The relationship between apparent potentiation and the magnitude of the control response [0.03%]
控制反应的大小与表观增效的关系
Joe Henry Steinbach,Gustav Akk
Joe Henry Steinbach
The effect of a potentiating drug on ion channel function is typically evaluated by comparing current responses to the control agonist in the presence and absence of the potentiator. Differences in ratios of responses are then taken as proo...
Inhibition of CaV1.4 channels by CaV3 channel antagonists ML218 and Z944 [0.03%]
CaV3通道拮抗剂ML218和Z944对CaV1.4通道的抑制作用
Jinglang Sun,Juan de la Rosa Vázquez,Adriana Hernández-González et al.
Jinglang Sun et al.
Among the three classes of voltage-gated Ca2+ channels (CaV1, CaV2, and CaV3), CaV3 T-type channels are drug targets for disorders, including epilepsy and pain. Antagonists such as Z944 and ML218 are highly selective for CaV3 compared with ...
Godfrey L Smith,David A Eisner
Godfrey L Smith
The presence of significant amounts of the transition metal, manganese, is essential for living cells where it is bound to some intracellular enzymes. The free (i.e., unbound) Mn2+ concentration in both extracellular and intracellular space...
A critical residue mediates proper assembly and gating of GIRK2 channels [0.03%]
一个关键性残基调控GIRK2通道的正确装配和闸门功能
Ha Nguyen,Jonathan Mount,Keino Hutchinson et al.
Ha Nguyen et al.
G protein-gated inwardly rectifying potassium (GIRK) channels mediate membrane hyperpolarization in response to G protein-coupled receptor activation and are critical for regulating neuronal excitability. The membrane phospholipid phosphati...
Exploring voltage-gated sodium channel conformations and protein-protein interactions using AlphaFold2 [0.03%]
利用AlphaFold2探索电压门控钠通道构象和蛋白质-蛋白质相互作用
Diego Lopez-Mateos,Kush Narang,Vladimir Yarov-Yarovoy
Diego Lopez-Mateos
Voltage-gated sodium (NaV) channels are vital regulators of electrical activity in excitable cells. Given their importance in physiology, NaV channels are key therapeutic targets for treating numerous conditions, yet developing subtype-sele...
Ben Short
Ben Short
JGP study (De Giorgis et al. https://doi.org/10.1084/jgp.202413739) reveals that the auxiliary Cavβ3 subunit regulates the cardiac calcium channel Cav1.2 by modulating the two-step activation of VSD II. ...
Allosteric coupling of RyR calcium channels: Is it relevant to the [patho]physiology of heart and muscle? [0.03%]
骨骼肌和心肌ryanodine受体钙释放通道的别构耦联：其生理或病理生理意义何在？
Eduardo Rios
Eduardo Rios
This study reveals an examination of the phenomenon of coupled gating between ryanodine receptors, the Ca2+ channels of the sarcoplasmic reticulum of skeletal and cardiac muscle, essential for the execution of contraction upon electrical ex...
On the mechanism of K+ transport through the inter-subunit tunnel of KdpFABC [0.03%]
KdpFABC亚基间隧道中介导钾离子转运的机制研究
Hridya Valia Madapally,Adel Hussein,Martin Wazar Eriksen et al.
Hridya Valia Madapally et al.
KdpFABC is an ATP-dependent membrane complex that enables prokaryotes to maintain potassium homeostasis under potassium-limited conditions. It features a unique hybrid mechanism combining a channel-like selectivity filter in KdpA with the A...
Jenna L Lin,Baron Chanda
Jenna L Lin
Cyclic nucleotide-binding domain (CNBD) channels are critical components of numerous bioelectrical processes, including cardiac pacemaking, neuronal signaling, phototransduction in the eye, and stomatal regulation in plants. While members o...
Novel binding mode for negative allosteric NMDA receptor modulators [0.03%]
新的阴性变构N-甲基-D天冬氨酸受体调节剂的作用模式
James S Lotti,Jed T Syrenne,Avery J Benton et al.
James S Lotti et al.
NMDA-type ionotropic glutamate receptors mediate excitatory neurotransmission and synaptic plasticity, but aberrant signaling by these receptors is also implicated in brain disorders. Here, we present the binding site and the mechanism of a...