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Reversal of tumoral immune resistance by inhibition of tryptophan 2,3-dioxygenase
A TDO inhibitor was developed, which, upon systemic treatment, restored the ability of mice to reject TDO-expressing tumors and established proof-of-concept for the use of TDO inhibitors in cancer therapy. Expand
Crystal Structure of the Human Monoacylglycerol Lipase, a Key Actor in Endocannabinoid Signaling
The crystal structure of human MAGL is reported, and Cys201 is identified as the crucial residue in MAGL inhibition by N‐arachidonylmaleimide, a sulfhydryl‐reactive compound. Expand
The endoxylanases from family 11: computer analysis of protein sequences reveals important structural and phylogenetic relationships.
Eighty-two amino acid sequences of the catalytic domains of mature endoxylanases belonging to family 11 have been aligned using the programs MATCHBOX and CLUSTAL to allow the classification of the enzymes in groups according to sequence similarity. Expand
A review on the monoacylglycerol lipase: at the interface between fat and endocannabinoid signalling.
The milestones that punctuated MAGL history are reviewed, from its discovery to recent advances in the field of inhibitors development, and an emphasis is given on the recent elucidation of the tridimensional structure of the enzyme, which could offer new opportunities for rational drug design. Expand
Differential scanning calorimetry in life science: thermodynamics, stability, molecular recognition and application in drug design.
DSC is much used for the study of the stability and the folding of biomolecules, but it can also be applied in order to understand biomolecular interactions and can thus be an interesting technique in the process of drug design. Expand
Structural aspects of monoamine oxidase and its reversible inhibition.
  • J. Wouters
  • Chemistry, Medicine
  • Current medicinal chemistry
  • 1 April 1998
The major structural aspects of MAO, in relation with its primary sequence, secondary and three-dimensional structures, are reviewed, mainly focusing on the new generations of reversible and selective MAO inhibitors. Expand
Determination of physical changes of inulin related to sorption isotherms: An X-ray diffraction, modulated differential scanning calorimetry and environmental scanning electron microscopy study
Abstract This paper gives a relationship between powdered inulin behaviour and physical parameters determination. Glass transition temperature (Tg) and development of crystallinity were measured inExpand
A primordial RNA modification enzyme: the case of tRNA (m1A) methyltransferase.
It is reported that the TrmI enzyme from the archaeon Pyrococcus abyssi is also a homotetramer, whereas the P.abyssi enzyme is region-specific and catalyses the formation of m(1)A at two adjacent positions in the T-loop of certain tRNAs. Expand
Tryptophan 2,3-dioxygenase (TDO) inhibitors. 3-(2-(pyridyl)ethenyl)indoles as potential anticancer immunomodulators.
This study led to the identification of a very promising compound displaying good TDO inhibition (K(i) = 5.5 μM), high selectivity, and good oral bioavailability, and 58 was chosen for preclinical evaluation. Expand
Catalytic Mechanism of Escherichia coli Isopentenyl Diphosphate Isomerase Involves Cys-67, Glu-116, and Tyr-104 as Suggested by Crystal Structures of Complexes with Transition State Analogues and
Analysis of the crystal structures of complexes of Escherichia coli IPP·DMAPPs isomerase with a transition state analogue and a covalently attached irreversible inhibitor indicates that Glu-116, Tyr-104, and Cys-67 are involved in the antarafacial addition/elimination of protons during isomerization. Expand