Results 51 to 60 of about 2,691 (151)

Repositioning VU‐0365114 as a novel microtubule‐destabilizing agent for treating cancer and overcoming drug resistance

Molecular Oncology
Microtubule‐targeting agents represent one of the most successful classes of anticancer agents. However, the development of drug resistance and the appearance of adverse effects hamper their clinical implementation.
Yao‐Yu Hsieh, Jia‐Ling Du, Pei‐Ming Yang   +2 more
doaj   +1 more source

Deletion of the M ₅ muscarinic acetylcholine receptor attenuates morphine reinforcement and withdrawal but not morphine analgesia [PDF]

Proceedings of the National Academy of Sciences, 2002
Little is known about the physiological roles of the M 5 muscarinic receptor, the last member of the muscarinic receptor family (M 1 –M 5 ) to be cloned. In the brain, the M 5 receptor subtype is preferentially expressed by dopaminergic neurons ...
Anthony S, Basile, Irina, Fedorova, Agustin, Zapata, Xiaoguang, Liu, Toni, Shippenberg, Alokesh, Duttaroy, Masahisa, Yamada, Jurgen, Wess   +7 more
openaire   +2 more sources

Muscarinic agonist, (±)-quinuclidin-3-yl-(4-fluorophenethyl)(phenyl)carbamate: High affinity, but low subtype selectivity for human M1 – M5 muscarinic acetylcholine receptors [PDF]

Bioorganic & Medicinal Chemistry Letters, 2019
Novel quinuclidinyl N-phenylcarbamate analogs were synthesized, and binding affinities at M1-M5 muscarinic acetylcholine receptor (mAChR) subtypes were determined using Chinese hamster ovary (CHO) cell membranes stably expressing one specific subtype of human mAChR. Although not subtype selective, the lead analog (±)-quinuclidin-3-yl-(4-fluorophenethyl)
Na-Ra Lee, Satheesh Gujarathi, Shobanbabu Bommagani, Kiranbabu Siripurapu, Guangrong Zheng, Linda P. Dwoskin   +5 more
openaire   +2 more sources

