Search Results - "Trembleau, Laurent"
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A ribosomally synthesised and post-translationally modified peptide containing a β-enamino acid and a macrocyclic motif
Published in Nature communications (26-08-2022)“…Ribosomally synthesized and post-translationally modified peptides (RiPPs) are structurally complex natural products with diverse bioactivities. Here we report…”
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2
Design, Synthesis, and Antiproliferative Activity of New 5-Chloro-indole-2-carboxylate and Pyrrolo[3,4-b]indol-3-one Derivatives as Potent Inhibitors of EGFRT790M/BRAFV600E Pathways
Published in Molecules (Basel, Switzerland) (28-01-2023)“…Mutant EGFR/BRAF pathways are thought to be crucial targets for the development of anticancer drugs since they are over-activated in several malignancies. We…”
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3
The mechanism of patellamide macrocyclization revealed by the characterization of the PatG macrocyclase domain
Published in Nature structural & molecular biology (01-08-2012)“…The subtilisin-like domain of PatG can catalyze the macrocyclization of linear peptide. The crystal structure of the PatG macrocyclase domain, along with…”
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4
Design, synthesis, apoptotic, and antiproliferative effects of 5-chloro-3- (2-methoxyvinyl)-indole-2-carboxamides and pyrido[3,4-b]indol-1-ones as potent EGFRWT/EGFRT790M inhibitors
Published in Journal of enzyme inhibition and medicinal chemistry (01-12-2023)“…A new series of indole-2-carboxamides 5a-g, 6a-f and pyrido[3,4-b]indol-1-ones 7a and 7b have been developed as new antiproliferative agents that target both…”
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5
Synthesis and Biological Evaluation of Indole-2-Carboxamides with Potent Apoptotic Antiproliferative Activity as EGFR/CDK2 Dual Inhibitors
Published in Pharmaceuticals (Basel, Switzerland) (01-08-2022)“…The apoptotic antiproliferative actions of our previously reported CB1 allosteric modulators 5-chlorobenzofuran-2-carboxamide derivatives VIIa–j prompted us to…”
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Enzymatic Reconstitution and Biosynthetic Investigation of the Bacterial Carbazole Neocarazostatin A
Published in Journal of organic chemistry (20-12-2019)“…Tricyclic carbazole is an important scaffold in many naturally occurring metabolites, as well as valuable building blocks. Here we report the reconstitution of…”
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Design, Synthesis, and Biological Evaluation of Indole-2-carboxamides as Potential Multi-Target Antiproliferative Agents
Published in Pharmaceuticals (Basel, Switzerland) (01-07-2023)“…A small set of indole-based derivatives, and - , was designed and synthesized. Compounds - demonstrated promising antiproliferative activity, with GI values…”
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8
A Unique Tryptophan C-Prenyltransferase from the Kawaguchipeptin Biosynthetic Pathway
Published in Angewandte Chemie International Edition (07-03-2016)“…Cyanobactins are a rapidly growing family of linear and cyclic peptides produced by cyanobacteria. Kawaguchipeptins A and B, two macrocyclic undecapeptides…”
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9
Structure-Based Design, Synthesis and Bioactivity of a New Anti-TNFα Cyclopeptide
Published in Molecules (Basel, Switzerland) (19-02-2020)“…As opposed to small molecules, macrocyclic peptides possess a large surface area and are recognised as promising candidates to selectively treat diseases by…”
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10
A novel allosteric modulator of the cannabinoid CB1 receptor ameliorates hyperdopaminergia endophenotypes in rodent models
Published in Neuropsychopharmacology (New York, N.Y.) (01-01-2021)“…Abstract The endocannabinoid system (eCBs) encompasses the endocannabinoids, their synthetic and degradative enzymes, and cannabinoid (CB) receptors. The eCBs…”
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11
Helical Conformation of Alkanes in a Hydrophobic Cavitand
Published in Science (American Association for the Advancement of Science) (29-08-2003)“…Alkanes adopt extended conformations in solution that minimize steric interactions and maximize surface area. Folding can reduce the amount of hydrophobic…”
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12
Design and synthesis new indole-based aromatase/iNOS inhibitors with apoptotic antiproliferative activity
Published in Frontiers in chemistry (06-09-2024)“…The present study details the design, synthesis, and bio-evaluation of indoles as dual inhibitors of aromatase and inducible nitric oxide synthase (iNOS)with…”
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13
Helical Folding of Alkanes in a Self-Assembled, Cylindrical Capsule
Published in Journal of the American Chemical Society (20-10-2004)“…The reversible encapsulation of a series of normal alkane guests in a cylindrical host was studied by NMR methods. For small hydrocarbons such as n-pentane or…”
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14
Synthesis and characterisation of biologically compatible TiO2 nanoparticles
Published in Nanoscale research letters (14-06-2011)“…We describe for the first time the synthesis of biocompatible TiO 2 nanoparticles containing a functional NH 2 group which are easily dispersible in water. The…”
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15
Multigram-Scale Synthesis of Short Peptides via a Simplified Repetitive Solution-Phase Procedure
Published in Journal of organic chemistry (05-02-2010)“…A rapid repetitive solution-phase synthesis of peptides is described. The procedure involves coupling of amino acids and peptide acids, instead of the usual…”
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16
Kinetically Stable Complexes in Water: The Role of Hydration and Hydrophobicity
Published in Journal of the American Chemical Society (10-03-2004)“…We describe here the synthesis and characterization of a molecular receptor that forms kinetically and thermodynamically stable host−guest complexes in water…”
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17
Galmic, a Nonpeptide Galanin Receptor Agonist, Affects Behaviors in Seizure, Pain, and Forced-Swim Tests
Published in Proceedings of the National Academy of Sciences - PNAS (13-07-2004)“…The pharmacological exploitation of the galanin receptors as drug targets for treatment of epilepsy, depression, and pain has been hampered by the lack of…”
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A Weakened Immune Response to Synthetic Exo-Peptides Predicts a Potential Biosecurity Risk in the Retrieval of Exo-Microorganisms
Published in Microorganisms (Basel) (17-07-2020)“…The discovery of liquid water at several locations in the solar system raises the possibility that microbial life may have evolved outside Earth and as such…”
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Different N—H...π interactions in two indole derivatives
Published in Acta crystallographica. Section E, Crystallographic communications (01-05-2016)“…We describe the syntheses and crystal structures of two indole derivatives, namely 6-isopropyl-3-(2-nitro-1-phenylethyl)-1 H -indole, C 19 H 20 N 2 O 2 , (I),…”
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20
Weak interactions in the crystal structures of two indole derivatives
Published in Acta crystallographica. Section E, Crystallographic communications (01-07-2016)“…We describe the syntheses and crystal structures of two indole derivatives, namely a second monoclinic polymorph of ethyl 5-chloro-1 H -indole-2-carboxylate C…”
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