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Winum J.-Y.,Max Mousseron Institute of Biomolecules | Supuran C.T.,University of Florence
Journal of Enzyme Inhibition and Medicinal Chemistry | Year: 2015

In addition to the sulfonamides and their isosteres, recently novel carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) which act by binding to the metal ion from the active site were discovered. Based on the X-ray crystal structure of the CA II-trithiocarbonate adduct, dithiocarbamates, xanthates and thioxanthates were shown to potently inhibit α-and β-CAs. The hydroxamates constitute another class of recently studied CAIs both against mammalian and protozoan enzymes. Another chemotype for which CA inhibitory properties were recently reported is the salicylaldoxime scaffold. X-ray crystal structures were reported for CA II complexed with dithiocarbamates and hydroxamates, whereas the xanthates and salicylaldoximes were investigated by kinetic measurements and docking studies. The dithiocarbamates and the xanthates showed potent antiglaucoma activity in animal models of the disease whereas some hydroxamates inhibited the growth of Trypanosoma cruzii probably by inhibiting the protozoan CA. © 2014 Informa UK Ltd.


Tilly D.,CNRS Chemistry Institute of Rennes | Dayaker G.,Max Mousseron Institute of Biomolecules | Bachu P.,University of Queensland
Catalysis Science and Technology | Year: 2014

This review provides a perspective on C-H bond functionalization mediated by cobalt complexes used in either stoichiometric or catalytic amounts, without the contribution of any other transition metal, for organic synthesis applications. The competitive cost, availability and lower toxicity of cobalt compared to precious transition metals constitute valuable advantages of the methods. © the Partner Organisations 2014.


Pascal R.,Max Mousseron Institute of Biomolecules | Pross A.,Ben - Gurion University of the Negev
Journal of Systems Chemistry | Year: 2014

The conceptual divide separating the physical and biological sciences continues to challenge modern science. In this perspective it is proposed that the two sciences can be directly connected through the fundamental concept of stability. Physicochemical stability is shown to have a logical, rather than an empirical basis, and able to manifest itself in two distinct and often contrary ways, one thermodynamic, reflecting energetic considerations, and the other kinetic, reflecting time/persistence considerations. Each stability kind is shown to rest on a particular mathematical truism. Thermodynamic stability, the energetic expression, has a probabilistic/statistical basis due to Boltzmann, and leads to the Second Law of Thermodynamics. Dynamic kinetic stability (DKS), the time/persistence expression, is attributed to the stability associated with persistent replicating systems, and derives from the mathematics of exponential growth. The existence of two distinct stability kinds, each mathematically-based, leads to two distinct organizational forms of matter, animate and inanimate. That understanding offers insight into the reasons for the observation of just those two organizational forms, their different material characteristics, and provides a logical basis for understanding the nature of chemical and biological transformations, both within, and between, the two forms. © 2014 Pascal and Pross; licensee Chemistry Central Ltd.


Pascal R.,Max Mousseron Institute of Biomolecules | Pross A.,Ben - Gurion University of the Negev | Sutherland J.D.,University of Cambridge
Open Biology | Year: 2013

A sudden transition in a system from an inanimate state to the living state- defined on the basis of present day living ganisms-would constitute a highly unlikely event hardly predictable from physical laws. From this uncontroversial idea, a self-consistent representation of the origin of life process is built up, which is based on the possibility of a series of intermediate stages. This approach requires a particular kind of stability for these stages-dynamic kinetic stability (DKS)-which is not usually observed in regular chemistry, and which is reflected in the persistence of entities capable of self-reproduction. The necessary connection of this kinetic behaviour with far-from-equilibrium thermodynamic conditions is emphasized and this leads to an evolutionary view for the origin of life in which multiplying entities must be associated with the dissipation of free energy. Any kind of entity involved in this process has to pay the energetic cost of irreversibility, but, by doing so, the contingent emergence of new functions is made feasible. The consequences of these views on the studies of processes by which life can emerge are inferred. © 2013 The Authors. Published by the Royal Society under the terms of the Creative Commons Attribution License.


Vert M.,Max Mousseron Institute of Biomolecules
Macromolecular Bioscience | Year: 2011

Man-made artificial organic polymers are among the more recent sources of materials used by humans. In medicine, they contribute to applications in surgery, dentistry and pharmacology. Nowadays, innovations in the field of therapeutic polymers rely on novel polymers for specific applications such as guided tissue regeneration, tissue engineering, drug delivery systems, gene transfection, etc. Introducing reactive chemical functions within or along polymer backbones is an attractive route to generate functional polymers for medicine. However, any candidate to effective application must fulfil a number of requirements, grouped under the terms biocompatibility and biofunctionality, to be of real interest and have a future for effective application. Whenever the application requires a therapeutic aid for a limited period of time to help natural healing, bioresorbability is to be taken into account on top of biocompatibility and biofunctionality. This contribution presents the case of "artificial biopolymers" and discusses the potential of some members of the family with respect to temporary therapeutic applications that require functional polymers. © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


Vautrin J.,Max Mousseron Institute of Biomolecules
Neurochemistry International | Year: 2010

