Results 221 to 230 of about 107,657 (326)

Formulation and characterization of CMPI nanoparticles for enhanced targeting of brain nicotinic receptors by positive allosteric modulator. [PDF]

Sci Rep
Aly R, Sulthana S, Beaudoin R, Hamouda AK, Aryal S.   +4 more
europepmc   +1 more source

Cancer pain: current practice and emerging targets

British Journal of Pharmacology, EarlyView.
Cancer pain (CP) arises from a complex interplay between the tumour and its microenvironment. Many patients experience a mixed pain phenotype that encompasses nociceptive, neuropathic and neuroinflammatory mechanisms, and vary across tumour type and disease stage. Despite decades of intensive research, the mainstay of cancer pain treatment is still non‐
Yi Ye, Marcin Chwistek, Zhiting Gong, Vanessa Uzonwanne, Xiaojie Shi, Arpad Szallasi   +5 more
wiley   +1 more source

Targeting the noncatalytic activity of GSK3β modulates neuronal excitability in medium spiny neurons via Nav1.6 interactions

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose Kinases phosphorylate ion channels, but their noncatalytic roles via protein–protein interactions (PPI) are less understood. Here, we identified the peptidomimetic ZL141 to characterize the PPI between GSK3β and Nav1.6, revealing a noncatalytic role for GSK3β in regulating Nav1.6 currents and neuronal excitability ...
Aditya K. Singh, Zahra Haghighijoo, Akanksha Gurtu, Nolan M. Dvorak, Timothy J. Baumgartner, Nana A. Goode, Jully Singh, Matteo Bernabucci, Adam T. Szafran, Michael J. Bolt, Michael A. Mancini, Natalie M. Dvorak, Marijn Lijffijt, Zhiqing Liu, Yu Xue, Alyssa K. Thomas, Alejandro Villasante‐Tezanos, Balaji Krishnan, Jia Zhou, Fernanda Laezza   +19 more
wiley   +1 more source

Mu Opioid Receptor Positive Allosteric Modulator BMS-986122 Confers Agonist-Dependent G Protein Subtype Signaling Bias. [PDF]

Biochemistry
Grieble GM, Knapp BI, Bidlack JM.
europepmc   +1 more source

Cannabinoid and adenosine A2A receptor crosstalk regulates postnatal and adult hippocampal neurogenesis

British Journal of Pharmacology, EarlyView.
Background and purpose Adult neurogenesis is a tightly regulated process affected by both cannabinoid receptors (CB1 and CB2) and adenosine 2A (A2A) receptors, both of which modulate neural progenitor cell activity. While emerging evidence suggests an interaction between these neuromodulatory systems, the extent and mechanism of their interplay in ...
Rui S. Rodrigues, Adam Armada‐Moreira, Laura Gómez‐Acero, Filipa F. Ribeiro, Francisco M. Mouro, Ana M. Sebastião, Francisco Ciruela, Ester Aso, Sara Xapelli   +8 more
wiley   +1 more source

Further In Vitro and Ex Vivo Pharmacological and Kinetic Characterizations of CCF219B: A Positive Allosteric Modulator of the α_1A-Adrenergic Receptor. [PDF]

Pharmaceuticals (Basel)
Papay RS, Perez DM.
europepmc   +1 more source

Prevention of microglial activation and postoperative cognitive deficits by positive allosteric modulation of α5‐GABAA receptors

British Journal of Pharmacology, EarlyView.
Background and Purpose Long‐lasting cognitive deficits after surgery in aged individuals, referred to as perioperative neurocognitive disorder (NCD), are a significant public health concern. Such postoperative cognitive deficits are dependent on the presence of microglia in the brain, which, when activated, trigger neuroinflammation.
Jinrui Lyu, Rajasekar Nagarajan, Dishary Sharmin, Prithu Mondal, Maltesh Kambali, Muxiao Wang, Jinyan Zhou, Makoto Inoue, James M. Cook, Uwe Rudolph   +9 more
wiley   +1 more source

Positive allosteric modulator of GLT-1 reduces methamphetamine hyperlocomotion, sensitization and conditioned place preference in mice. [PDF]

Neurosci Res
Mokkarala P, Wiah S, Unterwald EM, Shi X, Stern DR, Fontana ACK, Salvino JM, Rawls SM.   +7 more
europepmc   +1 more source

Agonist‐specific conformational dynamics at the β2‐adrenoceptor dictate allosteric modulation of Gαs signalling and bronchodilation

British Journal of Pharmacology, EarlyView.
Abstract Background and Purpose β2‐adrenoceptor (β2AR) agonists are the cornerstone of asthma therapy and promote bronchodilation through Gαs signalling in airway smooth muscle (ASM), but their efficacy is limited by β‐arrestin‐mediated β2AR desensitization.
Sushrut D. Shah, Joshua Richard, Suvankar Ghosh, Jillian Jerwick, Joice T. Gavali, Raymond B. Penn, Alexander D. MacKerell Jr, Deepak A. Deshpande   +7 more
wiley   +1 more source

Multivalent antibody‐based conjugates as new tools for tailored modulation of G protein–coupled receptors

British Journal of Pharmacology, EarlyView.
The G protein–coupled receptor (GPCR) superfamily consists of the most common targets of approved drugs. Targeting GPCRs offers appealing avenues for therapeutic development. Antibodies and their fragments, such as single‐domain antibodies (VHHs or nanobodies), have emerged as useful alternatives to small molecule pharmacophores as building blocks in ...
Shivani Sachdev, Ross W. Cheloha
wiley   +1 more source