Molecular pharmacology of the onco-TRP channel TRPV6
Channels (Austin). 2023 Dec;17(1):2266669. doi: 10.1080/19336950.2023.2266669. Epub 2023 Oct 15.ABSTRACTTRPV6, a representative of the vanilloid subfamily of TRP channels, serves as the principal calcium uptake channel in the gut. Dysregulation of TRPV6 results in disturbed calcium homeostasis leading to a variety of human diseases, including many forms of cancer. Inhibitors of this oncochannel are therefore particularly needed. In this review, we provide an overview of recent advances in structural pharmacology that uncovered the molecular mechanisms of TRPV6 inhibition by a variety of small molecules, including synthetic...
Source: Channels - October 15, 2023 Category: Molecular Biology Authors: Arthur Neuberger Alexander I Sobolevsky Source Type: research
Type 3 IP3 receptor: Its structure, functions, and related disease implications
Channels (Austin). 2023 Dec;17(1):2267416. doi: 10.1080/19336950.2023.2267416. Epub 2023 Oct 11.ABSTRACTCell-fate decisions depend on the precise and strict regulation of multiple signaling molecules and transcription factors, especially intracellular Ca2+ homeostasis and dynamics. Type 3 inositol 1,4,5-triphosphate receptor (IP3R3) is an a tetrameric channel that can mediate the release of Ca2+ from the endoplasmic reticulum (ER) in response to extracellular stimuli. The gating of IP3R3 is regulated not only by ligands but also by other interacting proteins. To date, extensive research conducted on the basic structure of ...
Source: Channels - October 11, 2023 Category: Molecular Biology Authors: Lvying Wu Jin Chen Source Type: research
Type 3 IP3 receptor: Its structure, functions, and related disease implications
Channels (Austin). 2023 Dec;17(1):2267416. doi: 10.1080/19336950.2023.2267416. Epub 2023 Oct 11.ABSTRACTCell-fate decisions depend on the precise and strict regulation of multiple signaling molecules and transcription factors, especially intracellular Ca2+ homeostasis and dynamics. Type 3 inositol 1,4,5-triphosphate receptor (IP3R3) is an a tetrameric channel that can mediate the release of Ca2+ from the endoplasmic reticulum (ER) in response to extracellular stimuli. The gating of IP3R3 is regulated not only by ligands but also by other interacting proteins. To date, extensive research conducted on the basic structure of ...
Source: Channels - October 11, 2023 Category: Molecular Biology Authors: Lvying Wu Jin Chen Source Type: research
Overlap in synaptic neurological condition susceptibility pathways and the neural pannexin 1 interactome revealed by bioinformatics analyses
Channels (Austin). 2023 Dec;17(1):2253102. doi: 10.1080/19336950.2023.2253102. Epub 2023 Oct 8.ABSTRACTMany neurological conditions exhibit synaptic impairments, suggesting mechanistic convergence. Additionally, the pannexin 1 (PANX1) channel and signaling scaffold is linked to several of these neurological conditions and is an emerging regulator of synaptic development and plasticity; however, its synaptic pathogenic contributions are relatively unexplored. To this end, we explored connections between synaptic neurodevelopmental disorder and neurodegenerative disease susceptibility genes discovered by genome-wide associat...
Source: Channels - October 9, 2023 Category: Molecular Biology Authors: Simona D Frederiksen Leigh E Wicki-Stordeur Leigh Anne Swayne Source Type: research
Overlap in synaptic neurological condition susceptibility pathways and the neural pannexin 1 interactome revealed by bioinformatics analyses
Channels (Austin). 2023 Dec;17(1):2253102. doi: 10.1080/19336950.2023.2253102. Epub 2023 Oct 8.ABSTRACTMany neurological conditions exhibit synaptic impairments, suggesting mechanistic convergence. Additionally, the pannexin 1 (PANX1) channel and signaling scaffold is linked to several of these neurological conditions and is an emerging regulator of synaptic development and plasticity; however, its synaptic pathogenic contributions are relatively unexplored. To this end, we explored connections between synaptic neurodevelopmental disorder and neurodegenerative disease susceptibility genes discovered by genome-wide associat...
Source: Channels - October 9, 2023 Category: Molecular Biology Authors: Simona D Frederiksen Leigh E Wicki-Stordeur Leigh Anne Swayne Source Type: research
Structure of the voltage-gated potassium channel K < sub > V < /sub > 1.3: Insights into the inactivated conformation and binding to therapeutic leads
Channels (Austin). 2023 Dec;17(1):2253104. doi: 10.1080/19336950.2023.2253104.ABSTRACTThe voltage-gated potassium channel KV1.3 is an important therapeutic target for the treatment of autoimmune and neuroinflammatory diseases. The recent structures of KV1.3, Shaker-IR (wild-type and inactivating W434F mutant) and an inactivating mutant of rat KV1.2-KV2.1 paddle chimera (KVChim-W362F+S367T+V377T) reveal that the transition of voltage-gated potassium channels from the open-conducting conformation into the non-conducting inactivated conformation involves the rupture of a key intra-subunit hydrogen bond that tethers the select...
Source: Channels - September 11, 2023 Category: Molecular Biology Authors: K George Chandy Karoline Sanches Raymond S Norton Source Type: research