The vesicular hypothesis originally introduced to explain the quantal nature of presynaptic neurotransmitter (NT) release has been initially confirmed by the presence of NT within presynaptic vesicles and by an exo-endocytotic traffic associated with intense synaptic activity. Since then, an increasing number of synaptic transmission properties cannot be readily incorporated into the now popular model in which each quantal NT packet is prepared in a vesicle and is released by diffusion across the synaptic cleft when this vesicle fuses transiently or definitively with the plasma membrane. Interestingly, presynaptic exocytosis exhibits the characteristics of the ubiquitous secretory pathway by which all eukaryotic cells interact with their immediate environment, not just externalizing soluble products, but principally delivering at particular location of the cell surface specific glycoconjugates constituting the extracellular matrix (ECM) that mediates intercellular adhesion, recognition and signaling. Recent studies point to the involvement of vesicular glycoproteins in fast transmission after their incorporation into the transsynaptic ECM, or synaptomatrix. The notion of synaptomatrix is presented as a multimolecular tight arrangement that is dynamically remodeled in a use-dependent fashion via PKC to support synaptic morpho-functional plasticity. The data reviewed suggests that the synaptomatrix controls in a Ca2+ entry-dependent manner the solubility of the NT in the cleft to support fast transmission. © 2010 Elsevier Ltd.


Romuald C.,Max Mousseron Institute of Biomolecules | Coutrot F.,Max Mousseron Institute of Biomolecules
Angewandte Chemie - International Edition | Year: 2012

Collar and tie men: The smallest trefoil knot reported to date has been prepared by an active metal template synthesis. Copper(I) ions are able to constrain the well-designed structure so that it can form the loops by complexing to the bipyridine moieties in the core of the thread and the two ends of the entangled lace on opposite faces of the loop, before acting as a catalyst to close the lace (see picture). Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.


Martin A.R.,Max Mousseron Institute of Biomolecules | Vasseur J.-J.,Max Mousseron Institute of Biomolecules | Smietana M.,Max Mousseron Institute of Biomolecules
Chemical Society Reviews | Year: 2013

At the intersection of nucleic acid and boron chemistries lies a thriving world of possibilities. During the past decades, the merging of these research domains has led to fascinating discoveries in different fields ranging from material to medical sciences. In recent years the interplay of these two worlds has gained a lot of attention, as can be judged by the increasing number of articles in which boron and nucleic acids stand out for their potential medicinal, biotechnological or analytical applications. In this review, we present an outline of this crossroads by focusing on both the interaction of boronated compounds with nucleic acids and the modification of nucleic acids by boron containing moieties. © 2013 The Royal Society of Chemistry.


Oger C.,Max Mousseron Institute of Biomolecules | Balas L.,Max Mousseron Institute of Biomolecules | Durand T.,Max Mousseron Institute of Biomolecules | Galano J.-M.,Max Mousseron Institute of Biomolecules
Chemical Reviews | Year: 2013

Application to key polyfunctionalyzed precursors in a multistep synthesis thus required high chemo-, regio-, and stereoselective conditions. Depending on the substrate, the choice of the reduction conditions may be crucial for a successful result. The whole argument is organized in three sections. The first section includes an overview of the reducing methods described till now on monoalkynes. Mechanistic information was given except when the mechanism remains unclear. Effectively, their reduction may provide useful vinylsilane precursors while their absence of reactivity is an elegant means to temporarily mask a terminal alkyne, with the latter being an important key intermediate in organic synthesis. The hydroboration-protonolysis sequence affords (Z)-alkenes with good to excellent stereoselectivities and yields depending on the hydroborating reagent and reaction conditions.


Pascal R.,Max Mousseron Institute of Biomolecules
Journal of Systems Chemistry | Year: 2012

Any living organism can be considered as a component of a dissipative process coupling an irreversible consumption of energy to the growth, reproduction and evolution of living things. Close interactions between metabolism and reproduction are thus required, which means that metabolism has two main functions. The first one, which is the most easily perceptible, corresponds to the synthesis of the components of living beings that are not found in the environment (anabolism). The second one, which is usually associated with the former, is the dissipative process coupling the consumption of energy to self-organization and reproduction and introducing irreversibility in the process. Considering the origin of life, the formation of at least some of the building blocks constituting a living organism can be envisaged in a close to equilibrium situation under reducing conditions (for instance in hydrothermal vents). However, coupling irreversibly self-organization with the dissipation of an energy flux implies far from equilibrium conditions that are shown in this work to raise quantitative requirements on the height of kinetic barriers protecting metabolites from a spontaneous evolution into deactivated species through a quantitative relationship with the time scale of the progress of the overall process and the absolute temperature. The thermodynamic potential of physical sources of energy capable of feeding the emergence of this capacity can be inferred, which leads to the identification of photochemistry at the wavelength of visible light or processes capable of generating activated species by heating transiently a chemical environment above several thousand Kelvin as the only processes capable of fulfilling this requirement. © 2012 Pascal; licensee Chemistry Central Ltd.

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