The Concise Guide to PHARMACOLOGY 2025/26: G protein‐coupled receptors

British Journal of Pharmacology, Volume 182, Issue S1, Page S24-S151, December 2025.
The Concise Guide to Pharmacology 2025/26 marks the seventh edition in this series of biennial publications in the British Journal of Pharmacology. Presented in landscape format, the guide provides a comparative overview of the pharmacology of drug target families. The concise nature of the Concise Guide refers to the style of presentation, being clear,
Stephen P. H. Alexander, Anthony P. Davenport, Eamonn Kelly, Alasdair J. Gibb, Alistair A. Mathie, Chloe J. Peach, Emma L. Veale, Jane F. Armstrong, Elena Faccenda, Simon D. Harding, Christopher Southan, Jamie A. Davies, Maria Pia Abbracchio, George R. Abraham, Alexander Agoulnik, Wayne Alexander, Khaled Al‐hosaini, Magnus Bäck, Jillian G. Baker, Nicholas M. Barnes, Ross Bathgate, Jean‐Martin Beaulieu, Annette G. Beck‐Sickinger, Maik Behrens, Kirstie A. Bennett, Kenneth E. Bernstein, Bernhard Bettler, Nigel J. M. Birdsall, Victoria A. Blaho, Pascal Bonaventure, Francois Boulay, Corinne Bousquet, Hans Bräuner‐Osborne, Andrew J. Brown, Geoffrey Burnstock, Marta Busnelli, Girolamo Caló, Vanni Caruso, Justo P. Castaño, Kevin J. Catt, Stefania Ceruti, Paul Chazot, Nan Chiang, Bice Chini, Arthur Christopoulos, Jerold Chun, Antonia Cianciulli, Olivier Civelli, Lucie H. Clapp, Réjean Couture, Helen M. Cox, Zsolt Csaba, Claes Dahlgren, Frank M. Dautzenberg, Gordon Dent, Steven D. Douglas, Pascal Dournaud, Margarita L. Dubocovich, Satoru Eguchi, Emanuel Escher, Edward J. Filardo, Tung Fong, Huamei Fu Forsman, Marta Fumagalli, Raul R. Gainetdinov, Michael L. Garelja, Marc de Gasparo, Florence Gbahou, Craig Gerard, Marvin Gershengorn, Michelle Glass, David E. Gloriam, Fernand Gobeil, Theodore L. Goodfriend, Cyril Goudet, Lukas Grätz, Karen J. Gregory, Christian Gruber, Andrew L. Gundlach, Jörg Hamann, Julien Hanson, Deborah S. Hartman, Richard L. Hauger, Debbie L. Hay, Akos Heinemann, Laura Heitman, Deron R. Herr, Morley D. Hollenberg, Nicholas D. Holliday, Birgitte Holst, Mastgugu Horiuchi, Daniel Hoyer, László Hunyady, Ahsan Husain, Adriaan P. IJzerman, Tadashi Inagami, Paul A. Insel, Kenneth A. Jacobson, Laura H. Jacobson, Robert T. Jensen, Ralf Jockers, Deepa Jonnalagadda, Sadashiva Karnik, Klemens Kaupmann, Jacqueline Kemp, Charles Kennedy, Yasuyuki Kihara, Julia Kinsolving, Takio Kitazawa, Pawel Kozielewicz, Hans‐Jürgen Kreienkamp, Jyrki P. Kukkonen, Luxmichan Laishram, Tobias Langenhan, Christopher J. Langmead, Dan Larhammar, Katie Leach, Davide Lecca, John D. Lee, Susan E. Leeman, Jérôme Leprince, Rob Leurs, Xaria X. Li, Ines Liebscher, Stephen J. Lolait, Amelie Lupp, Robyn Macrae, Janet J. Maguire, Davide Malfacini, Maurice Manning, Davide Marangon, Kirill Martemyanov, Jean Mazella, Craig A. McArdle, Shlomo Melmed, Martin C. Michel, Laurence J. Miller, Vincenzo Mitolo, Bernard Mouillac, Christa E. Müller, Philip M. Murphy, Jean‐Louis Nahon, Richard R. Neubig, Tony Ngo, Xavier Norel, Duuamene Nyimanu, Anne‐Marie O’Carroll, Stefan Offermanns, Maria Antonietta Panaro, Marc Parmentier, Nicole Perry‐Hauser, Roger G. Pertwee, Jean‐Philippe Pin, Eric R. Prossnitz, Helena Chengxue Qin, Mark Quinn, Stefano Raffaele, Rithwik Ramachandran, Manisha Ray, Rainer K. Reinscheid, Alejandro Romeral Buzón, Philippe Rondard, Mette M. Rosenkilde, G. Enrico Rovati, Chiara Ruzza, Gareth J. Sanger, Nicole Scholz, Torsten Schöneberg, Gunnar Schulte, Stefan Schulz, Deborah L. Segaloff, Charles N. Serhan, Arun K. Shukla, Khuraijam Dhanachandra Singh, Craig M. Smith, Nicola J. Smith, Claudia Stäubert, Leigh A. Stoddart, Yukihiko Sugimoto, Roger Summers, Valerie P. Tan, David M. Thal, Walter ( Wally) Thomas, Pieter B. M. W. M. Timmermans, Kalyan Tirupula, Lawrence Toll, Giovanni Tulipano, Hamiyet Unal, Thomas Unger, Celine Valant, Patrick Vanderheyden, David Vaudry, Hubert Vaudry, Joseph G. Verbalis, Jean‐Pierre Vilardaga, Christopher S. Walker, Ji Ming Wang, Donald T. Ward, Hans‐Jürgen Wester, Gary B. Willars, Tom Lloyd Williams, Trent M. Woodruff, Huixian Wu, Cheng Yang, Chengcan Yao, Richard D. Ye, Nathan Zaidman   +206 more
wiley   +1 more source

Polypharmacy in mice disrupts left ventricular function and structure and promotes proteome reorganisation in an age‐ and sex‐specific fashion

