Results 201 to 210 of about 37,458 (256)

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

Mechanistic Insights into the Adenosine A1 Receptor's Positive Allosteric Modulation for Non-Opioid Analgesics. [PDF]

Cells
Weizmann T, Pearce A, Griffin P, Schild A, Flaßhoff M, Grossenbacher P, Lochner M, Reynolds CA, Ladds G, Deganutti G.   +9 more
europepmc   +1 more source

Flecainide binding dynamics in voltage‐gated sodium channels: A comparative isoform analysis of the state‐dependent block

British Journal of Pharmacology, EarlyView.
Background and Purpose Local anaesthetics and class I anti‐arrhythmic drugs block voltage‐gated Na+ channels, but the molecular basis for the isoform differences in drug sensitivity remains unclear. Understanding these mechanisms is essential for optimizing therapeutic efficacy and safety.
Tatsuo Munakata, Etsuko Kumada, Nao Katayama, Hiroki Nakagawa, Akihiko Sunami   +4 more
wiley   +1 more source

Allosteric Modulation of GCase Enhances Lysosomal Activity and Reduces ER Stress in GCase-Related Disorders. [PDF]

Int J Mol Sci
Fregno I, Pérez-Carmona N, Rudinskiy M, Soldà T, Bergmann TJ, Ruano A, Delgado A, Cubero E, Bellotto M, García-Collazo AM, Molinari M.   +10 more
europepmc   +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

Positive allosteric modulation of emodepside sensitive Brugia malayi SLO-1F and Onchocerca volvulus SLO-1A potassium channels by GoSlo-SR-5-69. [PDF]

PLoS Pathog
McHugh M, Njeshi CN, Smith N, Kashyap SS, Datta R, Sun H, Robertson AP, Martin RJ.   +7 more
europepmc   +1 more source

Allosteric modulation of protein kinase A in individuals affected by NLPD-PKA, a neurodegenerative disease in which the PRKAR1B L50R variant is expressed. [PDF]

FEBS J
Benjamin-Zukerman T, Pane V, Safadi-Safa R, Solomon M, Lev-Ram V, Aboraya M, Dakwar A, Bertinetti D, Hoy A, Mol MO, van Swieten J, Maillard R, Herberg FW, Ilouz R.   +13 more
europepmc   +1 more source

Allosteric modulation of NF1 GAP: Differential distributions of catalytically competent populations in loss-of-function and gain-of-function mutants. [PDF]

Protein Sci
Xu L, Jang H, Nussinov R.
europepmc   +1 more source

mGlu4R, mGlu7R, and mGlu8R allosteric modulation for treating acute and chronic neurodegenerative disorders. [PDF]

Pharmacol Rep
Domin H, Burnat G.
europepmc   +1 more source

Allosteric modulation of the Lon protease via ssDNA binding and local charge changes. [PDF]

J Biol Chem
Ogdahl JL, Chien P.
europepmc   +1 more source