The disclosure relates to modulators and/or antagonists of insulin-insulin receptor signaling complexes and methods for selecting such modulators and/or antagonists. Such modulators and/or antagonists are characterized by, for example, type 2 diabetes, obesity, hyperglycemia, hyperinsulinemia, insulin overdose, chronic kidney disease, type 1 diabetes, insulin resistance and insulin resistance. It can be used to treat a mammalian subject suffering from a disease state and condition, or to prevent the onset of a subject at risk as described above. The disclosure provides novel modulators and/or antagonists of insulin-insulin receptor signaling complexes, methods for selecting such modulators and/or antagonists, and disease states and conditions characterized by abnormally increased production and/or utilization of insulin. The use of such modulators and/or antagonists for the treatment or prevention of conditions of endogenous hyperinsulinism, preferably congenital hyperinsulinism (CHI) is also provided.
The invention relates to the field of post-operative complications. The invention provides a source of autophagy-inhibiting amino acids for parenteral application as a medicament for use in at least a per-operative treatment of the vascular system to reduce duration of post-operative complications (POCs) in a subject. Each of said amino acids is selected from the group consisting of alanine (in one letter code: A), glutamine (Q), glycine (G), valine (V), leucine (L), isoleucine (I), proline (P) and arginine (R). The invention also provides methods for reducing duration of post-operative complications (POC) in a subject.
The invention relates to the field of post-operative complications. The invention provides a source of autophagy-inhibiting amino acids for parenteral application as a medicament for use in at least a per-operative treatment of the vascular system to reduce duration of post-operative complications (POCs) in a subject. Each of said amino acids is selected from the group consisting of alanine (in one letter code: A), glutamine (Q), glycine (G), valine (V), leucine (L), isoleucine (I), proline (P) and arginine (R). The invention also provides methods for reducing duration of post-operative complications (POC) in a subject.
The disclosure shows that inflammation in metabolic syndrome is augmented by and hitherto overlooked lock-and-key activation of the elastin receptor, a protein involved in vascular (blood vessel) inflammation and elastin repair, with the C-peptide, a small protein that is produced in a 1:1 ratio alongside with widely known insulin. The elastin receptor is the lock that is activated by a key motif of amino acids (PG-domain) found in C-peptide and in breakdown products (PG-domain-fragments) thereof. Until now, no one has ever discovered this lock-and-key interaction between the two, now providing novel development of novel peptides for treatment of metabolic syndrome, exploiting the finding that not only the normal keys of the elastin receptor (elastin peptides), but also the C-peptide, a peptide we produce together with insulin every time glucose rises in our blood after a meal, interacts in a lock-and-key mode with the elastin receptor.
C07K 14/705 - RécepteursAntigènes de surface cellulaireDéterminants de surface cellulaire
C07K 14/78 - Peptides du tissu connectif, p. ex. collagène, élastine, laminine, fibronectine, vitronectine ou globuline insoluble à froid [CIG]
G01N 33/566 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet utilisant un support spécifique ou des protéines réceptrices comme réactifs pour la formation de liaisons par ligand
G01N 33/577 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet faisant intervenir des anticorps monoclonaux
5.
ANGIOGENIC CONTROL, PREFERABLY COMBINED WITH GLYCAEMIC CONTROL
The invention relates to a distinct and newly emerging class of drugs: peptide modulators of mTOR that act as autophagy inhibiting compounds and target the nutrient sensing system of the mechanistic target of rapamycine (mTOR) and induce angiogenic activity. The invention provides formulations, methods, and means to prevent or treat vasculopathy, in particular diabetic vasculopathy, to achieve or maintain angiogenic control, preferably concomitant with glycaemic control.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
Methods for the treatment of diseases involving autophagy by leukocytes, preferably neutrophil cells, which process, according to the disclosure, is involved in mechanisms of tissue repair, vascular permeability and immune responses. The disclosure provides methods and means to target a chemoattractant receptor, preferably a leukocyte cell-surface receptor specifically and to provide molecules and compositions comprising a specific targeting agent as well as amino acid compositions that are involved in the pathway of autophagy and the diseases related thereto. The disclosure also relates to peptide drug development, in particular, to (the improvement of) autophagy inhibiting amino acid containing peptides, more in particular, glutamine-containing peptides and/or glutamine and other autophagy-modulating amino acid containing compositions useful in the treatment of vascular and inflammatory conditions.
A61K 47/10 - AlcoolsPhénolsLeurs sels, p. ex. glycérolPolyéthylène glycols [PEG]PoloxamèresAlkyléthers de PEG/POE
A61K 47/68 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un anticorps, une immunoglobuline ou son fragment, p. ex. un fragment Fc
C07K 7/08 - Peptides linéaires ne contenant que des liaisons peptidiques normales ayant de 12 à 20 amino-acides
C07K 14/00 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés
7.
