Results 161 to 170 of about 3,697 (189)
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Discovery and characterization of novel TRPML1 agonists

Bioorganic and Medicinal Chemistry Letters
Screening a library of >100,000 compounds identified the substituted tetrazole compound 1 as a selective TRPML1 agonist. Both enantiomers of compound 1 were separated and profiled in vitro and in vivo. Their selectivity, ready availability and CNS penetration should enable them to serve as the tool compounds of choice in future TRPML1 channel ...
Duane Burnett   +2 more
exaly   +3 more sources

TRPML1 and TFEB, an Intimate Affair

2022
Ca2+ is a universal second messenger that plays a wide variety of fundamental roles in cellular physiology. Thus, to warrant selective responses and to allow rapid mobilization upon specific stimuli, Ca2+ is accumulated in organelles to keep it at very low levels in the cytoplasm during resting conditions.
openaire   +3 more sources

TRPML1: An Ion Channel in the Lysosome

2014
The first member of the mammalian mucolipin TRP channel subfamily (TRPML1) is a cation-permeable channel that is predominantly localized on the membranes of late endosomes and lysosomes (LELs) in all mammalian cell types. In response to the regulatory changes of LEL-specific phosphoinositides or other cellular cues, TRPML1 may mediate the release of Ca(
Wuyang, Wang   +3 more
openaire   +2 more sources

Lysosomal TRPML1 Channel: Implications in Cardiovascular and Kidney Diseases

2021
Lysosomal ion channels mediate ion flux from lysosomes and regulate membrane potential across the lysosomal membrane, which are essential for lysosome biogenesis, nutrient sensing, lysosome trafficking, lysosome enzyme activity, and cell membrane repair.
Guangbi, Li, Pin-Lan, Li
openaire   +2 more sources

TRPML1-induced autophagy inhibition triggers mitochondrial mediated apoptosis

Cancer Letters, 2022
Previous studies have demonstrated that autophagy tightly regulates apoptosis. However, the underlying mechanism whereby autophagy regulates apoptosis remains unclear. Here, we discover a "autophagy inhibition-mitochondrial turnover disruption-ROS elevation-DNA damage-p53 transactivation-apoptosis" axis that explicates the process of autophagy ...
Yucheng Liu   +8 more
openaire   +2 more sources

TRPML1-/TFEB-Dependent Regulation of Lysosomal Exocytosis

2019
Emerging experimental evidences indicate that the lysosome can trigger a calcium signaling, via TRPML1/calcineurin/TFEB pathway, that promotes lysosomal exocytosis and clearance of lysosomal accumulation in various cellular models of lysosomal storage disorders (LSDs).
Di Paola, Simone, Medina, DL
openaire   +4 more sources

MCOLN1/TRPML1 in the lysosome: a promising target for autophagy modulation in diverse diseases

Autophagy
MCOLN1/TRPML1 is a nonselective cationic channel specifically localized to the late endosome and lysosome. With its property of mediating the release of several divalent cations such as Ca2+, Zn2+ and Fe2+ from the lysosome to the cytosol, MCOLN1 plays a pivotal role in regulating a variety of cellular events including endocytosis, exocytosis ...
Jiansong Qi   +11 more
openaire   +2 more sources

Structural mechanism of allosteric activation of TRPML1 by PI(3,5)P 2 and rapamycin

Proceedings of the National Academy of Sciences of the United States of America, 2022
Ninghai Gan, Yan Han, Youxing Jiang
exaly  

The Regulation of Lysosomal TRPML1 Channel on Insulin Secretion

SSRN Electronic Journal, 2022
Wei Su   +4 more
openaire   +1 more source

HETEROCYCLIC TRPML1 AGONISTS

2021
PEVARELLO PAOLO   +6 more
openaire   +3 more sources

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