Xavier Guillory

Xavier Guillory
Université de Rennes 1 | UR1 · Institut des Sciences Chimiques de Rennes (ISCR) - UMR CNRS 6226

Post-doctoral Reasearcher Medicinal Chemistry & Chemical Biology

About

19
Publications
10,337
Reads
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154
Citations
Introduction
Researcher in Synthetic and Medicinal Chemistry with a passion for projects that aim at improving human health. For this very reason, I decided to build both my education and career towards Medicinal Chemistry and Biomaterials Design.
Additional affiliations
September 2019 - present
Université de Rennes 1
Position
  • Lecturer
Description
  • Since September 2019, I am working as a contracted Lecturer (Enseignant Chercheur LRU) at the Faculty of Pharmacy. My time is split between various chemistry related fields to students and doing research in medicinal chemistry.
May 2019 - August 2019
Université de Rennes 1
Position
  • PostDoc Position
Description
  • Postdoctoral researcher in Medicinal Chemistry at the University of Rennes 1 ; Chemistry, Oncognesis, stress, signalling group (COSS - Inserm U1242).
November 2016 - March 2019
Eindhoven University of Technology
Position
  • PostDoc Position
Description
  • Postdoctoral Researcher in Medicinal Chemistry & Chemical Biology
Education
September 2011 - July 2012
University of Nantes
Field of study
  • Organic and therapeutic Chemistry
September 2010 - July 2011
Université du Maine
Field of study
  • Organic and polymer Chemistry

Publications

Publications (19)
Preprint
Full-text available
Inositol Requiring Enzyme 1 (IRE1) is a bifunctional serine/threonine kinase and endoribonuclease. It is a major mediator of the Unfolded Protein Response (UPR), which is activated during endoplasmic reticulum (ER) stress. Tumor cells experience ER stress due to adverse microenvironmental cues such as hypoxia or nutrient shortage and high metabolic...
Preprint
Ganglioside-monosialic acid (GM1) gangliosidosis, a rare autosomal recessive disorder, is frequently caused by deleterious single nucleotide variants (SNVs) in GLB1 gene. These variants result in reduced beta-galactosidase (β-gal) activity, leading to neurodegeneration associated with premature death. Currently, no effective therapy for GM1 ganglio...
Article
The reactivity of eight purified depsides obtained from six european lichens and that display as 2-oxoalkyl chain in ortho-position of the ester bond was explored. These depsides were found to lead to 1H-Isochromen-1-ones, which exhibit a distinctive blue fluorescence at 365 nm, in the presence of a 10% aqueous solution of KOH. A mechanistic explan...
Article
Function-oriented molecular editing of the polycyclic scaffold of securinine led to the preparation of a library of simplified analogs that have been evaluated for their cytotoxicity potential against HCT116 and HL60 human cell lines. Chemical diversity at the C14 position (securinine numbering) was generated through the site-selective γ-iodination...
Preprint
Full-text available
Inositol Requiring Enzyme 1 (IRE1) is a bifunctional serine/threonine kinase and endoribonuclease. It is a major mediator of the Unfolded Protein Response (UPR), which is activated during endoplasmic reticulum (ER) stress. Tumor cells experience ER stress due to adverse microenvironmental cues such as hypoxia or nutrient shortage and high metabolic...
Chapter
IRE1α (inositol-requiring enzyme 1 alpha, referred to IRE1 hereafter) is an Endoplasmic Reticulum (ER) resident transmembrane enzyme with cytosolic kinase/RNAse activities. Upon ER stress IRE1 is activated through trans-autophosphorylation and oligomerization, resulting in a conformational change of the RNase domain, thereby promoting two signaling...
Article
Full-text available
IRE1α (inositol requiring enzyme 1 alpha, referred to IRE1 hereafter) is an Endoplasmic Reticulum (ER) resident transmembrane enzyme with cytosolic kinase/RNAse activities. Upon ER stress IRE1 is activated through trans-autophosphorylation and oligomerization, resulting in a conformational change of the RNase domain thereby promoting two signaling...
Article
Rational design of protein–protein interaction (PPI) inhibitors is challenging. Connecting a general supramolecular protein binder with a specific peptidic ligand provides a novel conceptual approach. Thus, lysine-specific molecular tweezers were conjugated to a peptide-based 14–3–3 ligand and produced a strong PPI inhibitor with 100-fold elevated...
Article
The Unfolded Protein response is an adaptive pathway triggered upon alteration of endoplasmic reticulum (ER) homeostasis. It is transduced by three major ER stress sensors, among which the Inositol Requiring Enzyme 1 (IRE1) is the most evolutionarily conserved. IRE1 is an ER-resident type I transmembrane protein exhibiting an ER luminal domain that...
Article
Full-text available
IRE1α (inositol requiring enzyme 1 alpha) is one of the main transducers of the unfolded protein response (UPR). IRE1α plays instrumental protumoral roles in several cancers, and high IRE1α activity has been associated with poorer prognoses. In this context, IRE1α has been identified as a potentially relevant therapeutic target. Pharmacological inh...
Article
Full-text available
Stabilization of protein-protein interactions (PPIs) holds great potential for therapeutic agents, as illustrated by the successful drugs rapamycin and lenalidomide. However, how such interface-binding molecules can be created in a rational, bottom-up manner is a largely unanswered question. We report here how a fragment-based approach can be used...
Article
Previous studies have indicated the presence of defined interactions between oligo or poly(ethylene glycol) (OEG or PEG) and lysine residues. In these interactions, the OEG or PEG residues 'wrap around' the lysine amino group, thereby enabling complexation of the amino group by the ether oxygen residues. The resulting biochemical binding affinity a...
Article
Full-text available
Protein regions that are involved in Protein-Protein Interactions (PPIs) very often display a high degree of intrinsic disorder, which is reduced during the recognition process. A prime example is binding of the rigid 14-3-3 adapter proteins to their numerous partner proteins, whose recognition motifs undergo an extensive disorder-to-order transiti...
Article
For hybrid materials, the relationship between the macroscopic properties and the molecular structures and dynamics at the microscopic between the organic and inorganic components level is crucial. The characterization of these components as well as their reactivity have to be emphasized in order to design and synthesize improved hybrids. We report...
Article
Full-text available
Polysaccharides are among the most abundant macromolecules on Earth. These polymers are easily obtained from various marine resources such as algae, microorganisms and crustacean shells. The structure of these natural carbohydrates is innovative and quite complex. Marine biopolymers represent key scaffolds toward large challenging fields, such as b...
Article
Full-text available
Hydroxypropylmethylcellulose (HPMC) is a biocompatible polymer and a good candidate to make injectable hydrogels. After chemical grafting of silanolate groups under basic conditions, the decrease of pH promotes a self-crosslinked network. Innovative Extra Cellular Matrices (ECMs) are obtained thanks to these particular chemical groups which induce...
Article
We have developed an efficient diastereoselective synthetic route towards a nardosinane sesquiterpene scaffold. The strategy used a key bicyclic diene intermediate 11a, and allowed access to valuable polyoxygenated sesquiterpenes 21 and 22, which may be regarded as analogues of the natural sesquiterpenes laevinol B and fulvol acetate, respectively....

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