Article
Immunology
Thauane Silva, Jairo R. Temerozo, Gabriele do Vale, Andre C. Ferreira, Vinicius Cardoso Soares, Suelen Silva Gomes Dias, Gabriela Sardella, Dumith Chequer Bou-Habib, Marilda Siqueira, Thiago Moreno L. Souza, Milene Miranda
Summary: This study found that ligands of the CCR5 receptor can inhibit IAV replication by significantly increasing SAMHD1 levels during the course of IAV infection, providing a new perspective on combating viral replication.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Annemiek Dickhout, Dawid M. Kaczor, Alexandra C. A. Heinzmann, Sanne L. N. Brouns, Johan W. M. Heemskerk, Marc A. M. J. van Zandvoort, Rory R. Koenen
Summary: After deposition on endothelial cells, CCL5 and CXCL4 are rapidly and actively internalized by the cells, primarily depending on dynamin, clathrin, and G protein-coupled receptors. The chemokines seem to be directed towards the nucleus, with internalization process not impacting leukocyte arrest.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Biotechnology & Applied Microbiology
Renlun Huang, Lang Guo, Menghan Gao, Jing Li, Songtao Xiang
Summary: Prostate cancer (PCa) is the most common cancer of urologic neoplasms, and the CCL5/CCR5 axis plays a significant role in its development, but challenges remain in precision oncology.
ONCOTARGETS AND THERAPY
(2021)
Article
Oncology
Wilfredo Alejandro Gonzalez-Arriagada, Ricardo D. Coletta, Carlo Lozano-Burgos, Cynthia Garcia, Jaime Maripillan, Francisca Alcayaga-Miranda, Bastian Godinez-Pacheco, Sebastian Oyarce-Pezoa, Rene Martinez-Flores, Isaac E. Garcia
Summary: The CCR5/CCL5 axis plays an important role in the behavior of oral cancer, with CCR5 expression associated with clinical stage and metastasis, and CCL5 associated with overall survival. The CCR5 antagonist Maraviroc can inhibit cell proliferation, increase apoptosis, and modify cytoskeletal organization. In vivo studies show that Maraviroc can reduce neck metastasis.
JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Reni Ajoy, Yu-Chun Lo, Man-Hau Ho, You-Yin Chen, Yun Wang, Yuan-Hao Chen, Chiu Jing-Yuan, Chun Austin Changou, Yuan-Chin Hsiung, Hui-Min Chen, Tzu-Hao Chang, Cheng-Yang Lee, Yung-Hsiao Chiang, Wen-Chang Chang, Barry Hoffer, Szu-Yi Chou
Summary: In addition to its neuroinflammatory functions, chemokine CCL5 also exhibits strong neurotrophic properties. CCL5 plays a critical role in promoting hippocampal glucoregulatory efficiency, which in turn enhances synaptic plasticity and memory and cognition functions. CCL5's actions on glucose aerobic metabolism are essential for mitochondrial function, contributing to hippocampal spine and synapse formation, ultimately improving learning and memory.
MOLECULAR PSYCHIATRY
(2021)
Article
Biology
Magdalena Makarewicz-Wujec, Jan Henzel, Mariusz Kruk, Cezary Kepka, Lukasz Wardziak, Piotr Trochimiuk, Andrzej Parzonko, Marcin Demkow, Zofia Dzielinska, Malgorzata Kozlowska-Wojciechowska
Summary: The study found that the DASH diet can lower the levels of inflammatory markers, which may have potential benefits for patients with atherosclerosis.
Article
Oncology
Karen J. Dunbar, Tatiana A. Karakasheva, Qiaosi Tang, Gizem Efe, Eric W. Lin, Michael Harris, Varun Sahu, Uma M. Sachdeva, Jianhua Hu, Andres J. Klein-Szanto, Brian Henick, Hiroshi Nakagawa, Anil K. Rustgi, J. Alan Diehl
Summary: Cancer-associated fibroblasts (CAF) play a role in promoting tumor growth, metastasis, and therapeutic resistance, and their communication with esophageal squamous cell carcinoma (ESCC) tumor cells is mediated by the secreted factor CC motif chemokine ligand 5 (CCL5). Loss of tumor-derived CCL5 reduces ESCC cell proliferation and the recruitment of CAFs to xenograft tumors, and CCR5 inhibition with Maraviroc mimics these effects. High CCL5 or CCR5 expression is associated with worse prognosis in low-grade esophageal carcinomas.
