Defining the polycystin pharmacophore through high-throughput screening and computational biophysics. [PDF]
An unbiased high throughput electrophysiology screen identifies potent PKD2L1 channel inhibitors with divergent chemical composition that bind to pore fenestration receptors and stabilise their inactivated state. Abstract Background and Purpose Polycystins (PKD2, PKD2L1) are voltage‐gated and Ca2+‐modulated members of the TRP family of ion channels ...
Guadarrama E, Vanoye CG, DeCaen PG.
europepmc +2 more sources
Transient Receptor Potential Channels as Key Regulators of Neuroinflammation in Neurological Disorders: Mechanistic Insights, Therapeutic Potentials, and Future Directions. [PDF]
This study elucidates the central role of transient receptor potential (TRP) channels in driving neuroinflammation across neurological disorders. Acting as critical molecular sensors on neurons and glial cells, TRP channels' activation initiates downstream pathways that promote the release of proinflammatory cytokines, a pathological mechanism in ...
Guo D +8 more
europepmc +2 more sources
Nonsteroidal Anti-Inflammatory Drugs as Modulators of Cation Channels: Fenamates Repurposing in Channelopathies. [PDF]
Beyond their established role as nonsteroidal anti‐inflammatory drugs (NSAIDs), fenamates (niflumic, flufenamic, mefenamic, meclofenamic, and tolfenamic acids) have recently been identified as modulators of cationic ion channels. This review highlights their differential effects on ion channel activity and explores their potential for repurposing in ...
Laghetti P +4 more
europepmc +2 more sources
Calcium signaling in oomycetes: an evolutionary perspective [PDF]
Oomycetes are a family of eukaryotic microbes that superficially resemble fungi, but which are phylogenetically distinct from them. These organisms cause major global economic losses to agriculture and fisheries, with representative pathogens being ...
Mackrill, John J., Zheng, Limian
core +4 more sources
Emerging Roles of L-Type Voltage-Gated and Other Calcium Channels in T Lymphocytes [PDF]
In T lymphocytes, calcium ion controls a variety of biological processes including development, survival, proliferation, and effector functions. These distinct and specific roles are regulated by different calcium signals, which are generated by various ...
Abdallah eBadou +4 more
core +8 more sources
A novel ion channel formed by interaction of TRPML3 with TRPV5. [PDF]
TRPML3 and TRPV5 are members of the mucolipin (TRPML) and TRPV subfamilies of transient receptor potential (TRP) cation channels. Based on sequence similarities of the pore forming regions and on structure-function evidence, we hypothesized that the pore
Becker, Lars +4 more
core +7 more sources
Apoptosis, a genetically programmed cell death, allows for homeostasis and tissue remodelling during development of all multi-cellular organisms. Phagocytes swiftly recognize, engulf and digest apoptotic cells. Yet, to date the molecular mechanisms underlying this phagocytic process are still poorly understood.
Emeline Van Goethem +4 more
openaire +4 more sources
TRPV4, TRPC1, and TRPP2 assemble to form a flow-sensitive heteromeric channel [PDF]
Transient receptor potential (TRP) channels, a superfamily of ion channels, can be divided into 7 subfamilies, including TRPV, TRPC, TRPP, and 4 others. Functional TRP channels are tetrameric complexes consisting of 4 pore-forming subunits.
Birnbaumer, Lutz +5 more
core +1 more source
The Concise Guide to PHARMACOLOGY 2015/16:Voltage-gated ion channels [PDF]
The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org),
, +11 more
core +4 more sources
Transient Receptor Potential Cation Channels in Cancer Therapy
In mammals, the transient receptor potential (TRP) channels family consists of six different families, namely TRPC (canonical), TRPV (vanilloid), TRPM (melastatin), TRPML (mucolipin), TRPP (polycystin), and TRPA (ankyrin), that are strictly connected ...
G. Santoni +4 more
semanticscholar +1 more source

