Parasitology and Hygiene , University of Antwerp , 2610 Wilrijk , Belgium.<br /><searchLink fieldCode="AU" term="%22de+Koning+HP%22">de Koning HP</searchLink>; Institute of Infection, Immunity and Inflammation , University of Glasgow , Glasgow G12 8TA , U.K.<br /><searchLink fieldCode="AU" term="%22Bailey+DS%22">Bailey DS</searchLink>; IOTA Pharmaceuticals , Cambridge CB4 0WS , U.K.<br /><searchLink fieldCode="AU" term="%22Sterk+GJ%22">Sterk GJ</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands.<br /><searchLink fieldCode="AU" term="%22de+Esch+IJP%22">de Esch IJP</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands.<br /><searchLink fieldCode="AU" term="%22Brown+DG%22">Brown DG</searchLink>; School of Biosciences , University of Kent , Canterbury CT2 7NJ , U.K.<br /><searchLink fieldCode="AU" term="%22Leurs+R%22">Leurs R</searchLink>; Division of Medicinal Chemistry, Amsterdam Institute for Molecules, Medicines and Systems , Vrije Universiteit Amsterdam , 1081 HZ Amsterdam , The Netherlands. – Name: TitleSource Label: Source Group: Src Data: <searchLink fieldCode="JN" term="%229716531%22">Journal of medicinal chemistry</searchLink> [J Med Chem] 2018 May 10; Vol. 61 (9), pp. 3870-3888. <i>Date of Electronic Publication: </i>2018 May 01. – Name: TypePub Label: Publication Type Group: TypPub Data: Journal Article; Research Support, Non-U.S. Gov't – Name: TitleSource Label: Journal Info Group: Src Data: <i>Publisher: </i><searchLink fieldCode="PB" term="%22American+Chemical+Society%22">American Chemical Society </searchLink><i>Country of Publication: </i>United States <i>NLM ID: </i>9716531 <i>Publication Model: </i>Print-Electronic <i>Cited Medium: </i>Internet <i>ISSN: </i>1520-4804 (Electronic) <i>Linking ISSN: </i><searchLink fieldCode="IS" term="%2200222623%22">00222623 </searchLink><i>NLM ISO Abbreviation: </i>J Med Chem <i>Subsets: </i>MEDLINE |
| PLink | https://search.ebscohost.com/login.aspx?direct=true&site=eds-live&db=mdl&AN=29672041 |
| RecordInfo | BibRecord: BibEntity: Identifiers: – Type: doi Value: 10.1021/acs.jmedchem.7b01670 Languages: – Code: eng Text: English PhysicalDescription: Pagination: StartPage: 3870 Titles: – TitleFull: Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity. Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Blaazer AR – PersonEntity: Name: NameFull: Singh AK – PersonEntity: Name: NameFull: de Heuvel E – PersonEntity: Name: NameFull: Edink E – PersonEntity: Name: NameFull: Orrling KM – PersonEntity: Name: NameFull: Veerman JJN – PersonEntity: Name: NameFull: van den Bergh T – PersonEntity: Name: NameFull: Jansen C – PersonEntity: Name: NameFull: Balasubramaniam E – PersonEntity: Name: NameFull: Mooij WJ – PersonEntity: Name: NameFull: Custers H – PersonEntity: Name: NameFull: Sijm M – PersonEntity: Name: NameFull: Tagoe DNA – PersonEntity: Name: NameFull: Kalejaiye TD – PersonEntity: Name: NameFull: Munday JC – PersonEntity: Name: NameFull: Tenor H – PersonEntity: Name: NameFull: Matheeussen A – PersonEntity: Name: NameFull: Wijtmans M – PersonEntity: Name: NameFull: Siderius M – PersonEntity: Name: NameFull: de Graaf C – PersonEntity: Name: NameFull: Maes L – PersonEntity: Name: NameFull: de Koning HP – PersonEntity: Name: NameFull: Bailey DS – PersonEntity: Name: NameFull: Sterk GJ – PersonEntity: Name: NameFull: de Esch IJP – PersonEntity: Name: NameFull: Brown DG – PersonEntity: Name: NameFull: Leurs R IsPartOfRelationships: – BibEntity: Dates: – D: 10 M: 05 Text: 2018 May 10 Type: published Y: 2018 Identifiers: – Type: issn-electronic Value: 1520-4804 Numbering: – Type: volume Value: 61 – Type: issue Value: 9 Titles: – TitleFull: Journal of medicinal chemistry Type: main |
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