日期:
2020 年 — 2026 年
2020
2021
2022
2023
2024
2025
2026
影响因子:

Leveraging fragment-based drug discovery to advance 3D scaffolds into potent ligands: application to the histamine H(1) receptor

利用基于片段的药物发现方法将3D支架转化为高效配体:以组胺H(1)受体为例

Dekker, Tom; van Linden, Oscar P J; Lim, Herman D; Dekker, Mabel E; Vischer, Henry F; Leurs, Rob; van der Meer, Tiffany; Buzink, Maurice C M L; Hamilton, David J; Zarzycka, Barbara; Janssen, Elwin; Wijtmans, Maikel; de Esch, Iwan J P

Structural visualization of small molecule recognition by CXCR3 uncovers dual-agonism in the CXCR3-CXCR7 system.

CXCR3 对小分子识别的结构可视化揭示了 CXCR3-CXCR7 系统中的双重激动作用

Saha Shirsha, Sano Fumiya K, Sharma Saloni, Ganguly Manisankar, Dalal Annu, Mishra Sudha, Tiwari Divyanshu, Akasaka Hiroaki, Kobayashi Takaaki A, Roy Nabarun, Zaidi Nashrah, Itoh Yuzuru, Leurs Rob, Banerjee Ramanuj, Shihoya Wataru, Nureki Osamu, Shukla Arun K

Recent Developments in the Optical Control of Adrenergic Signaling

肾上腺素能信号光学控制的最新进展

Shi, Shuang; Cao, Yangzhi; Wijtmans, Maikel; Vischer, Henry F; Leurs, Rob

Photo-clenbuterol: Optical Control of β(2)-Adrenergic Receptor Signaling by Photoswitchable Ligand Efficacy.

光克仑特罗:通过光开关配体效力对β(2)-肾上腺素能受体信号传导进行光学控制

Cao Yangzhi, Shi Shuang, Does Simone A H, Buzink Christian M L, Gao Meichun, de Esch Iwan J P, Vischer Henry F, Wijtmans Maikel, Leurs Rob

Design, Synthesis and Pharmacological Characterization of the First Photoswitchable Small-Molecule Agonist for the Atypical Chemokine Receptor 3

首个非典型趋化因子受体3的光开关小分子激动剂的设计、合成和药理学表征

Bérenger, Sophie; Adamska, Justyna M; Deflorian, Francesca; de Graaf, Chris; Palmer, Christie B; Szpakowska, Martyna; Chevigné, Andy; de Esch, Iwan J P; Zarzycka, Barbara; Vischer, Henry F; Wijtmans, Maikel; Leurs, Rob

Inhibition of constitutive activity of the atypical chemokine receptor 3 by the small-molecule inverse agonist VUF16840

小分子反向激动剂VUF16840对非典型趋化因子受体3组成活性的抑制

Bosma, Reggie; Nesheva, Desislava; Rijnsburger, Merel; Riemens, Rick; Adamska, Justyna M; Meyrath, Max; Mobach, Simon; Buzink, C Maurice; van der Pol, Suzanne; de Esch, Iwan J P; Szpakowska, Martyna; Wijtmans, Maikel; Chevigne, Andy; Vischer, Henry F; Leurs, Rob

Structural basis of ligand recognition and design of antihistamines targeting histamine H(4) receptor.

组胺H(4)受体配体识别的结构基础及抗组胺药设计

Xia Ruixue, Shi Shuang, Xu Zhenmei, Vischer Henry F, Windhorst Albert D, Qian Yu, Duan Yaning, Liang Jiale, Chen Kai, Zhang Anqi, Guo Changyou, Leurs Rob, He Yuanzheng

Inhibitors of malaria parasite cyclic nucleotide phosphodiesterases block asexual blood-stage development and mosquito transmission.

疟原虫环核苷酸磷酸二酯酶抑制剂可阻断无性血液期发育和蚊子传播

Gomez-Gonzalez Paula-Josefina, Gupta Antima, Drought Laura G, Patel Avnish, Okombo John, van der Watt Mariëtte, Walker-Gray Ryan, Schindler Kyra A, Burkhard Anna Y, Yeo Tomas, Narwal Sunil K, Bloxham Talia S, Flueck Christian, Walker Eloise M, Rey Joshua A, Fairhurst Kate J, Reader Janette, Park Heekuk, Pollard Harry G, Stewart Lindsay B, Brandner-Garrod Luke, Kristan Mojca, Sterk Geert-Jan, van Nuland Youri M, Manko Emilia, van Schalkwyk Donelly A, Zheng Yang, Leurs Rob, Dechering Koen J, Aguiar Anna Caroline C, Guido Rafael V C, Pereira Dhelio B, Tumwebaze Patrick K, Nosbya Samuel L, Rosenthal Philip J, Cooper Roland A, Palmer Mike, Parkinson Tanya, Burrows Jeremy N, Uhlemann Anne-Catrin, Birkholtz Lyn-Marié, Small-Saunders Jennifer L, Duffy James, Fidock David A, Brown Alan, Gardner Mark, Baker David A

Histamine H(3) Receptor Isoforms: Insights from Alternative Splicing to Functional Complexity

组胺H(3)受体亚型:从选择性剪接到功能复杂性的启示

Gao, Meichun; Ooms, Jasper F; Leurs, Rob; Vischer, Henry F

Small Molecule Fluorescent Ligands for the Atypical Chemokine Receptor 3 (ACKR3)

非典型趋化因子受体 3 (ACKR3) 的小分子荧光配体

Dekkers, Sebastian; Comez, Dehan; Karsai, Noemi; Arimont-Segura, Marta; Canals, Meritxell; Caspar, Birgit; de Graaf, Chris; Kilpatrick, Laura E; Leurs, Rob; Kellam, Barrie; Hill, Stephen J; Briddon, Stephen J; Stocks, Michael J