PEPTIDE MODULATORS OF THE INTERACTION BETWEEN HUMAN C-PEPTIDE AND HUMAN ELASTIN RECEPTOR FOR THERAPEUTIC USE
The present disclosure shows that inflammation in metabolic syndrome is augmented by and hitherto overlooked lock-and-key activation of the elastin receptor, a protein involved in vascular (blood vessel) inflammation and elastin repair, with the C-peptide, a small protein that is produced in a 1:1 ratio alongside with widely known insulin. The elastin receptor is the lock that is activated by a key motif of amino acids (PG-domain) found in C-peptide and in breakdown products (PG-domain-fragments) thereof. Until now, no one has ever discovered this lock-and-key interaction between the two, now providing novel development of novel peptides for treatment of metabolic syndrome, exploiting the finding that not only the normal keys of the elastin receptor (elastin peptides), but also the C-peptide, a peptide we produce together with insulin every time glucose rises in our blood after a meal, interacts in a lock-and-key mode with the elastin receptor.
G01N 33/53 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet
G01N 33/566 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet utilisant un support spécifique ou des protéines réceptrices comme réactifs pour la formation de liaisons par ligand
G01N 33/577 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet faisant intervenir des anticorps monoclonaux
8.
AUTOPHAGY-INHIBITING PEPTIDE AND ORGANIC ACID SALT THEREOF ADDRESSING ISSUES OF VASCULAR PERMEABILITY
The invention relates generally to biotechnology and medicine and to sources and salts of autophagy inhibiting peptides useful as pharmaceutical compounds. In particular, the invention provides method for reducing formyl-peptide-receptor (FPR) mediated p38 MAPK kinase activity of cells comprising providing said cells with a source of amino acids said source comprising at least 50%, more preferably at least 75%, most preferably at 100% amino acids selected from the group of autophagy inhibiting amino acids alanine (in one letter code: A), glutamine (Q), glycine (G), valine (V), leucine (L), proline (P), and arginine (R).
The disclosure relates to modulators and / or antagonists of insulin-insulin receptor signaling complexes and methods for selecting such modulators and / or antagonists. Such modulators and / or antagonists are characterized by, for example, type 2 diabetes, obesity, hyperglycemia, hyperinsulinemia, insulin overdose, chronic kidney disease, type 1 diabetes, insulin resistance and insulin resistance. It can be used to treat a mammalian subject suffering from a disease state and condition, or to prevent the onset of a subject at risk as described above. The disclosure provides novel modulators and / or antagonists of insulin-insulin receptor signaling complexes, methods for selecting such modulators and / or antagonists, and disease states and conditions characterized by abnormally increased production and / or utilization of insulin. The use of such modulators and / or antagonists for the treatment or prevention of conditions of endogenous hyperinsulinism, preferably congenital hyperinsulinism (CHI) is also provided.
Provided is a method of treatment comprising administering an AQGV peptide, or a functional analogue thereof, to a human subject, the human subject suffering from an infection, particularly a respiratory infection, more specifically, a viral infection, more in particular, a Corona virus infection, wherein the treatment of administering an AQGV peptide comprises maintaining or improving hemodynamic stability in the human subject.
Means and methods for treating diseases involving autophagy by cells, which is involved in mechanisms of tissue repair, vascular permeability and immune responses. Described are methods and means to target the elastin receptor complex specifically and to provide molecules and compositions comprising a specific targeting agent as well as amino acid compositions that are involved in the pathway of autophagy and the diseases related thereto. Also, peptide-drug development, in particular, to (the improvement of) autophagy inhibiting amino acid containing peptides, more, in particular, glutamine-containing peptides and/or glutamine and other autophagy modulating amino acid containing compositions useful in the treatment of vascular and inflammatory conditions. Improvement of glutamine peptides useful in the treatment of diabetic, vascular and/or inflammatory conditions. A Q-ER peptide, comprising a synthetic peptide or functional analogue thereof provided with at least one PG-domain amino acid motif xGxxPG or functional equivalent thereof, the PG-domain motif allowing targeting of the peptide to the elastin receptor complex (ER), wherein at least one amino acid at position x is selected from A, Q, G, V, L, I, P, and R.
