Abstract: The present invention relates to methods to inhibit the inflammatory caspases for ameliorating, preventing, or treating diseases associated with excessive inflammatory responses to pathogenic infection or danger signalization including coronaviruses infection and inflammatory consequences of coronaviruses infection in humans, SARS, MERS, COVID-19. The identification of a central role of the inflammatory Caspases in the pathogenic activity of the canonic and non-canonic inflammasomes provide a general method to treat acute diseases including SARS, MERS, COVID-19, cytokine release syndrome, cytokine storm syndrome, pyroptosis and inflammasome-related multi-organ failure, and pathogen-induced acute respiratory distress syndromes. Compounds to be repurposed and new pharmaceutical compositions are claimed.

Abstract: The present invention relates to a compound of formula (I): wherein P1, P3, P4 and P5 are amino acid residues or amino acid like structures. The invention also relates to a compound of formula (I) for its use as a Caspase-2 inhibitor and for its therapeutical use. It also concerns the use of a compound of formula (I) as activity base probe to selectively detect Caspase-2 activity.

Abstract: The present invention relates to a compound of formula (I): wherein P1, P3, P4 and P5 are amino acid residues or amino acid like structures. The invention also relates to a compound of formula (I) for its use as a Caspase-2 inhibitor and for its therapeutical use. It also concerns the use of a compound of formula (I) as activity base probe to selectively detect Caspase-2 activity.

Abstract: The present invention relates to a compound of formula (I) wherein P1, P3, P4 and P5 are amino acid residues. The invention also relates to a compound of formula (I) for its use as a Caspase-2 inhibitor and for its therapeutical use. It also concerns the use of a compound of formula (I) as activity base probe to selectively detect Caspase-2 activity.

Abstract: The present invention relates to a compound of formula (I): wherein P1, P3, P4 and P5 are amino acid residues or amino acid like structures. The invention also relates to a compound of formula (I) for its use as a Caspase-2 inhibitor and for its therapeutical use. It also concerns the use of a compound of formula (I) as activity base probe to selectively detect Caspase-2 activity.

Abstract: The present invention relates to a compound of formula (I) wherein P1, P3, P4 and P5 are amino acid residues. The invention also relates to a compound of formula (I) for its use as a Caspase-2 inhibitor and for its therapeutical use. It also concerns the use of a compound of formula (I) as activity base probe to selectively detect Caspase-2 activity.

Abstract: ANT-ligands having a substituted nitrogeneous heterocycle A wherein A is a substituted pyrimidinone of formula I wherein R1 is —(CH2)n-CO—OH; —(CH2)n-CO—OR; —(CH2)n-CO—NHR; —(CH2)n-CO—N(R, R?); —(CH2)n-OH; —(CH2)n-OR; —(CH2)n-OAr; —(CH2)n-C(R,R?)—(CH2)n-OH, R and R?, in the above radicals, being identical or different and representing H or a C1-C12 alkyl or cycloalkyl radical; and Ar is a phenyl or Het., Het.

Abstract: ANT-ligands having a substituted nitrogeneous heterocycle A wherein A is a substituted pyrimidinone of formula I wherein R1 is —(CH2)n-CO—OH; —(CH2)n-CO—OR; —(CH2)n-CO—NHR; —(CH2)n-CO—N(R, R?); —(CH2)n-OH; —(CH2)n-OR; —(CH2)n-OAr; —(CH2)n-C(R,R?)—(CH2)n-OH, R and R?, in the above radicals, being identical or different and representing H or a C1-C12 alkyl or cycloalkyl radical; and Ar is a phenyl or Het., Het.

Abstract: The invention relates to molecules ANT-ligands having a substituted nitrogeneous heterocycle A wherein A is a substituted pyrazinone of formula I wherein R1 is —(CH2)n—CO—OH; —(CH2)n—CO—OR; —(CH2)n—CO—NHR; —(CH2)n—CO—N(R,R?); —(CH2)n—OH; —(CH2)n—OR; —(CH2)n—OAr; —(CH2)n—C(R,R?)—(CH2)n—OH, R and R?, in the above radicals, being identical or different and representing H or a C1-C12 alkyl or cycloalkyl radical; and Ar is a phenyl or Het., Het.

Abstract: Inhibitors for preventing, blacking/silencing caspase-2 activity in cell death.

