Results 91 to 100 of about 373,653 (310)

Short‐chain mono‐carboxylates as negative modulators of allosteric transitions in Gloeobacter violaceus ligand‐gated ion channel, and impact of a pre‐β5 strand (Loop Ω) double mutation on crotonate, not butyrate effect

Physiological Reports
Using the bacterial proton‐activated pentameric receptor‐channel Gloeobacter violaceus ligand‐gated ion channel (GLIC): (1) We characterize saturated, mono‐carboxylates as negative modulators of GLIC (as previously shown for crotonate; Alqazzaz et al ...
Catherine Van Renterghem, Ákos Nemecz, Karima Medjebeur, Pierre‐Jean Corringer   +3 more
doaj   +1 more source

Towards a unified molecular mechanism for ligand-dependent activation of NR4A-RXR heterodimers

eLife
A subset of nuclear receptors (NRs) function as permissive heterodimers with retinoid X receptor (RXR), defined by transcriptional activation in response to RXR agonist ligands.
Xiaoyu Yu, Yuanjun He, Thedore M Kamenecka, Douglas J Kojetin   +3 more
doaj   +1 more source

Neuropilin 1: A Novel Entry Factor for SARS-CoV-2 Infection and a Potential Therapeutic Target

Biologics: Targets & Therapy, 2021
Endeshaw Chekol Abebe,1 Teklie Mengie Ayele,2 Zelalem Tilahun Muche,3 Tadesse Asmamaw Dejenie4 1Department of Medical Biochemistry, College of Health Sciences, Debre Tabor University, Debre Tabor, Ethiopia; 2Department of Pharmacy, College of Health ...
Chekol Abebe E, Mengie Ayele T, Tilahun Muche Z, Asmamaw Dejenie T   +3 more
doaj  

The Active Site Sulfenic Acid Ligand in Nitrile Hydratases Can Function as a Nucleophile [PDF]

, 2014
Nitrile hydratase (NHase) catalyzes the hydration of nitriles to their corresponding commercially valuable amides at ambient temperatures and physiological pH.
Holz, Richard C., Liu, Dali, Martinez, Salette, Sanishvili, Ruslan, Wu, Rui   +4 more
core   +3 more sources

The PI3Kδ inhibitor roginolisib (IOA‐244) preserves T‐cell function and activity

Molecular Oncology, EarlyView.
Identification of novel PI3K inhibitors with limited immune‐related adverse effects is highly sought after. We found that roginolisib and idelalisib inhibit chronic lymphocytic leukemia (CLL) cells and Treg suppressive functions to similar extents, but roginolisib affects cytotoxic T‐cell function and promotion of pro‐inflammatory T helper subsets to a
Elise Solli, Alessio Bevilacqua, Mathias Wenes, Denis Migliorini, Lars van der Veen, Sigrid S Skånland, Giusy Di Conza, Kjetil Taskén   +7 more
wiley   +1 more source

The Use of Isomeric Testosterone Dimers to Explore Allosteric Effects in Substrate Binding to Cytochrome P450 CYP3A4 [PDF]

, 2016
: Cytochrome P450 CYP3A4 is the main drug-metabolizing enzyme in the human liver, being responsible for oxidation of 50% of all pharmaceuticals metabolized by human P450 enzymes.
Bastien, Dominic, Bérubé, Gervais, Denisov, Ilia G., Grinkova, Yelena V., Kincaid, James R., Mak, Piotr J., Sligar, Stephen G.   +6 more
core   +2 more sources

Tumour–host interactions in Drosophila: mechanisms in the tumour micro‐ and macroenvironment

Molecular Oncology, EarlyView.
This review examines how tumour–host crosstalk takes place at multiple levels of biological organisation, from local cell competition and immune crosstalk to organism‐wide metabolic and physiological collapse. Here, we integrate findings from Drosophila melanogaster studies that reveal conserved mechanisms through which tumours hijack host systems to ...
José Teles‐Reis, Tor Erik Rusten
wiley   +1 more source

Genetic attenuation of ALDH1A1 increases metastatic potential and aggressiveness in colorectal cancer

Molecular Oncology, EarlyView.
Aldehyde dehydrogenase 1A1 (ALDH1A1) is a cancer stem cell marker in several malignancies. We established a novel epithelial cell line from rectal adenocarcinoma with unique overexpression of this enzyme. Genetic attenuation of ALDH1A1 led to increased invasive capacity and metastatic potential, the inhibition of proliferation activity, and ultimately ...
Martina Poturnajova, Zuzana Kozovska, Ondrej Pos, Kristina Pavlov, Sachin Gulati, Peter Makovicky, Kristina Jakic, Monika Burikova, Eva Sedlackova, Barbora Svitkova, Silvia Tyciakova, Vojtech Bystry, Nicolas Blavet, Boris Tichy, Matej Hrnciar, Jaroslav Budis, Miroslav Tomas, Peter Dubovan, Georgina Kolnikova, Veronika Repaska, Nikoleta Mojzesova, Eva Zomborska, Daniel Pindak, Michal Mego, Tomas Szemes, Miroslava Matuskova   +25 more
wiley   +1 more source

Structural Immunology of Complement Receptors 3 and 4

Frontiers in Immunology, 2018
Complement receptors (CR) 3 and 4 belong to the family of beta-2 (CD18) integrins. CR3 and CR4 are often co-expressed in the myeloid subsets of leukocytes, but they are also found in NK cells and activated T and B lymphocytes.
Thomas Vorup-Jensen, Thomas Vorup-Jensen, Rasmus Kjeldsen Jensen   +2 more
doaj   +1 more source

Conformational selection in protein binding and function

, 2014
Protein binding and function often involves conformational changes. Advanced NMR experiments indicate that these conformational changes can occur in the absence of ligand molecules (or with bound ligands), and that the ligands may 'select' protein ...
Paul, Fabian, Weikl, Thomas R.
core   +1 more source