Results 51 to 60 of about 205,233 (331)

Structural insight into small molecule action on Frizzleds

Nature Communications, 2020
WNT-Frizzled (FZD) signaling plays a critical role in embryonic development, tissue homeostasis and human disease but no small molecule drugs targeting FZD with distinct efficacy have emerged so far.
Paweł Kozielewicz, Ainoleena Turku, Carl-Fredrik Bowin, Julian Petersen, Jana Valnohova, Maria Consuelo Alonso Cañizal, Yuki Ono, Asuka Inoue, Carsten Hoffmann, Gunnar Schulte   +9 more
doaj   +1 more source

Discovery of novel brain permeable and G protein-biased beta-1 adrenergic receptor partial agonists for the treatment of neurocognitive disorders. [PDF]

PLoS ONE, 2017
The beta-1 adrenergic receptor (ADRB1) is a promising therapeutic target intrinsically involved in the cognitive deficits and pathological features associated with Alzheimer's disease (AD).
Bitna Yi, Alam Jahangir, Andrew K Evans, Denise Briggs, Kristine Ravina, Jacqueline Ernest, Amir B Farimani, Wenchao Sun, Jayakumar Rajadas, Michael Green, Evan N Feinberg, Vijay S Pande, Mehrdad Shamloo   +12 more
doaj   +1 more source

Adaptaquin is selectively toxic to glioma stem cells through disruption of iron and cholesterol metabolism

Molecular Oncology, EarlyView.
Adaptaquin selectively kills glioma stem cells while sparing differentiated brain cells. Transcriptomic and proteomic analyses show Adaptaquin disrupts iron and cholesterol homeostasis, with iron chelation amplifying cytotoxicity via cholesterol depletion, mitochondrial dysfunction, and elevated reactive oxygen species.
Adrien M. Vaquié, Davod R. Shah, Eliane E. S. Brechbühl, Michael McNicholas, Zhaoyang Xu, John H. Stockley, Laura Morcom, Diana Gold Diaz, Gemma C. Girdler, Rachel V. Seear, Gabriel Balmus, Rajiv R. Ratan, Harry Bulstrode, James A. Nathan, Manav Pathania, Kevin M. Brindle, David H. Rowitch   +16 more
wiley   +1 more source

Aripiprazole-induced hyperprolactinemia in a young female with delusional disorder

Indian Journal of Psychological Medicine, 2016
Hyperprolactinemia is a common adverse effect of antipsychotic medication. Switching over to aripiprazole or adjunctive aripiprazole has been advocated for optimal management of antipsychotic-induced hyperprolactinemia.
Sam Padamadan Joseph
doaj   +1 more source

Label-free phenotypic profiling identified D-luciferin as a GPR35 agonist. [PDF]

PLoS ONE, 2012
Fluorescent and luminescent probes are essential to both in vitro molecular assays and in vivo imaging techniques, and have been extensively used to measure biological function.
Haibei Hu, Huayun Deng, Ye Fang
doaj   +1 more source

Treatment of type 2 diabetes by free fatty acid receptor agonists [PDF]

, 2014
Dietary free fatty acids (FFAs), such as ω-3 fatty acids, regulate metabolic and anti-inflammatory processes, with many of these effects attributed to FFAs interacting with a family of G protein-coupled receptors.
Hudson, Brian D., Milligan, Graeme, Ulven, Trond, Watterson, Kenneth R.   +3 more
core   +2 more sources

Potential therapeutic targeting of BKCa channels in glioblastoma treatment

Molecular Oncology, EarlyView.
This review summarizes current insights into the role of BKCa and mitoBKCa channels in glioblastoma biology, their potential classification as oncochannels, and the emerging pharmacological strategies targeting these channels, emphasizing the translational challenges in developing BKCa‐directed therapies for glioblastoma treatment.
Kamila Maliszewska‐Olejniczak, Karolina Pytlak, Sandra Jaworowska, Bogusz Kulawiak, Piotr Bednarczyk   +4 more
wiley   +1 more source

Both Ligand- and Cell-Specific Parameters Control Ligand Agonism in a Kinetic Model of G Protein–Coupled Receptor Signaling [PDF]

, 2007
G protein–coupled receptors (GPCRs) exist in multiple dynamic states (e.g., ligand-bound, inactive, G protein–coupled) that influence G protein activation and ultimately response generation. In quantitative models of GPCR signaling that incorporate these
Kinzer-Ursem, Tamara L., Linderman, Jennifer J.   +1 more
core   +3 more sources

New MT2 Melatonin Receptor-Selective Ligands: Agonists and Partial Agonists [PDF]

International Journal of Molecular Sciences, 2017
The search for melatonin receptor agonists and antagonists specific towards one of the receptor subtypes will extend our understanding of the role of this system in relaying circadian information to the body. A series of compounds derived from a hit compound discovered in a screening process led to powerful agonists specific for one of the isoform of ...
Jean Boutin, Anne Bonnaud, Chantal Brasseur, Olivier Bruno, Nolwenn Lepretre, Peter Oosting, Sophie Coumailleau, Philippe Delagrange, Olivier Nosjean, Céline Legros   +9 more
openaire   +1 more source

Redox regulation meets metabolism: targeting PRDX2 to prevent hepatocellular carcinoma

Molecular Oncology, EarlyView.
PRDX2 acts as a central redox hub linking metabolic dysfunction‐associated steatohepatitis (MASH) to hepatocellular carcinoma (HCC). In normal hepatocytes, PRDX2 maintains redox balance and metabolic homeostasis under oxidative stress. In contrast, during malignant transformation, PRDX2 promotes oncogenic signaling, stemness, and tumor initiation ...
Naroa Goikoetxea‐Usandizaga, María Luz Martinez‐Chantar, Carolina Conter   +2 more
wiley   +1 more source