Results 131 to 140 of about 774,543 (406)

Ligand-guided homology modeling drives identification of novel histamine H3 receptor ligands [PDF]

, 2019
In this study, we report a ligand-guided homology modeling approach allowing the analysis of relevant binding site residue conformations and the identification of two novel histamine H3 receptor ligands with binding affinity in the nanomolar range.
Hagenow, Stefanie, Schaller, David, Stark, Holger, Wolber, Gerhard   +3 more
core   +2 more sources

Neutrophil deficiency increases T cell numbers at the site of tissue injury in mice

FEBS Letters, EarlyView.
In wild‐type mice, injury or acute inflammation induces neutrophil influx followed by macrophage accumulation. Mcl1ΔMyelo (neutrophil‐deficient) mice lack neutrophils, and in response to muscle injury show fewer macrophages and exhibit strikingly elevated T‐cell numbers, primarily non‐conventional “double‐negative” (DN) αβ and γδ T cells.
Hajnalka Halász, Albert Bálint Papp, Lukács Sándor Lesinszki, Attila Mócsai, Tamás Varga, László Nagy, Péter Gogolák   +6 more
wiley   +1 more source

Design and characterization of superpotent bivalent ligands targeting oxytocin receptor dimers via a channel-like structure [PDF]

, 2016
Dimeric/oligomeric states of G-protein coupled receptors have been difficult to target. We report here bivalent ligands consisting of two identical oxytocin-mimetics that induce a three order magnitude boost in G-protein signaling of oxytocin receptors ...
Bice Chini, Chini B., Daniela Braida, Fanelli F., G. Enrico Rovati, Gunnar Kleinau, Lesley A. Howell, Lucka Bibic, Mariaelvina Sala, Markus Muttenthaler, Marta Busnelli, Maurice Manning, Peter J. McCormick, Simona Di Lascio, Stoytcho Stoev, Tommaso Bellini   +15 more
core   +5 more sources

MET variants with activating N‐lobe mutations identified in hereditary papillary renal cell carcinomas still require ligand stimulation

Molecular Oncology, EarlyView.
MET variants in the N‐lobe of the kinase domain, found in hereditary papillary renal cell carcinoma, require ligand stimulation to promote cell transformation, in contrast to other RTK variants. This suggests that HGF expression in the microenvironment is important for tumor growth in such patients. Their sensitivity to MET inhibitors opens the way for
Célia Guérin, Audrey Vinchent, Marie Fernandes, Isabelle Damour, Agathe Laratte, Rémi Tellier, Gabriella O. Estevam, Jean‐Pascal Meneboo, Céline Villenet, Clotilde Descarpentries, James S. Fraser, Martin Figeac, Alexis B. Cortot, Etienne Rouleau, David Tulasne   +14 more
wiley   +1 more source

Functional selectivity of GPCR-directed drug action through location bias. [PDF]

, 2017
G-protein-coupled receptors (GPCRs) are increasingly recognized to operate from intracellular membranes as well as the plasma membrane. The β 2 -adrenergic GPCR can activate G s -linked cyclic AMP (G s -cAMP) signaling from endosomes.
Conti, Marco, Huang, Bo, Irannejad, Roshanak, Mika, Delphine, Pessino, Veronica, von Zastrow, Mark, Wedegaertner, Philip B.   +6 more
core   +3 more sources

Response to neoadjuvant chemotherapy in early breast cancers is associated with epithelial–mesenchymal transition and tumor‐infiltrating lymphocytes

Molecular Oncology, EarlyView.
Epithelial–mesenchymal transition (EMT) and tumor‐infiltrating lymphocytes (TILs) are associated with early breast cancer response to neoadjuvant chemotherapy (NAC). This study evaluated EMT and TIL shifts, with immunofluorescence and RNA sequencing, at diagnosis and in residual tumors as potential biomarkers associated with treatment response.
Françoise Derouane, Jérôme Ambroise, Cédric van Marcke, Mieke Van Bockstal, Martine Berlière, Christine Galant, Hélène Dano, Médina Lougué, Elena Benidovskaya, Guy Jerusalem, Vincent Bours, Claire Josse, Jérôme Thiry, Aurélie Daumerie, Caroline Bouzin, Cyril Corbet, François P. Duhoux   +16 more
wiley   +1 more source

On the role of G protein-coupled receptors oligomerization [PDF]

, 2013
The existence of a supramolecular organization of the G protein-coupled receptor (GPCR) is now being widely accepted by the scientific community.
Ahern, Siobhán, Ciruela Alférez, Francisco, Fernández Dueñas, Víctor, Gómer Soler, Maricel   +3 more
core   +2 more sources

G Protein–Coupled Receptor Rhodopsin [PDF]

Annual Review of Biochemistry, 2006
The rhodopsin crystal structure provides a structural basis for understanding the function of this and other G protein–coupled receptors (GPCRs). The major structural motifs observed for rhodopsin are expected to carry over to other GPCRs, and the mechanism of transformation of the receptor from inactive to active forms is thus likely conserved ...
openaire   +3 more sources

Peripheral blood proteome biomarkers distinguish immunosuppressive features of cancer progression

Molecular Oncology, EarlyView.
Immune status significantly influences cancer progression. This study used plasma proteomics to analyze benign 67NR and malignant 4T1 breast tumor models at early and late tumor stages. Immune‐related proteins–osteopontin (Spp1), lactotransferrin (Ltf), calreticulin (Calr) and peroxiredoxin 2 (Prdx2)–were associated with systemic myeloid‐derived ...
Yeon Ji Park, Jae Won Oh, Hyewon Chung, Jung Won Kwon, Yi Rang Na, Kwang Pyo Kim, Seung Hyeok Seok   +6 more
wiley   +1 more source

Representation Learning for Class C G Protein-Coupled Receptors Classification

Molecules, 2018
G protein-coupled receptors (GPCRs) are integral cell membrane proteins of relevance for pharmacology. The complete tertiary structure including both extracellular and transmembrane domains has not been determined for any member of class C GPCRs.
Raúl Cruz-Barbosa, Erik-German Ramos-Pérez, Jesús Giraldo   +2 more
doaj   +1 more source