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The discovery of a novel series of potential ERRα inverse agonists based on p-nitrobenzenesulfonamide template for triple-negative breast cancer in vivo
Author / Creator:Gao, Zhipei ; Wang, Tianxiao ; Li, Rui ; Du, Yongli ; Lv, Han ; Zhang, Liudi ; Chen, Haifei ; Shi, Xiaojin ; Li, Qunyi ; Shen, Jingkang
Publisher:England: Taylor & Francis
Journal title:Journal of enzyme inhibition and medicinal chemistry, 2022-12, Vol.37 (1), p.125-134
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Crystallography-guided discovery of carbazole-based retinoic acid-related orphan receptor gamma-t (RORγt) modulators: insights into different protein behaviors with “short” and “long” inverse agonists
Author / Creator:Yu, Ming-cheng ; Yang, Feng ; Ding, Xiao-yu ; Sun, Nan-nan ; Jiang, Zheng-yuan ; Huang, Ya-fei ; Yan, Yu-rong ; Zhu, Chen ; Xie, Qiong ; Chen, Zhi-feng ; Guo, Si-qi ; Jiang, Hua-liang ; Chen, Kai-xian ; Luo, Cheng ; Luo, Xiao-min ; Chen, Shi-jie ; Wang, Yong-hui
Publisher:Singapore: Springer Singapore
Journal title:Acta pharmacologica Sinica, 2021-09, Vol.42 (9), p.1524-1534
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Molecular Dynamics Simulations Based on 1-Phenyl-4-Benzoyl-1-Hydro-Triazole ERRα Inverse Agonists
Author / Creator:Gao, Zhipei ; Du, Yongli ; Sheng, Xiehuang ; Shen, Jingkang
Publisher:Switzerland: MDPI AG
Journal title:International journal of molecular sciences, 2021-04, Vol.22 (7), p.3724
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Piperazine- and Piperidine-Containing Thiazolo[5,4-d]pyrimidine Derivatives as New Potent and Selective Adenosine A2A Receptor Inverse Agonists
Author / Creator:Varano, Flavia ; Catarzi, Daniela ; Vigiani, Erica ; Vincenzi, Fabrizio ; Pasquini, Silvia ; Varani, Katia ; Colotta, Vittoria
Publisher:Basel: MDPI AG
Journal title:Pharmaceuticals (Basel, Switzerland), 2020-07, Vol.13 (8), p.161
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Flipping the GPCR Switch: Structure-Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists
Author / Creator:Kosar, Miroslav ; Sarott, Roman C. ; Sykes, David A. ; Viray, Alexander E. G. ; Vitale, Rosa Maria ; Tomašević, Nataša ; Li, Xiaoting ; Ganzoni, Rudolf L. Z. ; Kicin, Bilal ; Reichert, Lisa ; Patej, Kacper J. ; Gómez-Bouzó, Uxía ; Guba, Wolfgang ; McCormick, Peter J. ; Hua, Tian ; Gruber, Christian W. ; Veprintsev, Dmitry B. ; Frank, James A. ; Grether, Uwe ; Carreira, Erick M.
Publisher:United States: American Chemical Society
Journal title:ACS central science, 2024-05, Vol.10 (5), p.956-968
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RORγt inverse agonists demonstrating a margin between inhibition of IL-17A and thymocyte apoptosis RORγt inverse agonists demonstrating a margin between inhibition of IL-17A and thymocyte apoptosis
Author / Creator:Mia Collins ; Rikard Pehrson ; Hanna Grindebacke ; Agnes Leffler ; Marie Ramnegård ; Helena Rannikmäe ; Nina Krutrök ; Linda Yrlid ; Charlotte Pollard ; Ian Dainty ; Frank Narjes ; Stefan von Berg ; Antonio Llinas ; Anna Malmberg ; Jane McPheat ; Eva Hansson ; Elisabeth Bäck ; Jenny Bernström ; Thomas G. Hansson ; David Keeling ; Johan Jirholt
Publisher:Public Library of Science (PLoS)
Journal title:PloS one, 2025-01, Vol.20 (1)
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Structure-Based Identification of Potent Natural Product Chemotypes as Cannabinoid Receptor 1 Inverse Agonists
Author / Creator:Pandey, Pankaj ; Roy, Kuldeep K. ; Liu, Haining ; Ma, Guoyi ; Pettaway, Sara ; Alsharif, Walid F. ; Gadepalli, Rama S. ; Rimoldi, John M. ; McCurdy, Christopher R. ; Cutler, Stephen J. ; Doerksen, Robert J.
Publisher:Switzerland: MDPI
Journal title:Molecules (Basel, Switzerland), 2018-10, Vol.23 (10), p.2630
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Biology and therapeutic potential of cannabinoid CB2 receptor inverse agonists
Author / Creator:Lunn, C A ; Reich, E‐P ; Fine, J S ; Lavey, B ; Kozlowski, J A ; Hipkin, R W ; Lundell, D J ; Bober, L
Publisher:Oxford, UK: Blackwell Publishing Ltd
Journal title:British journal of pharmacology, 2008-01, Vol.153 (2), p.226-239
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2-Arylpropionic Acid Pyrazolamides as Cannabinoid CB2 Receptor Inverse Agonists Endowed with Anti-Inflammatory Properties
Author / Creator:de Oliveira, Daniela R. ; Maia, Rodolfo C. ; de Carvalho França, Patrícia R. ; Fernandes, Patrícia D. ; Barbosa, Gisele ; Lima, Lídia M. ; Fraga, Carlos A. Manssour
Publisher:Switzerland: MDPI AG
Journal title:Pharmaceuticals (Basel, Switzerland), 2022-12, Vol.15 (12), p.1519
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Docking 14 Million Virtual Isoquinuclidines against the μ and κ Opioid Receptors Reveals Dual Antagonists–Inverse Agonists with Reduced Withdrawal Effects