Abstract: The invention relates to selective new caspase-2 inhibitors that recognize caspase-2 and prevent and block its activity based on the following backbone: 2-Quinolinylcarbonyl-L-Valinyl-L-Aspartyl (methyl ester)-L-Valinyl-L-Alanyl-L-Aspartyl (methyl ester) 2,6-difluorophenyl ester SEQ ID NO:1) and derivatives thereof, SEQ ID NO:1 corresponding to formulae Ia or Ib. Application of the inhibitors for preventing and treating diseases involving caspase-2.

Abstract: The invention relates to molecules ANT-ligands having a substituted nitrogeneous heterocycle A wherein —A is a substituted pyrazinone of formula I wherein R1 is —(CH2)n —CO—OH; —(CH2)n —CO—OR; —(CH2)n —CO—NHR; —(CH2)n —CO—N(R, R?); —(CH2)n —OH; —(CH2)n —OR; —(CH2)n —OAr; —(CH2)n —C(R,R?) —(CH2)n —OH, R and R?, in the above radicals, being identical or different and representing H or a C1-C12 alkyl or cycloalkyl radical; and Ar is a phenyl or Het., Het.

Abstract: The inventors have studied the kinetic and hierarchy of activation of apoptogenic caspases during myocardial ischemia and have found that caspase 2 plays a major role during the cardiac pathology by a very fast activation after an ischemic episode. Experiments were carried out on animal models of transitory or permanent myocardial ischemia. It was then observed that electrophysiological remodeling and post-ischemic fibrosis were prevented by using caspase-2 specific inhibitors. The invention is then based on the demonstration that caspase-2 and its activation represents an early and transitory step of the cardiac apoptotic mechanisms resulting from a myocardial ischemic and involved in the development of hypertrophy and cardiac insufficiency. The invention thus relates to a method of treatment of cardiovascular pathologies resulting from ischemia by using certain caspase-2 specific inhibitors.

Abstract: Inhibitors for preventing, blacking/silencing caspase-2 activity in cell death.

Abstract: The invention relates to selective new caspase-2 inhibitors that recognize caspase-2 and prevent and block its activity based on the following backbone: 2-Quinolinylcarbonyl-L-Valinyl-L-Aspartyl (methyl ester)-L-Vanilyl-L-Alaninyl-L-Aspartyl (methyl ester) 2,6-difluorophenyl ester (SEQ1) and derivatives thereof, SEQ 1 corresponding to formulae (Ia) or (Ib). Application of said inhibitors for preventing and treating diseases involving caspase-2.

Abstract: The invention relates to a method for screening modulators of mitochondrial function comprising adding a compound to be tested in a purified, isolated mitochondria preparation and simultaneously using fluorimetric analysis of mitochondrial morphology, and especially real-time fluorimetric analysis, combining analysis of morphometric parameters (SSC/FSC parameters) with analysis of membrane integrity by dye fluorescence. Application to the obtention of peptides which induce mitochondrial membrane permeabilization.

Abstract: The invention relates to cyclised peptides corresponding to sequence SEQ ID No1: X1X2RGDX3FGX4X5LLFIHFX6IGSX7HSX8IX9, wherein: the letters without any numerical index correspond to amino acids defined by the single-letter international code; X1 is G or GG having an amino-terminal end which may or may not be free; X2 is either a C, in which case X2=X4, the two Cs being connected by a disulphide bridge, or X2 is capable of forming a lactam bridge with X4, either X2 or X4 being an amino acid bearing an acid group, such as A or D, and the other bearing an amino function such as Q, N; X3 is either an M pattern or a norleucine pattern; X5 is one or several di-, tri-, or tetra-peptide patterns comprising G or a combination of G and S, or X5 is a C pattern having a side-chain which serves as a covalent linkage point with a 3-nitro-2-pyridinesulphenyl group which is located at the N-terminal end of the next amino acid (L); X6 is either an R pattern or a K pattern; X7 is either an R pattern or a K pattern; X8 is either

Abstract: Inhibitors for preventing, blacking/silencing caspase-2 activity in cell death.

Abstract: ARNi which can selectively inhibit expression of an isoform of ANT, characterized in that said ARNi are an ARN duplex, one of the strands being highly homologous to a fragment of ARNm coding for said isoform of ANT.

Abstract: The invention is directed to the induction of mitochondrial membrane permeabilization via the physical and functional interaction of the HIV-1 Vpr protein with the mitochondrial inner membrane protein ANT (adenine nucleotide translocator, also called adenine nucleotide translocase or ADP/ATP carrier). Reagents and methods for inducing and/or inhibiting the binding of Vpr to ANT, mitochondrial membrane permeabilization, and apoptosis are provided.