MOLECULAR CANCER RESEARCH
(2023)
Article
Gastroenterology & Hepatology
Jiaqi Yang, David Sontag, Yuewen Gong, Gerald Y. Minuk
Summary: The study found different CCR expression profiles in intrahepatic and extrahepatic cholangiocarcinoma cells, with CCR5 antagonists inhibiting tumor cell aggressiveness and CCR5 agonists increasing cell proliferation and invasion in specific cell types.
ANNALS OF HEPATOLOGY
(2021)
Article
Multidisciplinary Sciences
Yanchun Huang, Lijuan Wu, Yong Sun, Jiwen Li, Nan Mao, Yeqing Yang, Ming Zhao, Sichong Ren
Summary: This study conducted a comprehensive pan-cancer analysis to explore the value of CCL5 in patient prognosis. The results showed that CCL5 was overexpressed in most tumors and significantly associated with clinical prognosis in 10 out of 33 types of tumors. CCL5 was found to be related to tumor mutational burden, DNA methylation, immune infiltration, immune checkpoints, and cytokine signaling, indicating its potential role in tumor pathogenesis and prognosis.
Article
Biochemistry & Molecular Biology
Anju Krishnan Anitha, Pratibha Narayanan, Neethu Ajayakumar, Krishnankutty Chandrika Sivakumar, Kesavakurup Santhosh Kumar
Summary: This study designed and generated peptide ligands targeting CCR5, which showed significant CCR5 specificity and did not mediate migration of responsive cells.
JOURNAL OF BIOCHEMISTRY
(2022)
Article
Immunology
Qi Tian, Yina Li, Shi Feng, Chengli Liu, Yujia Guo, Guijun Wang, Heng Wei, Zhibiao Chen, Lijuan Gu, Mingchang Li
Summary: Inhibition of CCR1 attenuates neuroinflammation after subarachnoid hemorrhage (SAH) via the JAK2/STAT3 signaling pathway, which may provide a new target for the treatment of SAH.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2023)
Article
Pharmacology & Pharmacy
Weiwei Yu, Ting Ye, Jie Ding, Yi Huang, Yang Peng, Qin Xia, Zhang Cuntai
Summary: The study found that the expression of CCL3 is increased in COPD, causing damage to TJs through CCR5, while miR-4456 can suppress the effect of CCL3 on TJs by binding to the 3'-UTR of CCL3, suggesting that the miR-4456/CCL3/CCR5 pathway could be a potential target for COPD treatment.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Chemistry, Medicinal
Boshi Huang, Huiqun Wang, Yi Zheng, Mengchu Li, Guifeng Kang, Victor Barreto-de-Souza, Nima Nassehi, Pamela E. Knapp, Dana E. Selley, Kurt F. Hauser, Yan Zhang
Summary: The bivalent ligand VZMC013 targets the MOR and CCR5 receptors, showing nanomolar binding affinity and improved anti-HIV-1 activity. It inhibits viral infection in cells expressing both receptors, and has a concentration-dependent inhibition of HIV-1 entry in PBMC cells, particularly in the presence of opioids.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Biology
Pandian Sokkar, Mirja Harms, Christina Stuerzel, Andrea Gilg, Goenuel Kizilsavas, Martina Raasholm, Nico Preising, Manfred Wagner, Frank Kirchhoff, Ludger Staendker, Gilbert Weidinger, Benjamin Mayer, Jan Muench, Elsa Sanchez-Garcia
Summary: The research identified the key interaction motifs of EPI-X4 with CXCR4, explaining its receptor antagonization. Subsequently, shortened derivatives of EPI-X4 with optimized receptor antagonizing properties were developed as new leads for CXCR4 inhibitors.
COMMUNICATIONS BIOLOGY
(2021)
Article
Biology
Fanny Momboisse, Giacomo Nardi, Philippe Colin, Melanie Hery, Nelia Cordeiro, Simon Blachier, Olivier Schwartz, Fernando Arenzana-Seisdedos, Nathalie Sauvonnet, Jean-Christophe Olivio-Marin, Bernard Lagane, Thibault Lagache, Anne Brelot
Summary: This study investigated the impact of different states on the biological function and therapeutic targeting of CC chemokine receptor 5 (CCR5). The researchers used microscopy and statistical methods to track and classify the motion of different receptor subpopulations. The results showed that CCR5 exists in various ligand-free forms, stabilized by different ligands. Agonist stimulation restricted the mobility of CCR5 and led to its clustering, while inverse agonist stimulation had the opposite effect. The study also demonstrated the importance of CCR5 dimerization in its coupling to G proteins, immobilization and clustering upon activation, and receptor endocytosis.
