Review
Endocrinology & Metabolism
Siyuan Shen, Chang Zhao, Chao Wu, Suyue Sun, Ziyan Li, Wei Yan, Zhenhua Shao
Summary: GPCRs, as the largest family of transmembrane proteins, regulate various physiological processes. However, their complicated signal transduction pathways and difficulties in drug development have presented challenges. By identifying new ligands that bind to allosteric sites, safer drugs for treating various diseases can be designed.
FRONTIERS IN ENDOCRINOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Andreas Bock, Marcel Bermudez
Summary: Bias agonism in GPCRs is likely a result of preferential allosteric coupling from the ligand binding pocket to a specific transducer, leading to selective activation of desired signaling pathways and potentially reducing side effects.
Article
Chemistry, Physical
Jianfeng Wang, Perveen Fazil, Muhammad Ishaq Ali Shah, Amir Zada, Natasha Anwar, Ghazala Gul Zain, Waliullah Khan, Farooq Jan, Tongfei Lei, Muhammad Ateeq
Summary: Researchers achieved the goal of generating hydrogen gas from water through photocatalysis by growing silver nanoparticles on the surface of SnO2 coupled g-C3N4 nanocomposite. The optimized nanocomposite exhibited superior photocatalytic activity for hydrogen evolution compared to pure g-C3N4 and SnO2.
INTERNATIONAL JOURNAL OF HYDROGEN ENERGY
(2023)
Article
Materials Science, Multidisciplinary
Xiang-Dong Jiang, Wen-Rui Xu, Nasir Ilyas, Ming-Cheng Li, Rui-Kang Guo, Rajwali Khan, Wei Li, Ji-Min Wang
Summary: The CPWR-based optical sensor shows superior sensitivity and figure of merit compared to traditional sensors, and can be tuned to the near-infrared region by adjusting structural parameters.
RESULTS IN PHYSICS
(2021)
Article
Biochemistry & Molecular Biology
Liudi Zhang, Jesse I. Mobbs, Lauren T. May, Alisa Glukhova, David M. Thal
Summary: G-protein coupled receptors (GPCRs) are important therapeutic targets for human disease. Allosteric modulators, which target alternative binding sites, offer opportunities for new therapeutics.
CURRENT OPINION IN STRUCTURAL BIOLOGY
(2023)
Review
Endocrinology & Metabolism
Fanhua Wang, Mingyao Liu, Ning Wang, Jian Luo
Summary: This review discusses the role of G-protein coupled receptors (GPCRs) in osteoarthritis (OA), including the pathophysiological processes involved, preclinical and clinical trial data, and the challenges in developing therapies targeting GPCRs for OA.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Longmei Li, Jin Zhang, Wenjing Sun, Weimin Gong, Changlin Tian, Pan Shi, Chaowei Shi
Summary: This study used F-19 solution NMR spectroscopy to investigate the conformational changes of G proteins upon interaction with detergent mimicking membrane and receptor. The results showed that there are two equilibrium states in the Gain apo states, and the interaction with detergents accelerates the conformational transformation.
CHINESE CHEMICAL LETTERS
(2022)
Review
Biochemistry & Molecular Biology
Alexander O. Shpakov
Summary: Allosteric regulation plays a critical role in the functioning of GPCRs and their signaling pathways. The complexity of allosteric effects caused by various regulators determines the multiplicity and topology of allosteric sites in GPCRs. These sites are involved in the regulation of receptor activity, GPCR-complex formation, and endocytosis. They are also targets for synthetic allosteric regulators and modulators. The review provides an overview of the principles and mechanisms of GPCRs allosteric regulation, the diversity of allosteric sites, and the endogenous and synthetic allosteric regulators.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Physical
Yun Zhou, Peng Zheng, Fang Wang, Fangna Gu, Wenqing Xu, Qinyang Lu, Tingyu Zhu, Ziyi Zhong, Guangwen Xu, Fabing Su
Summary: This study successfully prepared a three-dimensional honeycomb N-doped carbon nanomaterial with good photothermal catalytic performance, and investigated the synergistic effect of NiO@Ni and NC on the CO2 reduction reaction and water splitting reaction.
Article
Chemistry, Medicinal
Claire Shepherd, Sean Robinson, Alice Berizzi, Laura E. J. Thompson, Louise Bird, Simone Culurgioni, Simon Varzandeh, Philip B. Rawlins, Reid H. J. Olsen, Iva Hopkins Navratilova
Summary: This study demonstrates the use of SPR-based biosensors to study the entire human family of adenosine receptors and identify biologically active novel binders with a range of selectivity to human adenosine 2a receptor (hA(2A)R) from ultralow weight fragment library and the public GlaxoSmithKline (GSK) kinase library. SPR campaigns are highly effective chemical filters for screening small building block fragments that can be used to enable drug discovery programs.
ACS MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Biochemistry & Molecular Biology
Alan Stampini Benhame de Castro, Hauster Maximiler Campos de Paula, Yara Luiza Coelho, Eliara Acipreste Hudson, Ana Clarissa S. Pires, Luis Henrique M. da Silva
Summary: Understanding nonionic surfactant-protein interactions is crucial for both technological and scientific purposes, yet there is a lack of kinetic data. By using surface plasmon resonance (SPR), this study investigated the kinetic and thermodynamic parameters of bovine lactoferrin-Brij58 interactions at different temperatures under physiological conditions. The results showed that the adsorption process was accelerated with increasing temperature, leading to a more thermodynamically stable complex formation. The energetic parameters indicated that the potential energy barrier for complex formation primarily arises from the reduction in system entropy.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Review
Pharmacology & Pharmacy
Kate F. Byrne, Ajay Pal, James F. Curtin, John C. Stephens, Gemma K. Kinsella
Summary: The focus of the review is on G-protein-coupled receptor (GPCR) targets, with chemokine, cannabinoid, and dopamine receptors showing promise. Further research is needed on potential targets such as MC4R, adhesion receptors, LPA, and Smo receptors to develop new drug-screening strategies for safe and effective GBM therapies.
