Results 121 to 130 of about 209,245 (296)

The alpha-latrotoxin mutant LTXN4C enhances spontaneous and evoked transmitter release in CA3 pyramidal neurons

open access: yes, 2003
Alpha-latrotoxin (LTX) stimulates vesicular exocytosis by at least two mechanisms that include (1) receptor binding-stimulation and (2) membrane pore formation.
Emptage, NJ   +4 more
core  

Unusual accelerated rate of deletions and insertions in toxin genes in the venom glands of the pygmy copperhead (Austrelaps labialis) from kangaroo island

open access: yesBMC Evolutionary Biology, 2008
Background Toxin profiling helps in cataloguing the toxin present in the venom as well as in searching for novel toxins. The former helps in understanding potential pharmacological profile of the venom and evolution of toxins, while the latter ...
Kini R Manjunatha   +3 more
doaj   +1 more source

Longitudinal genome‐wide aneuploidy measurements in circulating cell‐free DNA to predict lack of benefit from pembrolizumab in patients with metastatic urothelial cancer

open access: yesMolecular Oncology, EarlyView.
Many patients with urothelial cancer do not benefit from treatment with pembrolizumab, while at risk of severe side effects. Changes in the levels of circulating tumor DNA early during treatment, measured by a simple and affordable assay that can be easily implemented in the clinic, can be used as a prognostic tool to identify these patients.
Youssra Salhi   +14 more
wiley   +1 more source

A novel quinazolinone insulin receptor inhibitor and its synergy with an EGFR inhibitor in glucose‐driven glioblastoma

open access: yesMolecular Oncology, EarlyView.
The novel styrylquinazolinone‐based molecule W1B effectively suppresses glioblastoma by inhibiting IGF1R and EGFR. In high‐glucose microenvironments driving tumor resistance, W1B acts synergistically with the EGFR inhibitor dacomitinib. This combination safely blocks compensatory survival signaling in zebrafish xenograft models. Showcasing promising in
Patryk Rurka   +9 more
wiley   +1 more source

Pertussis toxin inhibits endothelium-dependent relaxations evoked by fluoride

open access: yes, 1990
Fluoride is a direct activator of G-proteins. In isolated rings of canine coronary artery, fluoride caused relaxation of rings with endothelium, but only slight contraction of rings denuded of endothelium.
Flavahan, NA, Vanhoutte, PM
core   +1 more source

Inhibition of cyclin‐dependent kinases 12/13 using CT7439 as a treatment for colorectal cancer with CDK12 upregulation

open access: yesMolecular Oncology, EarlyView.
The proposed mechanism of action for the CDK12/13 inhibitor and cyclin K degrader, CT7439. CDK12/13 inhibition interrupts transcription elongation, leading to increased DNA damage that results in cell death. This agent is a potentially novel treatment option for patients with colorectal cancer. Created in BioRender. Cyclin‐dependent kinase (CDK) 12 and
Wylie K. Watlington   +10 more
wiley   +1 more source

ZW4864‐mediated inhibition of the β‐catenin/BCL9/BCL9L complex reveals therapeutic potential in bladder cancer

open access: yesMolecular Oncology, EarlyView.
BCL9 and BCL9L drive bladder cancer progression by enhancing β‐catenin signaling, promoting proliferation, migration, invasion, and organoid growth. Genetic depletion of BCL9(L) suppresses malignant phenotypes, while pharmacological disruption of the β‐catenin/BCL9(L) complex with ZW4864 inhibits canonical Wnt signaling and tumor‐associated cellular ...
Roland Kotolloshi   +11 more
wiley   +1 more source

The cytosolic fate of ricin A chain in target cells [PDF]

open access: yes
Ricin is a heterodimeric, toxic plant protein. It is able to deliver its catalytic A chain (RTA) into the cytosol of target cells. RTA crosses the endoplasmic reticulum (ER) membrane into the cytosol, masquerading as a substrate of ER-associated ...
Hart, Philip John
core  

Establishing an assay to evaluate d‐amino acid oxidase enzyme kinetics and inhibition using WST‐8 redox dye

open access: yesFEBS Open Bio, EarlyView.
This study investigated a novel WST‐8‐based assay for evaluating d‐Amino acid oxidase (DAO) inhibitors. We confirmed its effectiveness using known inhibitors and found that uremic toxins possess relatively weak inhibitory activity compared to existing drugs.
Kahoko Miyake   +4 more
wiley   +1 more source

Requirement of PKA activity in Bb α-toxin protein induced larval lethality.

open access: yes, 2016
Representative composite gel of cAMP-dependent phosphorylation of Kemptide; The far right lane represents PKA activity. (A) PKA activity was measured after Bb α-toxin protein treatment in BmE cells. (B) PKA activity of larvae following Bb α-toxin protein
Ping Lin (146330)   +6 more
core   +1 more source

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