Abstract: Provided herein are MK2 activators, and compositions comprising an MK2 activator, for the treatment of a vascular disorder or an endothelial barrier disorder in a patient in need thereof, whereby the MK2 activator has a molecular weight below 1000 Da and binds to a binding pocket located on the C-lobe domain and C-terminal Regulatory Domain of MK2. Also provided are methods of treating a vascular disorder or an endothelial barrier disorder in a patient by administering to the patient an MK2 activator.

Abstract: The coronavirus SARS-Cov-2 which started in Wuhan, China, in December 2019 induced a threat to global health. Patients with mental disorders were thought to be at increased risk of becoming infected for several reasons but very much to the inventors' surprise, these psychiatric units remained nearly empty during the lock-down period as if psychiatric patients were protected from SARS-Cov-2 infection. Thus the inventors mined the literature to identify approved drugs with in vitro antiviral activities with a special emphasis on psychotropic drugs and compared these molecules using chemoinformatics strategies to the drugs most commonly used in their psychiatric department. A large number of compounds were found to be cationic amphiphilic drugs (CADs) and as such tend to also be phospholipidosis inducers in vitro (PLD). Several molecules most commonly used in their department were also found to have in vitro antiviral activity and/or can be clustered with compounds with known in vitro antiviral activity.

Abstract: The proprotein convertases (PCs) are implicated in the activation of various precursor proteins that play a crucial role in various cancers. Using structure-based virtual screening and a compound collection containing FDA approved drugs; the inventors identified Sulconazole as a small molecule able to repress furin activity. Moreover, the inventor show that Sulconazole is particularly suitable for repressing the expression of immune checkpoint protein (e.g. PD-1). 10 Therefore, Sulconazole would be particularly suitable for the treatment of disease involving furin activity in particular for the treatment of cancers.

Abstract: The invention relates to a compound inhibiting the interaction between a Grb14 protein and an insulin receptor of Formula (I) or Formula (II), their salts, solvates, and/or diastereoisomers, for use for therapeutic purposes, in particular for the treatment of insulin resistance, and to pharmaceutical compositions containing such compounds.

Abstract: The invention relates to a compound inhibiting the interaction between a Grb14 protein and an insulin receptor of Formula (I) or Formula (II), their salts, solvates, and/or diastereoisomers, for use for therapeutic purposes, in particular for the treatment of insulin resistance, and to pharmaceutical compositions containing such compounds.

Abstract: The present invention relates to polypeptides for the treatment of angiogenesis or lymphangiogenesis-related diseases. In particular, the present invention relates to a a polypeptide which comprises or consists of a sequence of at least 5 consecutive amino acids in SEQ ID NO: 1 and which comprises at least one amino acid selected from the group consisting of Q182, R184, Q195, T199.

Abstract: The present invention relates to the C-13 molecule (methyl 2-{5-[(3-benzyl-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]-2-furyl}-benzoate) and to organic molecules functionally equivalent to the C-13 molecule, capable of inhibiting the binding of an antibody or antibody fragment with the human Syk protein tyrosine kinase, to the use of these molecules for the production of medicaments for the prevention or treatment of diseases dependent on metabolic pathways involving Syk, and also to a method for identifying such molecules.

Abstract: The present invention relates to the C-13 molecule (methyl 2-{5-[(3-benzyl-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]-2-furyl}-benzoate) and to organic molecules functionally equivalent to the C-13 molecule, capable of inhibiting the binding of an antibody or antibody fragment with the human Syk protein tyrosine kinase, to the use of these molecules for the production of medicaments for the prevention or treatment of diseases dependent on metabolic pathways involving Syk, and also to a method for identifying such molecules.

Abstract: A method for treating and/or ameliorating and/or preventing a disease or a disorder, the method comprising administering to an individual in need thereof at least one nitrogen heterocycle derivative of formula (I): The at least one nitrogen heterocycle derivative may also be used as a proteasome activity modulator in the manufacture of a pharmaceutical composition intended to prevent and/or treat a disease condition mediated by the proteasome activity.

Abstract: The present invention relates to the C-13 molecule (methyl 2-{5-[(3-benzyl-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]-2-furyl}-benzoate) and to organic molecules functionally equivalent to the C-13 molecule, capable of inhibiting the binding of an antibody or antibody fragment with the human Syk protein tyrosine kinase, to the use of these molecules for the production of medicaments for the prevention or treatment of diseases dependent on metabolic pathways involving Syk, and also to a method for identifying such molecules.