Results 231 to 240 of about 67,162 (289)

The potential for biased signalling in the P2Y receptor family of GPCRs

British Journal of Pharmacology, EarlyView.
The purinergic receptor family is primarily activated by nucleotides, and contains members of both the G protein coupled‐receptor (GPCR) superfamily (P1 and P2Y) and ligand‐gated ion channels (P2X). The P2Y receptors are widely expressed in the human body, and given the ubiquitous nature of nucleotides, purinergic signalling is involved with a plethora
Claudia M. Sisk, Simon Pitchford, Graham Ladds   +2 more
wiley   +1 more source

The mechanism of allosteric regulation of calcium-independent phospholipase A₂ by ATP and calmodulin binding to the ankyrin domain. [PDF]

Proc Natl Acad Sci U S A
Mouchlis VD, Hsu YH, Hayashi D, Cao J, Li S, McCammon JA, Dennis EA.   +6 more
europepmc   +1 more source

An intracellular recombinant single‐chain variable antibody fragment as a new class of phosphodiesterase type 5 inhibitors

British Journal of Pharmacology, EarlyView.
Background and Purpose Cyclic guanosine monophosphate (cGMP) is a ubiquitous second messenger involved in human (patho‐)physiology. Phosphodiesterase 5 (PDE5) is a major cGMP hydrolyzing enzyme in many cell types including vascular smooth muscle cells (VSMCs). Several highly selective PDE5 inhibitors are in clinical use. However, there are currently no
Kürsat Kirkgöz, Sophie Sprenger, Olga Schweigert, Sanika Mohagaonkar, Matti Walsdorff, Tanja Zeller, Filip Berisha, Viacheslav O. Nikolaev, Sergei D. Rybalkin   +8 more
wiley   +1 more source

Novel approaches for drug development against chronic primary pain: A systematic review

British Journal of Pharmacology, EarlyView.
Abstract Chronic primary pain (CPP) persisting for more than 3 months, associated with significant emotional distress without any known underlying cause, is an unmet medical need. Traditional or adjuvant analgesics do not provide satisfactory pain relief for a great proportion of these patients.
Valéria Tékus, Éva Borbély, Andreas Goebel, Ralf Baron, Zsófia Hajna, Zsuzsanna Helyes   +5 more
wiley   +1 more source

Sodium butyrate ameliorates renal tubular lipid accumulation through a protein phosphatase 2A/transcription factor EB axis in diabetic nephropathy

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Extensive evidence indicates that lipid accumulation causes renal tubular injury, which further contributes to diabetic nephropathy (DN) progression. Short‐chain fatty acids (SCFAs) play an important role in the maintenance of cellular metabolic health.
Jiayin Tao, Sinan Ai, Yaoxian Wang, Yuning Liu, Jingwei Zhou, Qingqing Liu, Xu Wang, Danting Li, Xin Li, Lin Wang, Jinyi Hou, Liang Peng, Zhen Wang   +12 more
wiley   +1 more source

Molecular basis for a pore block of Tentonin 3 expressed in HEK293 cells by a conopeptide, NMB‐1

British Journal of Pharmacology, EarlyView.
Background and Purpose Tentonin 3 (TTN3/TMEM150C) is a mechanosensitive ion channel that plays critical roles in mechanotransduction processes. TTN3 forms a tetramer with a predicted rectangular shape and a central pore. A conotoxin ρ‐TIA and its synthetic analog, noxious mechanosensation blocker 1 (NMB‐1), were initially developed to inhibit slowly ...
Sujin Lim, Junhyuk Woo, Sungmin Pak, Joonho Paik, Gyu‐Sang Hong, Ji Hun Wi, Sanghee Lee, Cristina Fenollar‐Ferrer, Kyungreem Han, Young Kee Shin, Uhtaek Oh   +10 more
wiley   +1 more source

Purine nucleosides replace cAMP in allosteric regulation of PKA in trypanosomatid pathogens. [PDF]

Elife
Ober VT, Githure GB, Volpato Santos Y, Becker S, Moya Munoz G, Basquin J, Schwede F, Lorentzen E, Boshart M.   +8 more
europepmc   +1 more source

Evaluation of preclinical antipsychotic models used to support first‐in‐human clinical trials

British Journal of Pharmacology, EarlyView.
Abstract Schizophrenia is regarded as a complex and heterogeneous psychiatric disorder, characterised by diverse symptoms and comorbidities, which complicate both clinical management and drug development. Current pharmacological treatment, primarily based on dopamine D2 receptor antagonism or partial agonism, which has not markedly progressed since the
Thi Viet Ha Nguyen, Declan P. McKernan, John P. Kelly   +2 more
wiley   +1 more source

A PK/PD study on antihyperalgesia by an α2/3‐GABAA receptor PAM in mice: Lack of tolerance liability and potential involvement of γ1‐GABAA receptors

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose GABAA receptors (GABAARs) are heteropentameric ion channels that control almost all CNS functions, including spinal nociception. Most GABAARs contain a γ2 subunit but differ in their α and β subunit composition. TPA023B is an α2/α3 subtype selective, non‐sedative, positive allosteric modulator (PAM) with antihyperalgesic
Elena Neumann, Mariana O. Popa, Karen T. Elvers, Misa Oyama, Daniel Ulrich, Marcus Hanley, Gui Jie Feng, Thomas Hathaway, William T. Ralvenius, Thomas Grampp, Dietmar Benke, John R. Atack, Hanns Ulrich Zeilhofer   +12 more
wiley   +1 more source