Search Results - "Calmels, Thierry"
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Connexin 30 is expressed in the mouse sino-atrial node and modulates heart rate
Published in Cardiovascular research (01-01-2010)“…Aims This study aimed at characterizing expression and the functional role of the Gjb6 gene, encoding for connexin 30 (Cx30) protein, in the adult mouse heart…”
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Refined Docking as a Valuable Tool for Lead Optimization: Application to Histamine H3 Receptor Antagonists
Published in Archiv der Pharmazie (Weinheim) (01-10-2008)“…Drug‐discovery projects frequently employ structure‐based information through protein modeling and ligand docking, and there is a plethora of reports relating…”
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Human p63RhoGEF, a novel RhoA-specific guanine nucleotide exchange factor, is localized in cardiac sarcomere
Published in Journal of cell science (01-02-2002)“…The Rho small GTPases are crucial proteins involved in regulation of signal transduction cascades from extracellular stimuli to cell nucleus and cytoskeleton…”
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In situ hybridization: a technique to study localization of cardiac gene expression
Published in Methods in molecular biology (Clifton, N.J.) (2007)“…In situ hybridization allows the detection of specific gene transcripts in tissues, cells or, chromosomes. In the cardiovascular field, this powerful and rapid…”
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Cell Type-specific Localization of Human Cardiac S1P Receptors
Published in The journal of histochemistry and cytochemistry (01-05-2002)“…Sphingosine 1-phosphate (S1P), which derives from the metabolism of sphingomyelin, is mainly synthesized, stored, and released from platelets after activation…”
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Genomic organization and alternative transcripts of the human Connexin40 gene
Published in Gene (13-02-2003)“…The human Cx40 gene ( NT_004434.5) was sorted out from the GenBank database and as a result of a BLAST homology search, two ESTs ( BE784549 from a human lung…”
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uDENN, DENN, and dDENN: Indissociable Domains in Rab and MAP Kinases Signaling Pathways
Published in Biochemical and biophysical research communications (28-09-2001)“…DENN domains are found in a variety of signaling proteins but their exact function remains undefined. Some of the DENN-containing proteins, such as rat Rab3GEP…”
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Constitutive expression of the DNA-binding domain of Ets1 increases endothelial cell adhesion and stimulates their organization into capillary-like structures
Published in Oncogene (10-02-2000)“…We previously reported that the Ets1 transcription factor is expressed in endothelial cells during angiogenesis both in normal and pathological development. We…”
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Dual Piperidine-Based Histamine H3 and Sigma‑1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain
Published in Journal of medicinal chemistry (27-07-2023)“…In search of new dual-acting histamine H3/sigma-1 receptor ligands, we designed a series of compounds structurally based on highly active in vivo ligands…”
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Dual Piperidine-Based Histamine H 3 and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain
Published in Journal of medicinal chemistry (27-07-2023)“…In search of new dual-acting histamine H /sigma-1 receptor ligands, we designed a series of compounds structurally based on highly active ligands previously…”
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12
Biophysical interaction between phospholamban and protein phosphatase 1 regulatory subunit GM
Published in FEBS letters (20-11-1998)“…Regulation of the sarco(endo)plasmic reticulum Ca 2+-ATPase (SERCA 2a) depends on the phosphorylation state of phospholamban (PLB). When PLB is phosphorylated,…”
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Synthesis and evaluation of a 2-benzothiazolylphenylmethyl ether class of histamine H4 receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-11-2016)“…[Display omitted] Synthesis and biological evaluation of a new class of histamine H4 receptor ligands, distinct from the previously reported chemotypes, are…”
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Discovery of nanomolar ligands with novel scaffolds for the histamine H4 receptor by virtual screening
Published in European journal of medicinal chemistry (05-01-2017)“…The involvement of histamine H4 receptor (H4R) in immune cells chemotaxis and mediator release makes it an attractive target for the treatment of inflammation…”
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Improving selectivity of dopamine D3 receptor ligands
Published in Bioorganic & medicinal chemistry letters (01-02-2016)“…[Display omitted] The seminal human dopamine D3 receptor (hD3R) ligand BP 897 has shown interesting properties during clinical trials. However, its lack of…”
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Novel and highly potent histamine H3 receptor ligands. Part 1: withdrawing of hERG activity
Published in Bioorganic & medicinal chemistry letters (15-09-2011)“…Pre-clinical investigation of some aryl-piperidinyl ether histamine H3 receptor antagonists revealed a strong hERG binding. To overcome this issue, we have…”
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Determination of the binding mode and interacting amino-acids for dibasic H3 receptor antagonists
Published in Bioorganic & medicinal chemistry (01-08-2013)“…Due to its involvement in major CNS functions, the histamine H3 receptor (H3R) is the subject of intensive medicinal chemistry investigation, supported by the…”
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High efficiency transformation of Tolypocladium geodes conidiospores to phleomycin resistance
Published in Current genetics (01-09-1991)“…A convenient and efficient transformation system has been developed for the filamentous fungus Tolypocladium geodes. In contrast to most of the commonly…”
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Hybrid approach for the design of highly affine and selective dopamine D 3 receptor ligands using privileged scaffolds of biogenic amine GPCR ligands
Published in Bioorganic & medicinal chemistry (01-12-2007)“…The design and optimization of dopamine D 3 receptor ligands has been performed applying a hybrid structure development. Novel ligands were synthesized…”
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Novel and highly potent histamine H3 receptor ligands. Part 3: An alcohol function to improve the pharmacokinetic profile
Published in Bioorganic & medicinal chemistry letters (01-05-2013)“…Synthesis and biological evaluation of potent histamine H3 receptor antagonists incorporating a hydroxyl function are described. Compounds in this series…”
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