Results 71 to 80 of about 3,750,504 (279)

IMPDH inhibition enhances cytarabine efficacy in SAMHD1‐expressing leukaemia cells via guanine nucleotide depletion

Molecular Oncology, EarlyView.
Cytarabine is a key therapy for acute myeloid leukaemia (AML), but its efficacy is limited by the dNTPase SAMHD1, which hydrolyses its active metabolite. Screening nucleotide biosynthesis inhibitors revealed that IMPDH inhibitors selectively sensitise SAMHD1‐proficient AML cells to cytarabine.
Miriam Yagüe‐Capilla, Christopher Dirks, Caroline Eiden, Sonja K. Fesenmayer, Femke M. Hormann, Yolande Klootsema, Ingrid Lilienthal, Si Min Zhang, Nikolas Herold, Sean G. Rudd   +9 more
wiley   +1 more source

Loss of proton‐sensing TDAG8 increases tumor progression in mouse models of colon cancer

Molecular Oncology, EarlyView.
Loss of the pH‐sensing receptor TDAG8 accelerates colorectal cancer progression in mice. Animals lacking TDAG8 expression had increased tumor growth, DNA damage, and recruitment of tumor‐associated immune cells, including macrophages, neutrophils, and monocytes.
Ermanno Malagola, Yasmine Illi, Anna Bircher, Marijn Wilmink, Rachele F. Malagutti, Solenn Ottié, Cordelia Schuler, Pedro A. Ruiz, Cheryl de Vallière, Klaus Seuwen, Gerhard Rogler, Martin Hausmann   +11 more
wiley   +1 more source

Distinct potency of compounds targeting the T1R3 subunit in modulating the response of human sweet and umami taste receptors

Scientific Reports
The heterodimeric G-protein-coupled receptors T1R2/T1R3 and T1R1/T1R3 have been identified as sweet and umami taste receptors, respectively, and both of these receptors share the T1R3 subunit.
Maiko Kawasaki, Yuta Kidera, Ryusei Goda, Chiaki Taketani, Misato Ide, Wataru Fujii, Tomoya Nakagita, Takumi Misaka   +7 more
doaj   +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

Pitfalls of NMDA Receptor Modulation by Neuroactive Steroids. The Effect of Positive and Negative Modulation of NMDA Receptors in an Animal Model of Schizophrenia

Biomolecules, 2021
Evidence from clinical and preclinical studies implicates dysfunction of N-methyl-D-aspartate receptors (NMDARs) in schizophrenia progression and symptoms.
Kristina Holubova, Marketa Chvojkova, Barbora Hrcka Krausova, Vojtech Vyklicky, Eva Kudova, Hana Chodounska, Ladislav Vyklicky, Karel Vales   +7 more
doaj   +1 more source

A New Negative Allosteric Modulator AP14145 for the Study of Small Conductance Calcium-Activated Potassium Channels [PDF]

, 2017
Background and purpose: Small conductance Ca2+-activated K+ (KCa2) channels represent a promising atrial-selective target for treatment of atrial fibrillation (AF).
Speerschneider, Tobias, Simo Vicens, Rafel, Jeppe E Kirchhoff, Tobias Speerschneider, Rafel Simó-Vicens, Kirchhoff, Jeppe Egedal, Bo H Bentzen, Abildgaard, Lea, Jonas G Diness, Lea Abildgaard, Grunnet, Morten, Dolce , Bernardo, Diness, Jonas Goldin, Morten Grunnet, Bentzen, Bo Hjorth, Bernardo Dolce, Ulrik S Sørensen, Sørensen, Ulrik Svane   +17 more
core   +1 more source

Translating whole‐genome doubling into precision medicine in cancer

Molecular Oncology, EarlyView.
Whole‐genome doubling creates a WGD‐positive tumor state characterized by persistent chromosomal instability, karyotypic diversification, and cellular stress. These same biological pressures drive aggressive tumor evolution while exposing therapeutic vulnerabilities, providing a rationale for WGD‐informed precision medicine. Whole‐genome doubling (WGD)
Sejung Lee, Junghyeok Lim, Jinhyuk Bhin
wiley   +1 more source

Cannabidiol is a negative allosteric modulator of the cannabinoid CB1 receptor. [PDF]

Br J Pharmacol, 2015
Background and Purpose Cannabidiol has been reported to act as an antagonist at cannabinoid CB 1 receptors. We hypothesized that cannabidiol would inhibit cannabinoid agonist activity through negative allosteric modulation of CB
Laprairie RB, Bagher AM, Kelly ME, Denovan-Wright EM.   +3 more
europepmc   +4 more sources

A novel class of negative allosteric modulators of NMDA receptor function

Bioorganic & Medicinal Chemistry Letters, 2015
NMDA receptors mediate a slow Ca(2+)-permeable component of excitatory synaptic transmission, and are involved in numerous normal brain functions including learning and memory. NMDA receptor over-activation can lead to cell death and abnormal excitation in ischemia associated with stroke, traumatic brain injury, and epilepsy.
Brooke M. Katzman, Riley E. Perszyk, Hongjie Yuan, Yesim Altas Tahirovic, Ayodeji E. Sotimehin, Stephen F. Traynelis, Dennis C. Liotta   +6 more
openaire   +3 more sources

Discovery of a Negative Allosteric Modulator of GABA_B Receptors

, 2016
Initialized from the scaffold of CGP7930, an allosteric agonist of GABAB receptors, a series of noncompetitive antagonists were discovered. Among these compounds, compounds 3, 6, and 14 decreased agonist GABA-induced maximal effect of IP3 production in ...
Zhi-Xiong Xia (1780636), Lin-Hai Chen (1780633), Yang Zhang (30734), Tong-Jie Xu (1780630), Jian-Feng Liu (260508), Bing Sun (44691), Fa-Jun Nan (62994)   +6 more
core   +1 more source