Search Results - "van de Stolpe, Andrea"

Green Drug Discovery: Novel Fragment Space from the Biomass-Derived Molecule Dihydrolevoglucosenone (Cyrene TM ) by Dekker, Tom, Harteveld, Jaap W, Wágner, Gábor, de Vries, Max C M, Custers, Hans, van de Stolpe, Andrea C, de Esch, Iwan J P, Wijtmans, Maikel

“…Biomass-derived molecules can provide a basis for sustainable drug discovery. However, their full exploration is hampered by the dominance of millions of…”
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Optical control of the β2-adrenergic receptor with opto-prop-2: A cis-active azobenzene analog of propranolol by Bosma, Reggie, Dijon, Nicola C., Zheng, Yang, Schihada, Hannes, Hauwert, Niels J., Shi, Shuang, Arimont, Marta, Riemens, Rick, Custers, Hans, van de Stolpe, Andrea, Vischer, Henry F., Wijtmans, Maikel, Holliday, Nicholas D., Kuster, Diederik W.D., Leurs, Rob

“…In this study, we synthesized and evaluated new photoswitchable ligands for the beta-adrenergic receptors β1-AR and β2-AR, applying an azologization strategy…”
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Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'Receptor knock-down' tool by VAN MUIJLWIJK-KOEZEN, Jacqueline E, TIMMERMAN, Henk, VAN DER SLUIS, Richard P, VAN DE STOLPE, Andrea C, MENGE, Wiro M. P. B, BEUKERS, Margot W, VAN DER GRAAF, Piet H, DE GROOTE, Miriam, IJZERMAN, Adriaan P

“…A new preparative synthetic route for the irreversible adenosine A1 antagonist…”
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Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists by STORELLI, Stefania, VERDIJK, Pauline, VERZIJL, Dennis, TIMMERMAN, Henk, VAN DE STOLPE, Andrea C, TENSEN, Cornelis P, SMIT, Martine J, DE ESCH, Iwan J. P, LEURS, Rob

“…A series of 3-phenyl-3H-quinazolin-4-ones have been synthesized and tested for affinity and activity at the chemokine CXCR3 receptor. The most potent compound…”
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Molecular Determinants of Ligand Binding Modes in the Histamine H 4 Receptor: Linking Ligand-Based Three-Dimensional Quantitative Structure–Activity Relationship (3D-QSAR) Models to in Silico Guided Receptor Mutagenesis Studies by Istyastono, Enade P., Nijmeijer, Saskia, Lim, Herman D., van de Stolpe, Andrea, Roumen, Luc, Kooistra, Albert J., Vischer, Henry F., de Esch, Iwan J. P., Leurs, Rob, de Graaf, Chris

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Catechol Pyrazolinones as Trypanocidals: Fragment-Based Design, Synthesis, and Pharmacological Evaluation of Nanomolar Inhibitors of Trypanosomal Phosphodiesterase B1 by Orrling, Kristina M, Jansen, Chimed, Vu, Xuan Lan, Balmer, Vreni, Bregy, Patrick, Shanmugham, Anitha, England, Paul, Bailey, David, Cos, Paul, Maes, Louis, Adams, Emily, van den Bogaart, Erika, Chatelain, Eric, Ioset, Jean-Robert, van de Stolpe, Andrea, Zorg, Stèphanie, Veerman, Johan, Seebeck, Thomas, Sterk, Geert Jan, de Esch, Iwan J. P, Leurs, Rob

“…Trypanosomal phosphodiesterases B1 and B2 (TbrPDEB1 and TbrPDEB2) play an important role in the life cycle of Trypanosoma brucei, the causative parasite of…”
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Molecular Determinants of Ligand Binding Modes in the Histamine H4 Receptor: Linking Ligand-Based Three-Dimensional Quantitative Structure–Activity Relationship (3D-QSAR) Models to in Silico Guided Receptor Mutagenesis Studies by Istyastono, Enade P, Nijmeijer, Saskia, Lim, Herman D, van de Stolpe, Andrea, Roumen, Luc, Kooistra, Albert J, Vischer, Henry F, de Esch, Iwan J. P, Leurs, Rob, de Graaf, Chris

“…The histamine H4 receptor (H4R) is a G protein-coupled receptor (GPCR) that plays an important role in inflammation. Similar to the homologous histamine H3…”
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Synthesis and Structure−Activity Relationships of Carboxyflavones as Structurally Rigid CysLT 1 (LTD4) Receptor Antagonists by Zwaagstra, Mariël E, Timmerman, Henk, van de Stolpe, Andrea C, de Kanter, Frans J. J, Tamura, Masahiro, Wada, Yasushi, Zhang, Ming-Qiang