British Journal of Pharmacology, Volume 182, Issue 19, Page 4625-4646, October 2025.
Background and Purpose Most older people use polypharmacy (≥5 medications), particularly those with cardiovascular disease. The effects of polypharmacy on the cardiovascular system are not well described. We examined the effect of a chronic polypharmacy regimen on left ventricular (LV) function, structure and proteome in young and old mice of both ...
Trang Tran, Kevin Winardi, Scott P. Levick, Alexander Widiapradja, Gizem Gemikonakli, Susan E. Howlett, Matthew J. McKay, Mark P. Molloy, John Mach, Sarah N. Hilmer   +9 more
wiley   +1 more source

GPCR‐G protein signalling and its mutational landscape in cancer—Driver or passenger

British Journal of Pharmacology, Volume 182, Issue 17, Page 3975-3989, September 2025.
G protein‐coupled receptors (GPCRs) play a crucial role in cellular signalling, regulating various physiological processes. Abnormal expression and mutations of GPCRs have been implicated in several types of cancer, influencing tumour initiation, progression and immune response.
Chenlin Feng, Jasper F. Ooms, Erik H. J. Danen, Laura H. Heitman   +3 more
wiley   +1 more source

Light‐Activated Pharmacological Tools for Exploring the Cholinergic System

Medicinal Research Reviews, Volume 45, Issue 4, Page 1251-1274, July 2025.
ABSTRACT Cholinergic transmission plays a critical role in both the central and peripheral nervous systems, affecting processes such as learning, memory, and inflammation. Conventional cholinergic drugs generally suffer from poor selectivity and temporal precision, leading to undesired effects and limited therapeutic efficacy. Photopharmacology aims to
Alessio Colleoni, Giulia Galli, Clelia Dallanoce, Marco De Amici, Pau Gorostiza, Carlo Matera   +5 more
wiley   +1 more source

Towards the convergent therapeutic potential of G protein‐coupled receptors in autism spectrum disorders

British Journal of Pharmacology, Volume 182, Issue 14, Page 3044-3067, July 2025.
Abstract Autism spectrum disorders (ASDs) are diagnosed in 1/100 children worldwide, based on two core symptoms: deficits in social interaction and communication, and stereotyped behaviours. G protein‐coupled receptors (GPCRs) are the largest family of cell‐surface receptors that transduce extracellular signals to convergent intracellular signalling ...
Anil Annamneedi, Caroline Gora, Ana Dudas, Xavier Leray, Véronique Bozon, Pascale Crépieux, Lucie P. Pellissier   +6 more
wiley   +1 more source

G protein‐coupled receptor‐mediated autophagy in health and disease

British Journal of Pharmacology, Volume 182, Issue 14, Page 3151-3162, July 2025.
G protein‐coupled receptors (GPCRs) constitute the largest and most diverse superfamily of mammalian transmembrane proteins. These receptors are involved in a wide range of physiological functions and are targets for more than a third of available drugs in the market. Autophagy is a cellular process involved in degrading damaged proteins and organelles
Devrim Öz‐Arslan, Zeynep Aslıhan Durer, Beki Kan   +2 more
wiley   +1 more source

D-pinitol modulates the anti-emetic effects of aprepitant, domperidone, and ondansetron in chicks

Pharmaceutical Science Advances
Naturally occurring substance, D-pinitol (DPL) belongs to the significant inositol family has numerous pharmacological activity. In this study we evaluated the anti-emetic effect as well as modulation activities of DPL on the recent market drugs ...
Md. Elit Rahman, Md. Anisur Rahman, Salehin Sheikh, Md. Jannatul Islam Polash, Sozoni Khatun, Mst. Sonia Akter Bristi, Md. Showkoth Akbor, Mst. Farjanamul Haque, Mehedi Hasan Bappi, Tohidul Islam Tanim, Siddique Akber Ansari, Irfan Aamer Ansari, Elaine Cristina Pereira Lucetti, Carolina Bandeira Domiciano, Henrique D.M. Coutinho, Muhammad Torequl Islam   +15 more
doaj   +1 more source