Results 91 to 100 of about 31,206 (230)

Direct Gαq Gating Is the Sole Mechanism for TRPM8 Inhibition Caused by Bradykinin Receptor Activation

open access: yesCell Reports, 2019
Summary: Activation of Gαq-coupled receptors by inflammatory mediators inhibits cold-sensing TRPM8 channels, aggravating pain and inflammation. Both Gαq and the downstream hydrolysis of phosphatidylinositol 4, 5-bisphosphate (PIP2) inhibit TRPM8. Here, I
Xuming Zhang
doaj   +1 more source

Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt

open access: yesBritish Journal of Pharmacology, EarlyView.
Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown   +2 more
wiley   +1 more source

Growth of the PIP2-rich phase (blue lower patch).

open access: yes, 2012
The color scale shows the gradation of PIP2 content: the color is the relative concentration difference between PIP3 and PIP2 at a given site. The system at initial time is in a uniform PIP3-rich phase (red), apart from an initial PIP2-rich seed germ of ...
Guido Serini (181212)   +4 more
core   +1 more source

Depletion of Cholesterol Reduces ENaC Activity by Decreasing Phosphatidylinositol-4,5-Bisphosphate in Microvilli

open access: yesCellular Physiology and Biochemistry, 2018
Background/Aims: The epithelial sodium channel (ENaC) in cortical collecting duct (CCD) principal cells plays a critical role in regulating systemic blood pressure.
Yu-Jia Zhai   +11 more
doaj   +1 more source

Natural product‐derived TRPM7 channel inhibitors in neurological injury: Mechanisms, pharmacological potential and translational challenges

open access: yesBritish Journal of Pharmacology, EarlyView.
Disruption of intracellular ionic homeostasis is a convergent pathological feature across diverse neurological injuries and disorders, including ischaemic and haemorrhagic stroke, hypoxic–ischaemic brain injury, traumatic brain injury, epilepsy and brain tumour.
Xinyang Zhang   +5 more
wiley   +1 more source

Fixation-induced cell blebbing on spread cells inversely correlates with phosphatidylinositol 4,5-bisphosphate level in the plasma membrane

open access: yesFEBS Open Bio, 2014
While most attention has been focused on physiologically generated blebs, the molecular mechanisms for fixation-induced cell blebbing are less investigated. We show that protein-fixing (e.g. aldehydes and picric acid) but not lipid-stabilizing (e.g. OsO4
Siyuan Zhao   +5 more
doaj   +1 more source

Effect of PIP2 and phosphorylation on dimerization.

open access: yes, 2023
(A) Gel fractionation of purified Merlin-NL in the absence (black circles) or presence (grey circles) of 200 μM PIP2-DiC8. (B) An image of the dimerization assay using 100 nM purified Merlin-GFP and Merlin-NL incubated with increasing concentrations of ...
Nancy Ratner (375065)   +4 more
core   +1 more source

MyD88‐Family Adaptors: Compartmentalised Signalling and Non‐Immune Functions

open access: yesImmunology, EarlyView.
MyD88‐family adaptors coordinate receptor‐ and compartment‐specific innate immune signalling across plasma membrane and endosomal pathways. At the plasma membrane, TIRAP/MAL supports MyD88‐dependent signalling downstream of TLR2 and TLR4, whereas endosomal TLR7, TLR8 and TLR9 recruit MyD88 directly.
Seshu Vardhan Pothabathula   +6 more
wiley   +1 more source

TMEM16A channel signalling microdomains in the regulation of vascular function

open access: yesThe Journal of Physiology, EarlyView.
Abstract figure legend Schematic representation of TMEM16A channel signalling microdomains. Calcium influx or calcium release from the endoplasmic/sarcoplasmic reticulum (ER/SR) activates TMEM16A channels through interactions with regulatory proteins in vascular smooth muscle cells or endothelial cells. TMEM16A channel activation drives chloride efflux,
Fênix Araujo, Swapnil K. Sonkusare
wiley   +1 more source

How cholesterol regulates endothelial biomechanics

open access: yesFrontiers in Physiology, 2012
As endothelial cells form the barrier between blood flow and surrounding tissue, many of their functions depend on mechanical integrity, in particular that of the plasma membrane.
Zhongkui eHong   +6 more
doaj   +1 more source

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