Author / Creator:Vigneron, Seth F. ; Ohno, Shohei ; Braz, Joao ; Kim, Joseph Y. ; Kweon, Oh Sang ; Webb, Chase ; Billesbølle, Christian B. ; Srinivasan, Karthik ; Bhardwaj, Karnika ; Irwin, John J. ; Manglik, Aashish ; Basbaum, Allan I. ; Ellman, Jonathan A. ; Shoichet, Brian K.
Publisher:United States: American Chemical Society
Journal title:ACS central science, 2025-05, Vol.11 (5), p.770-790
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Design, synthesis, and anticonvulsant effects evaluation of nonimidazole histamine H3 receptor antagonists/inverse agonists containing triazole moiety
Author / Creator:Song, Mingxia ; Yan, Rui ; Zhang, Yanhui ; Guo, Dongfu ; Zhou, Naiming ; Deng, XianQing
Publisher:Abingdon: Taylor & Francis
Journal title:Journal of enzyme inhibition and medicinal chemistry, 2020-01, Vol.35 (1), p.1310-1321
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Cannabinoid-1 receptor inverse agonists: current understanding of mechanism of action and unanswered questions
Author / Creator:Fong, T.M ; Heymsfield, S.B
Publisher:London: Nature Publishing Group UK
Journal title:International Journal of Obesity, 2009-09, Vol.33 (9), p.947-955
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Molecular Mechanism of Action of RORγt Agonists and Inverse Agonists: Insights from Molecular Dynamics Simulation
Author / Creator:Sun, Nannan ; Yuan, Congmin ; Ma, Xiaojun ; Wang, Yonghui ; Gu, Xianfeng ; Fu, Wei
Publisher:Switzerland: MDPI AG
Journal title:Molecules (Basel, Switzerland), 2018-12, Vol.23 (12), p.3181
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Histamine H3 receptor inverse agonists/antagonists influence intra-regional cortical activity and inter-regional synchronization during resting state: an exploratory cortex-wide imaging study in mice
Author / Creator:Kaita, Sentaro ; Morishita, Yoshikazu ; Kobayashi, Kenta ; Nomura, Hiroshi
Publisher:London: BioMed Central Ltd
Journal title:Molecular brain, 2024-11, Vol.17 (1), p.88-12, Article 88
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Structural mechanism of CB 1 R binding to peripheral and biased inverse agonists
Author / Creator:Kumari, Punita ; Dvorácskó, Szabolcs ; Enos, Michael D ; Ramesh, Karthik ; Lim, Darrix ; Hassan, Sergio A ; Kunos, George ; Cinar, Resat ; Iyer, Malliga R ; Rosenbaum, Daniel M
Publisher:England
Journal title:Nature communications, 2024-12, Vol.15 (1), p.10694
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Discovery and structural optimization of 4-(4-(benzyloxy)phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists
Author / Creator:Wu, Xi-shan ; Wang, Rui ; Xing, Yan-li ; Xue, Xiao-qian ; Zhang, Yan ; Lu, Yong-zhi ; Song, Yu ; Luo, Xiao-yu ; Wu, Chun ; Zhou, Yu-lai ; Jiang, Jian-qin ; Xu, Yong
Publisher:London: Nature Publishing Group UK
Journal title:Acta pharmacologica Sinica, 2016-11, Vol.37 (11), p.1516-1524
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Towards Translation of PqsR Inverse Agonists: From In Vitro Efficacy Optimization to In Vivo Proof‐of‐Principle (Adv. Sci. 5/2023)
Author / Creator:Hamed, Mostafa M. ; Abdelsamie, Ahmed S. ; Rox, Katharina ; Schütz, Christian ; Kany, Andreas M. ; Röhrig, Teresa ; Schmelz, Stefan ; Blankenfeldt, Wulf ; Arce‐Rodriguez, Alejandro ; Borrero‐de Acuña, José Manuel ; Jahn, Dieter ; Rademacher, Jessica ; Ringshausen, Felix C. ; Cramer, Nina ; Tümmler, Burkhard ; Hirsch, Anna K. H. ; Hartmann, Rolf W. ; Empting, Martin
Publisher:Weinheim: John Wiley & Sons, Inc
Journal title:Advanced science, 2023-02, Vol.10 (5), p.n/a
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Mechano-sensitivity of β2-adrenoceptors enhances constitutive activation of cAMP generation that is inhibited by inverse agonists
Author / Creator:Cullum, Sean A. ; Platt, Simon ; Dale, Natasha ; Isaac, Oliver C. ; Wragg, Edward S. ; Soave, Mark ; Veprintsev, Dmitry B. ; Woolard, Jeanette ; Kilpatrick, Laura E. ; Hill, Stephen J.
Publisher:London: Nature Publishing Group UK
Journal title:Communications biology, 2024-04, Vol.7 (1), p.417-16, Article 417
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Regulation of cannabinoid CB2 receptor constitutive activity in vivo: repeated treatments with inverse agonists reverse the acute activation of JNK and associated apoptotic signaling in mouse brain
Author / Creator:Salort, Glòria ; Álvaro-Bartolomé, María ; García-Sevilla, Jesús A.
Publisher:Berlin/Heidelberg: Springer Berlin Heidelberg
Journal title:Psychopharmacology, 2017-03, Vol.234 (6), p.925-941
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Should inverse agonists be defined by pharmacological mechanism or clinical effect?
Author / Creator:Burstein, Ethan S.
Publisher:New York, USA: Cambridge University Press
Journal title:CNS spectrums, 2019-08, Vol.24 (4), p.349-351
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The discovery of a novel series of potential ERRα inverse agonists based on p-nitrobenzenesulfonamide template for triple-negative breast cancer in vivo

