Results 91 to 100 of about 11,557,555 (285)

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

Molecular 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, Divya L. Dayanidhi, Mohammad Zokaasadi, John B. Mantyh, Pelumi D. Olawuni, Gabrielle Rupprecht, Jeremy M. Force, Shannon McCall, Ashwani K. Bahl, David S. Hsu, Jason A. Somarelli   +10 more
wiley   +1 more source

Emergence of functional sensory subtypes as defined by transient receptor potential channel expression [PDF]

, 2007
The existence of heterogeneous populations of dorsal root ganglion (DRG) neurons conveying different somatosensory information is the basis for the perception of touch, temperature, and pain. A differential expression of transient receptor potential (TRP)
Hjerling-Leffler, J, Ernfors, P, Ernfors, P,, Koltzenburg, M, AlQatari, M   +4 more
core   +1 more source

In vitro and in silico modelling of ROS1‐positive non‐small cell lung cancer reveals fusion‐dependent tyrosine kinase inhibitor responses

Molecular Oncology, EarlyView.
Drug resistance limits treatment success in a subset of lung cancers driven by ROS1 gene alterations. Using patient‐derived cells and computer simulations, we studied three key mutations and how they affect five targeted drugs. The mutations reduced drug effectiveness in different ways by altering protein structure and behavior.
Farhan Ul Haq, Marc Terrones, Felicia Rodrigues Fortes, Anne Schepers, Alessia Denis, Christophe Deben, Ken Op de Beeck, Guy Van Camp, Geert Vandeweyer   +8 more
wiley   +1 more source

Synaptic activation of transient receptor potential channels by metabotropic glutamate receptors in the lateral amygdala

, 2006
Classical mammalian transient receptor potential channels form non-selective cation channels that open in response to activation of phospholipase C-coupled metabotropic receptors, and are thought to play a key role in calcium homeostasis in non-excitable
Sedlak, P, Sedlak, P., Vidovic, M., Faber, E. S. L., Sah, P., Vidovic, Maria, Sah, Pankaj, Faber, Elizabeth (Louise)   +7 more
core   +1 more source

The VHL tumor suppressor at the crossroad of protein folding, aggregation, and cancer

Molecular Oncology, EarlyView.
Mutations, environmental stress, and chaperone dysfunction can destabilize pVHL, promoting its conversion from the native folded state into amyloid‐like assemblies. This transition may contribute to protein storage, cell dormancy, survival, and drug resistance.
Lara Abad, Silvio Carlo Ermanno Tosatto, Emanuela Leonardi   +2 more
wiley   +1 more source

Pharmacology of Vanilloid Transient Receptor Potential Cation Channels [PDF]

Molecular Pharmacology, 2009
Depending on their primary structure, the 28 mammalian transient receptor potential (TRP) cation channels identified so far can be sorted into 6 subfamilies: TRPC ("Canonical"), TRPV ("Vanilloid"), TRPM ("Melastatin"), TRPP ("Polycystin"), TRPML ("Mucolipin"), and TRPA ("Ankyrin").
Vriens, Joris, Appendino, Giovanni, Nilius, Bernd   +2 more
openaire   +5 more sources

Mutant p53R273H disrupts PDPK1 homodimerization and contributes to PDPK1 activation

Molecular Oncology, EarlyView.
How mutant p53R273H drives AKT signaling is unclear. We show that p53R273H, but not wild‐type, directly binds PDPK1 via a mutation‐dependent conformational change. This interaction disrupts inhibitory PDPK1 homodimerization and enhances AKT phosphorylation.
Mei Chee Lim, Alvin Kunyao Guo, Yoko Itahana, Srinivasaraghavan Kannan, Valerie Goh, Mingmin Ong, Terina Yan Wen Tay, Weiying Ye, Sabhashina Radha Krishnan, Jun Nishiyama, Chandra S Verma, Koji Itahana   +11 more
wiley   +1 more source

Transient receptor potential channels in bladder function

, 2013
The transient receptor potential (TRP) superfamily of cationic ion channels includes proteins involved in the transduction of several physical and chemical stimuli to finely tune physiological functions.
Avelino, A., Cruz, C., Frias, B., Cruz, F., Boudes, M., de Ridder, D., Charrua, Ana   +6 more
core   +1 more source

The multifaceted roles of lysosomes in cancer

Molecular Oncology, EarlyView.
Lysosomes support cancer cell adaptation by integrating macromolecule degradation and nutrient recycling with nutrient sensing, inter‐organelle communication and immune regulation. These interconnected functions can promote tumour growth, stress tolerance and therapy resistance, while also creating context‐dependent vulnerabilities that may be ...
Jia Li, Kevin M. Ryan
wiley   +1 more source

Quantification and Potential Functions of Endogenous Agonists of Transient Receptor Potential Channels in Patients With Irritable Bowel Syndrome [PDF]

, 2015
In mice, activation of the transient receptor potential cation channels (TRP) TRPV1, TRPV4, and TRPA1 causes visceral hypersensitivity. These receptors and their agonists might be involved in development of irritable bowel syndrome (IBS). We investigated
Liedtke, Wolfgang, Bertrand Michel, Justine, STANGHELLINI, VINCENZO, Vergnolle, Nathalie, Bertrand, Jessica, Rolland, Corinne, Poole, Daniel P, Le Faouder, Pauline, Veldhuis, Nicholas A, Dubourdeau, Marc, Bunnett, Nigel W, Cenac, Nicolas, Bautzova, Tereza, ZECCHI, LISA, Bertrand-Michel, Justine, BARBARA, GIOVANNI   +15 more
core   +1 more source