Article
Cardiac & Cardiovascular Systems
Thomas J. Ford, David Corcoran, Sandosh Padmanabhan, Alisha Aman, Paul Rocchiccioli, Richard Good, Margaret McEntegart, Janet J. Maguire, Stuart Watkins, Hany Eteiba, Aadil Shaukat, Mitchell Lindsay, Keith Robertson, Stuart Hood, Ross McGeoch, Robert McDade, Eric Yii, Naveed Sattar, Li-Yueh Hsu, Andrew E. Arai, Keith G. Oldroyd, Rhian M. Touyz, Anthony P. Davenport, Colin Berry
EUROPEAN HEART JOURNAL
(2020)
Review
Pharmacology & Pharmacy
Steve P. H. Alexander, Jane F. Armstrong, Anthony P. Davenport, Jamie A. Davies, Elena Faccenda, Simon D. Harding, Francesca Levi-Schaffer, Janet J. Maguire, Adam J. Pawson, Christopher Southan, Michael Spedding
BRITISH JOURNAL OF PHARMACOLOGY
(2020)
Review
Biotechnology & Applied Microbiology
Anthony P. Davenport, Conor C. G. Scully, Chris de Graaf, Alastair J. H. Brown, Janet J. Maguire
NATURE REVIEWS DRUG DISCOVERY
(2020)
Letter
Cardiac & Cardiovascular Systems
Emma L. Robinson, Kanar Alkass, Olaf Bergmann, Janet J. Maguire, H. Llewelyn Roderick, Anthony P. Davenport
JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY
(2020)
Article
Pharmacology & Pharmacy
Stephen P. H. Alexander, Arthur Christopoulos, Anthony P. Davenport, Eamonn Kelly, Alistair Mathie, John A. Peters, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Adam J. Pawson, Christopher Southan, Jamie A. Davies, Maria Pia Abbracchio, Wayne Alexander, Khaled Al-hosaini, Magnus Baeck, Nicholas M. Barnes, Ross Bathgate, Jean-Martin Beaulieu, Kenneth E. Bernstein, Bernhard Bettler, Nigel J. M. Birdsall, Victoria Blaho, Francois Boulay, Corinne Bousquet, Hans Braeuner-Osborne, Geoffrey Burnstock, Girolamo Calo, Justo P. Castano, KevinJ Catt, Stefania Ceruti, Paul Chazot, Nan Chiang, Bice Chini, Jerold Chun, Antonia Cianciulli, Olivier Civelli, Lucie H. Clapp, Rejean Couture, Zsolt Csaba, Claes Dahlgren, Gordon Dent, Khuraijam Dhanachandra Singh, Steven D. Douglas, Pascal Dournaud, Satoru Eguchi, Emanuel Escher, Edward J. Filardo, Tung Fong, Marta Fumagalli, Raul R. Gainetdinov, Marc de Gasparo, Craig Gerard, Marvin Gershengorn, Fernand Gobeil, Theodore L. Goodfriend, Cyril Goudet, Karen J. Gregory, Andrew L. Gundlach, Joerg Hamann, Julien Hanson, Richard L. Hauger, Debbie L. Hay, Akos Heinemann, Morley D. Hollenberg, Nicholas D. Holliday, Mastgugu Horiuchi, Daniel Hoyer, Laszlo Hunyady, Ahsan Husain, Adriaan P. IJzerman, Tadashi Inagami, Kenneth A. Jacobson, Robert T. Jensen, Ralf Jockers, Deepa Jonnalagadda, Sadashiva Karnik, Klemens Kaupmann, Jacqueline Kemp, Charles Kennedy, Yasuyuki Kihara, Takio Kitazawa, Pawel Kozielewicz, Hans-Juergen Kreienkamp, Jyrki P. Kukkonen, Tobias Langenhan, Katie Leach, Davide Lecca, John D. Lee, Susan E. Leeman, Jerome Leprince, Xaria X. Li, Tom Lloyd Williams, Stephen J. Lolait, Amelie Lupp, Robyn Macrae, Janet Maguire, Jean Mazella, Craig A. McArdle, Shlomo Melmed, Martin C. Michel, Laurence J. Miller, Vincenzo Mitolo, Bernard Mouillac, Christa E. Mueller, Philip Murphy, Jean-Louis Nahon, Tony Ngo, Xavier Norel, Duuamene Nyimanu, Anne-Marie Ocarroll, Stefan Offermanns, Maria Antonietta Panaro, Marc Parmentier, Roger G. Pertwee, Jean-Philippe Pin, Eric R. Prossnitz, Mark Quinn, Rithwik Ramachandran, Manisha Ray, Rainer K. Reinscheid, Philippe Rondard, G. Enrico Rovati, Chiara Ruzza, Gareth J. Sanger, Torsten Schoeneberg, Gunnar Schulte, Stefan Schulz, Deborah L. Segaloff, Charles N. Serhan, Leigh A. Stoddart, Yukihiko Sugimoto, Roger Summers, Valerie P. Tan, David Thal, Walter (Wally) Thomas, PieterB M. W. M. Timmermans, Kalyan Tirupula, Giovanni Tulipano, Hamiyet Unal, Thomas Unger, Celine Valant, Patrick Vanderheyden, David Vaudry, Hubert Vaudry, Jean-Pierre Vilardaga, Christopher S. Walker, Ji Ming Wang, Donald T. Ward, Hans-Juergen Wester, Gary B. Willars, Trent M. Woodruff, Chengcan Yao, Richard D. Ye
Summary: The Concise Guide to PHARMACOLOGY 2021/22 presents concise overviews of nearly 1900 human drug targets with an emphasis on selective pharmacology, along with links to a more detailed knowledgebase. It serves as a permanent, citable record for researchers, providing useful information in the field of pharmacology.