“…The synthesis and Cys LT 1 receptor affinities of a new series of highly rigid 3‘- and 4‘-(2-quinolinylmethoxy)- or 3‘- and…”
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Synthesis and Structure−Activity Relationships of Carboxyflavones as Structurally Rigid CysLT1 (LTD4) Receptor Antagonists by ZWAAGSTRA, Mariël E., TIMMERMAN, Henk, VAN DE STOLPE, Andrea C., DE KANTER, Frans J. J., TAMURA, Masahiro, WADA, Yasushi, ZHANG, Ming-Qiang

“…The synthesis and CysLT1 receptor affinities of a new series of highly rigid 3'- and 4'-(2-quinolinylmethoxy)- or 3'- and…”
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Clobenpropit analogs as dual activity ligands for the histamine H 3 and H 4 receptors: Synthesis, pharmacological evaluation, and cross-target QSAR studies by Lim, Herman D., Istyastono, Enade P., van de Stolpe, Andrea, Romeo, Giuseppe, Gobbi, Silvia, Schepers, Marjo, Lahaye, Roger, Menge, Wiro M.B.P., Zuiderveld, Obbe P., Jongejan, Aldo, Smits, Rogier A., Bakker, Remko A., Haaksma, Eric E.J., Leurs, Rob, de Esch, Iwan J.P.

“…Some clobenpropit analogs were synthesized and pharmacologically characterized as dual activity ligands for the histamine H 3 and H 4 receptors. QSAR models…”
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Clobenpropit analogs as dual activity ligands for the histamine H3 and H4 receptors: Synthesis, pharmacological evaluation, and cross-target QSAR studies by LIM, Herman D, ISTYASTONO, Enade P, SMITS, Rogier A, BAKKER, Remko A, HAAKSMA, Eric E. J, LEURS, Rob, DE ESCH, Iwan J. P, VAN DE STOLPE, Andrea, ROMEO, Giuseppe, GOBBI, Silvia, SCHEPERS, Marjo, LAHAYE, Roger, MENGE, Wiro M. B. P, ZUIDERVELD, Obbe P, JONGEJAN, Aldo

“…Previous studies have demonstrated that clobenpropit (N-(4-chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothiourea) binds to both the human histamine H(3)…”
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Clobenpropit analogs as dual activity ligands for the histamine H sub(3 and H) sub(4) receptors: Synthesis, pharmacological evaluation, and cross-target QSAR studies by Lim, Herman D, Istyastono, Enade P, Van de Stolpe, Andrea, Romeo, Giuseppe, Gobbi, Silvia, Schepers, Marjo, Lahaye, Roger, Menge, Wiro MBP, Zuiderveld, Obbe P, Jongejan, Aldo, Smits, Rogier A, Bakker, Remko A, Haaksma, Eric EJ, Leurs, Rob, De Esch, Iwan JP

“…Previous studies have demonstrated that clobenpropit (N-(4-chlorobenzyl)-S-[3-(4(5)-imidazolyl)propyl]isothiourea) binds to both the human histamine H sub(3…”
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Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies by Istyastono, Enade P, Nijmeijer, Saskia, Lim, Herman D, van de Stolpe, Andrea, Roumen, Luc, Kooistra, Albert J, Vischer, Henry F, de Esch, Iwan J P, Leurs, Rob, de Graaf, Chris

“…The histamine H(4) receptor (H(4)R) is a G protein-coupled receptor (GPCR) that plays an important role in inflammation. Similar to the homologous histamine…”
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Synthesis and structure–activity relationship of 3-phenyl-3 H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists by Storelli, Stefania, Verdijk, Pauline, Verzijl, Dennis, Timmerman, Henk, van de Stolpe, Andrea C., Tensen, Cornelis P., Smit, Martine J., De Esch, Iwan J.P., Leurs, Rob

“…[Display omitted] A series of 3-phenyl-3 H-quinazolin-4-ones have been synthesized and tested for affinity and activity at the chemokine CXCR3 receptor. The…”
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Synthesis and use of FSCPX, an irreversible adenosine A 1 antagonist, as a ‘Receptor Knock-Down’ tool by Muijlwijk-Koezen, Jacqueline E.van, Timmerman, Henk, der Sluis, Richard P.van, van de Stolpe, Andrea C, Menge, Wiro M.P.B, Beukers, Margot W, van der Graaf, Piet H, de Groote, Miriam, IJzerman, Adriaan P

“…A new preparative synthetic route for the irreversible adenosine A 1 antagonist 8-cyclopentyl-3- N-[3-((3-(4-fluorosulphonyl)benzoyl)-oxy)-propyl]-1-…”
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