DRUG DISCOVERY TODAY
(2021)
Article
Chemistry, Physical
Jinhua Liu, Xuemiao Zhao, Xinxin Liu, Dong Zhang, Qinglin Wang, Lina Zhao, Shuhong Li, Qiang Shi, Cailong Liu, Bingyuan Zhang, Wenjun Wang, Qingru Wang
Summary: Coupled plasmons have been investigated for their potential in enhancing luminescence. In this study, a gap coupled nanostructure consisting of Au nanorods, a space layer, and Ag nanoparticles was designed to enhance the photoluminescence of Eu film. The results showed a maximum enhancement factor of 53.5-fold. The Ag nanoparticles film enhanced the electromagnetic field, while the space layer adjusted the distance to reduce nonradiative energy transfer. The Au nanorods played a dominant role in luminescence enhancement due to their perfect match with the emission spectrum of Eu.
JOURNAL OF ALLOYS AND COMPOUNDS
(2022)
Review
Biochemistry & Molecular Biology
Dekel David, Ziv Bentulila, Merav Tauber, Yair Ben-Chaim
Summary: GPCRs are involved in signal transduction processes, and although they span the cell membrane, they have not been considered to be regulated by membrane potential. Recent studies, however, have shown that several GPCRs are voltage regulated. This review discusses the advances in understanding the voltage dependence of GPCRs, the suggested molecular mechanisms, and the possible physiological roles.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Multidisciplinary
Prashant Donthamsetti, David B. Konrad, Belinda Hetzler, Zhu Fu, Dirk Trauner, Ehud Y. Isacoff
Summary: G protein-coupled receptors (GPCRs) are common drug discovery targets, but the complexity of in vivo receptor activation has hindered drug development. Photopharmacology offers the potential to control drug action using light. Recent advances include a photoswitchable allosteric agonist that selectively activates receptors.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2021)
Review
Pharmacology & Pharmacy
Jeremy Besnard, Philip S. Jones, Andrew L. Hopkins, Andrew D. Pannifer
DRUG DISCOVERY TODAY
(2015)
Article
Infectious Diseases
Alessandra Guidi, Nuha R. Mansour, Ross A. Paveley, Ian M. Carruthers, Jeremy Besnard, Andrew L. Hopkins, Ian H. Gilbert, Quentin D. Bickle
PLOS NEGLECTED TROPICAL DISEASES
(2015)
Review
Chemistry, Medicinal
Iva Navratilova, Andrew L. Hopkins
FUTURE MEDICINAL CHEMISTRY
(2011)
Editorial Material
Multidisciplinary Sciences
Andrew L. Hopkins
Article
Multidisciplinary Sciences
Jeremy Besnard, Gian Filippo Ruda, Vincent Setola, Keren Abecassis, Ramona M. Rodriguiz, Xi-Ping Huang, Suzanne Norval, Maria F. Sassano, Antony I. Shin, Lauren A. Webster, Frederick R. C. Simeons, Laste Stojanovski, Annik Prat, Nabil G. Seidah, Daniel B. Constam, G. Richard Bickerton, Kevin D. Read, William C. Wetsel, Ian H. Gilbert, Bryan L. Roth, Andrew L. Hopkins
Review
Biochemistry & Molecular Biology
Andrew L. Hopkins
NATURE CHEMICAL BIOLOGY
(2008)
Article
Biochemistry & Molecular Biology
Tudor I. Oprea, Cristian G. Bologa, Scott Boyer, Ramona F. Curpan, Robert C. Glen, Andrew L. Hopkins, Christopher A. Lipinski, Garland R. Marshall, Yvonne C. Martin, Liliana Ostopovici-Halip, Gilbert Rishton, Oleg Ursu, Roy J. Vaz, Chris Waller, Herbert Waldmann, Larry A. Sklar
NATURE CHEMICAL BIOLOGY
(2009)
News Item
Biochemistry & Molecular Biology
Andrew L. Hopkins, G. Richard Bickerton
NATURE CHEMICAL BIOLOGY
(2010)
Article
Chemistry, Multidisciplinary
G. Richard Bickerton, Gaia V. Paolini, Jeremy Besnard, Sorel Muresan, Andrew L. Hopkins
Article
Infectious Diseases
Ross A. Paveley, Nuha R. Mansour, Irene Hallyburton, Leo S. Bleicher, Alex E. Benn, Ivana Mikic, Alessandra Guidi, Ian H. Gilbert, Andrew L. Hopkins, Quentin D. Bickle
PLOS NEGLECTED TROPICAL DISEASES
(2012)
Review
Chemistry, Medicinal
Andrew L. Hopkins, G. Richard Bickerton, Ian M. Carruthers, Stephen K. Boyer, Harvey Rubin, John P. Overington
CURRENT TOPICS IN MEDICINAL CHEMISTRY
(2011)