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Crystallography-guided discovery of carbazole-based retinoic acid-related orphan receptor gamma-t (RORγt) modulators: insights into different protein behaviors with “short” and “long” inverse agonists

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Molecular Dynamics Simulations Based on 1-Phenyl-4-Benzoyl-1-Hydro-Triazole ERRα Inverse Agonists

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Piperazine- and Piperidine-Containing Thiazolo[5,4-d]pyrimidine Derivatives as New Potent and Selective Adenosine A2A Receptor Inverse Agonists

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Flipping the GPCR Switch: Structure-Based Development of Selective Cannabinoid Receptor 2 Inverse Agonists

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RORγt inverse agonists demonstrating a margin between inhibition of IL-17A and thymocyte apoptosis RORγt inverse agonists demonstrating a margin between inhibition of IL-17A and thymocyte apoptosis

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Structure-Based Identification of Potent Natural Product Chemotypes as Cannabinoid Receptor 1 Inverse Agonists

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Biology and therapeutic potential of cannabinoid CB2 receptor inverse agonists

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2-Arylpropionic Acid Pyrazolamides as Cannabinoid CB2 Receptor Inverse Agonists Endowed with Anti-Inflammatory Properties

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Docking 14 Million Virtual Isoquinuclidines against the μ and κ Opioid Receptors Reveals Dual Antagonists–Inverse Agonists with Reduced Withdrawal Effects

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Design, synthesis, and anticonvulsant effects evaluation of nonimidazole histamine H3 receptor antagonists/inverse agonists containing triazole moiety

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Cannabinoid-1 receptor inverse agonists: current understanding of mechanism of action and unanswered questions

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Molecular Mechanism of Action of RORγt Agonists and Inverse Agonists: Insights from Molecular Dynamics Simulation

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Histamine H3 receptor inverse agonists/antagonists influence intra-regional cortical activity and inter-regional synchronization during resting state: an exploratory cortex-wide imaging study in mice

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Structural mechanism of CB 1 R binding to peripheral and biased inverse agonists

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Discovery and structural optimization of 4-(4-(benzyloxy)phenyl)-3,4-dihydropyrimidin-2(1H)-ones as RORc inverse agonists

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Towards Translation of PqsR Inverse Agonists: From In Vitro Efficacy Optimization to In Vivo Proof‐of‐Principle (Adv. Sci. 5/2023)

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Mechano-sensitivity of β2-adrenoceptors enhances constitutive activation of cAMP generation that is inhibited by inverse agonists

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Regulation of cannabinoid CB2 receptor constitutive activity in vivo: repeated treatments with inverse agonists reverse the acute activation of JNK and associated apoptotic signaling in mouse brain

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Should inverse agonists be defined by pharmacological mechanism or clinical effect?

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