BRITISH JOURNAL OF PHARMACOLOGY
(2021)
Review
Urology & Nephrology
Fiona A. Chapman, Duuamene Nyimanu, Janet J. Maguire, Anthony P. Davenport, David E. Newby, Neeraj Dhaun
Summary: The apelin system is emerging as a potential therapeutic target for chronic kidney disease, with beneficial effects on kidney function and cardiovascular health in patients with kidney disease.
NATURE REVIEWS NEPHROLOGY
(2021)
Article
Biology
Thomas L. Williams, Maria T. Colzani, Robyn G. C. Macrae, Emma L. Robinson, Stuart Bloor, Edward J. D. Greenwood, Jun Ru Zhan, Gregory Strachan, Rhoda E. Kuc, Duuamene Nyimanu, Janet J. Maguire, Paul J. Lehner, Sanjay Sinha, Anthony P. Davenport
Summary: Patients with cardiovascular comorbidities are more vulnerable to severe infection with SARS-CoV-2, which can directly harm cardiovascular tissue. Researchers have developed a screening platform using human embryonic stem cell-derived cardiomyocytes to identify new inhibitors of SARS-CoV-2 infection, with benztropine and DX600 found as potential inhibitors. This discovery of new medicines is crucial for protecting the heart in SARS-CoV-2 patients and those who cannot be vaccinated.
COMMUNICATIONS BIOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Simon D. Harding, Jane F. Armstrong, Elena Faccenda, Christopher Southan, Stephen P. H. Alexander, Anthony P. Davenport, Adam J. Pawson, Michael Spedding, Jamie A. Davies
Summary: The IUPHAR/BPS Guide to PHARMACOLOGY has expanded its content in the past two years, focusing on infection, malaria, and antibiotic resistance. It has included a new family of Coronavirus proteins and collaborated with Medicines for Malaria Venture and AntibioticDB to enhance coverage of malaria pharmacology and antibacterials.
NUCLEIC ACIDS RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Duuamene Nyimanu, Richard G. Kay, Rhoda E. Kuc, Alastair J. H. Brown, Fiona M. Gribble, Janet J. Maguire, Anthony P. Davenport
Summary: By developing an LC-MS/MS assay to identify ELA-32 metabolites, it was found that ELA-32 has a relatively long half-life in the human body, and a potentially more stable ELA-16 fragment was identified, suggesting it could be a novel template for drug development.
Article
Cardiac & Cardiovascular Systems
George R. Abraham, Duuamene Nyimanu, Rhoda E. Kuc, Janet J. Maguire, Anthony P. Davenport, Stephen P. Hoole
Summary: Coronary microvascular dysfunction (CMD) can complicate successful percutaneous coronary intervention (PCI). This study found that the levels of endothelin-1 (ET-1) and its precursor peptide Big ET-1 significantly increased after PCI, and the increased ET-1 trans-myocardial extraction was correlated with increased microcirculatory resistance.
JOURNAL OF INTERVENTIONAL CARDIOLOGY
(2022)
Meeting Abstract
Cardiac & Cardiovascular Systems
Robyn Macrae, William G. Bernard, Rhoda E. Kuc, Maria T. Colzani, Thomas Williams, Duuamene Nyimanu, Janet Maguire, Sanjay Sinha, Anthony P. Davenport