A series of aromatic/heterocyclic sulfonamides incorporating 2,3:4,5-bis-O-(isopropylidene)-beta-d-fructopyranosyl-thioureido moieties has been synthesized and assayed for the inhibition of seven human isoforms of the zinc enzyme carbonic... more
A series of aromatic/heterocyclic sulfonamides incorporating 2,3:4,5-bis-O-(isopropylidene)-beta-d-fructopyranosyl-thioureido moieties has been synthesized and assayed for the inhibition of seven human isoforms of the zinc enzyme carbonic anhydrase (hCA, EC 4.2.1.1). The new derivatives behaved as weak hCA I inhibitors (K(I)s of 9.4 -13.3microM), were efficient hCA II inhibitors (K(I)s of 6-750nM), and slightly inhibited isoforms hCA IV and hCA VA. Only the sulfanilamide derivative showed efficient and selective inhibition of hCA IV (K(I) of 10nM). These derivatives also showed excellent hCA VII inhibitory activity (K(I)s of 10-79nM), being less efficient as inhibitors of the transmembrane isoforms hCA IX (K(I)s of 10-4500nM) and hCA XIV (K(I)s of 21-3500nM). Two of the new compounds showed anticonvulsant action in a maximal electroshock seizure test in mice, with the fluorosulfanilamide derivative being a more efficient anticonvulsant than the antiepileptic drug topiramate.
Research Interests: Chemistry, Anticonvulsant, Glaucoma, Animals, Drug Design, and 15 moreFluorides, Enzyme Inhibition, Enzyme, Cattle, Anions, Carbonic anhydrase, Acetazolamide, Enzyme activity, Bioorganic and medicinal Chemistry, Cyanides, Antiepileptic Drug, Chemical Synthesis, Biochemistry and cell biology, Acetamides, and Chlorides
Research Interests: Chemistry, Cytotoxicity, Antioxidant, DPPH, Quercetin, and 4 moreTyrosinase, Chlorogenic Acid, Caffeic Acid, and Rutin
An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely... more
An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
Periodic mesoporous organosilica nanoparticles targeted to the mannose 6-phosphate receptor for rhabdomyosarcoma photodynamic therapy using a pulsed laser.
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Pompe disease is a rare disorder due to deficiency of the acid α-glucosidase (GAA) treated by enzyme replacement therapy. The present authorized treatment with rhGAA, the recombinant human enzyme, provides an important benefit in the... more
Pompe disease is a rare disorder due to deficiency of the acid α-glucosidase (GAA) treated by enzyme replacement therapy. The present authorized treatment with rhGAA, the recombinant human enzyme, provides an important benefit in the infantile onset; however, the juvenile and adult forms of the disease corresponding to >80% of the patients are less responsive to this treatment. This resistance has been mainly attributed to an insufficiency of mannose 6-phosphate residues in rhGAA to address lysosomes through the cation-independent mannose 6-phosphate receptor (CI-M6PR). As yet, several attempts to improve the enzyme delivery by increasing the number of mannose 6-phosphate on the enzyme were poorly effective on the late onset form of the disease. Here, we show that chemical conjugation of a synthetic analogue of the mannose 6-phosphate, named AMFA, onto rhGAA improves the affinity for CI-M6PR and the uptake of the enzyme in fibroblasts and myoblasts of adult Pompe patients. More i...
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Porous silicon nanoparticles grafted with a mannose-6-phosphate analogue were designed for targeting prostate cancer cells.
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Multifunctionalized porous Si NPs and their application in NIR photodynamic therapy and imaging of cancer are reported.
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Nowadays, nanomedicine brings new opportunities for diagnosis and treatment through innovative combinations of materials structured at the nanoscale, biomolecules and physicochemical processes. If the intrinsic properties of nanomaterials... more
Nowadays, nanomedicine brings new opportunities for diagnosis and treatment through innovative combinations of materials structured at the nanoscale, biomolecules and physicochemical processes. If the intrinsic properties of nanomaterials appear of major importance in this new discipline, the functionalization of these nanotools with biomolecules improves both their biocompatibility and efficacy. This is the case of carbohydrate derivatives, natural or synthetic, which are increasingly being used in nanostructures for medical purposes. As in current medicine, sugars are used to mimic their physiological roles. Indeed, carbohydrates enhance the solubility and reduce the clearance of drugs. They are used to mask immunogenic components of nano-objects and escape the body defenses and finally facilitate the delivery to the target tissue. All these properties explain the growing importance of sugars in nanomedicine.
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The development of personalized and non-invasive cancer therapies based on new targets combined with nanodevices is a major challenge in nanomedicine. In this work, the over-expression of a membrane lectin, the cation-independent mannose... more
The development of personalized and non-invasive cancer therapies based on new targets combined with nanodevices is a major challenge in nanomedicine. In this work, the over-expression of a membrane lectin, the cation-independent mannose 6-phosphate receptor (M6PR), was specifically demonstrated in prostate cancer cell lines and tissues. To efficiently target this lectin a mannose-6-phosphate analogue was synthesized in six steps and grafted onto the surface of functionalized mesoporous silica nanoparticles (MSNs). These MSNs were used for in vitro and ex vivo photodynamic therapy to treat prostate cancer cell lines and primary cell cultures prepared from patient biopsies. The results demonstrated the efficiency of M6PR targeting for prostate cancer theranostic.
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Abstract GaAs MESFETs, which form the basis of photonic MMIC's and OEIC's, have drawn considerable attention in recent years. However, their optical, microwave and electrical characteristics are largely dependent on... more
Abstract GaAs MESFETs, which form the basis of photonic MMIC's and OEIC's, have drawn considerable attention in recent years. However, their optical, microwave and electrical characteristics are largely dependent on internal parameters. In this context, we measure ...
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ABSTRACT We report the study of the functionalization of small sized MSNs with mannose. Classical procedures which were efficient with 100 nm diameter MSNs led to aggregation of small sized MSNs. Therefore, we grafted long chain amino... more
ABSTRACT We report the study of the functionalization of small sized MSNs with mannose. Classical procedures which were efficient with 100 nm diameter MSNs led to aggregation of small sized MSNs. Therefore, we grafted long chain amino silane and PEG-silane on the surface of the MSNs and reacted squarate mannose with NH2 groups. Although the MSN suspension was stable in EtOH, immediate aggregation was noticed in PBS which is attributed to remaining amino groups on the surface of the MSNs. We therefore grafted silylated mannose and PEG-silane on the MSN surface. Depending on the conditions, reversible aggregation was observed in PBS when heating to 37 °C and cooling to RT, or stable suspensions were obtained. The stable mannose-functionalized MSN suspensions were used for the imaging of retinoblastoma cells.
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Research Interests: Engineering, Materials Science, Fluorescence Microscopy, Nanoparticle, Nanoparticles, and 15 moreConfocal Microscopy, Advanced Materials, Porphyrins, Medicine, Humans, Porosity, Endocytosis, Cell Death, Physical sciences, CHEMICAL SCIENCES, Photochemotherapy, Photons, Biocompatible Materials, Mannose, and Infrared Rays
In this mini-review, we focus on different strategies to bring nanotools specifically to cancer cells. We discuss about a better targeting of tumor, combining the characteristics of tumor environment, the increase in nanoparticles life... more
In this mini-review, we focus on different strategies to bring nanotools specifically to cancer cells. We discuss about a better targeting of tumor, combining the characteristics of tumor environment, the increase in nanoparticles life time, the biomarkers overexpressed on cancer cells and different physical methods for non invasive therapies. Here we detail the necessity of a synergy between passive and active targeting for an actual specificity of cancer cells.