A61K 47/68 - Préparations médicinales caractérisées par les ingrédients non actifs utilisés, p. ex. les supports ou les additifs inertesAgents de ciblage ou de modification chimiquement liés à l’ingrédient actif l’ingrédient non actif étant chimiquement lié à l’ingrédient actif, p. ex. conjugués polymère-médicament l’ingrédient non actif étant un agent de modification l’agent de modification étant un anticorps, une immunoglobuline ou son fragment, p. ex. un fragment Fc
A61K 9/127 - Vecteurs à bicouches synthétiques, p. ex. liposomes ou liposomes comportant du cholestérol en tant qu’unique agent tensioactif non phosphatidylique
The invention relates to a distinct and newly emerging class of drugs: peptide modulators of mTOR that act as autophagy inhibiting compounds and target the nutrient sensing system of the mechanistic target of rapamycine (mTOR) and induce angiogenic activity. The invention provides formulations, methods, and means to prevent or treat vasculopathy, in particular diabetic vasculopathy, to achieve or maintain angiogenic control, preferably concomitant with glycaemic control.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
The invention relates to a distinct and newly emerging class of drugs: peptide modulators of mTOR that act as autophagy inhibiting compounds and target the nutrient sensing system of the mechanistic target of rapamycine (mTOR) and induce angiogenic activity. The invention provides formulations, methods, and means to prevent or treat vasculopathy, in particular diabetic vasculopathy, to achieve or maintain angiogenic control, preferably concomitant with glycaemic control.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
Abstract The invention relates to means and methods for the treatment of diseases involving autophagy by leukocytes, preferably neutrophil cells, which process according to the invention is involved in mechanisms of tissue repair, vascular permeability and immune responses. The invention provides methods and means to target a chemoattractant receptor, preferably a leukocyte cell-surface receptor specifically and to provide molecules and compositions comprising a specific targeting agent as well as amino acid compositions that are involved in the pathway of autophagy and the diseases related thereto. The disclosure also relates to peptide-drug development, in particular to (the improvement of) autophagy inhibiting amino acid containing peptides, more in particular glutamine-containing peptides and/or glutamine and other autophagy modulating amino acid containing compositions useful in the treatment of vascular and inflammatory conditions.
A61K 38/17 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'animauxPeptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés provenant d'humains
C07K 14/00 - Peptides ayant plus de 20 amino-acidesGastrinesSomatostatinesMélanotropinesLeurs dérivés
C07K 7/06 - Peptides linéaires ne contenant que des liaisons peptidiques normales ayant de 5 à 11 amino-acides
C07K 7/08 - Peptides linéaires ne contenant que des liaisons peptidiques normales ayant de 12 à 20 amino-acides
16.
AUTOPHAGY-INHIBITING PEPTIDE AND ORGANIC ACID SALT THEREOF ADDRESSING ISSUES OF VASCULAR PERMEABILITY
The invention relates generally to biotechnology and medicine and to sources and salts of autophagy inhibiting peptides useful as pharmaceutical compounds. In particular, the invention provides method for reducing formyl-peptide-receptor (FPR) mediated p38 MAPK kinase activity of cells comprising providing said cells with a source of amino acids said source comprising at least 50%, more preferably at least 75%, most preferably at 100% amino acids selected from the group of autophagy inhibiting amino acids alanine (in one letter code: A), glutamine (Q), glycine (G), valine (V), leucine (L), proline (P), and arginine (R).
The invention relates generally to biotechnology and medicine and to sources and salts of autophagy inhibiting peptides useful as pharmaceutical compounds. In particular, the invention provides method for reducing formyl-peptide-receptor (FPR) mediated p38 MAPK kinase activity of cells comprising providing said cells with a source of amino acids said source comprising at least 50%, more preferably at least 75%, most preferably at 100% amino acids selected from the group of autophagy inhibiting amino acids alanine (in one letter code: A), glutamine (Q), glycine (G), valine (V), leucine (L), proline (P), and arginine (R).
Provided is a method of treatment comprising administering an AQGV peptide, or a functional analogue thereof, to a human subject, the human subject suffering from an infection, particularly a respiratory infection, more specifically a viral infection, more in particular a Corona virus infection, wherein the treatment of administering an AQGV peptide comprises maintaining or improving hemodynamic stability in the human subject.
Provided is a method of treatment comprising administering an AQGV peptide, or a functional analogue thereof, to a human subject, the human subject suffering from an infection, particularly a respiratory infection, more specifically a viral infection, more in particular a Corona virus infection, wherein the treatment of administering an AQGV peptide comprises maintaining or improving hemodynamic stability in the human subject.
The invention relates to means and methods for the treatment of diseases involving autophagy by cells, which process according to the invention is involved in mechanisms of tissue repair, vascular permeability and immune responses. The invention provides methods and means to target the elastin receptor complex specifically and to provide molecules and compositions comprising a specific targeting agent as well as amino acid compositions that are involved in the pathway of autophagy and the diseases related thereto. The disclosure also relates to peptide-drug development, in particular to (the improvement of) autophagy inhibiting amino acid containing peptides, more in particular glutamine-containing peptides and/or glutamine and other autophagy modulating amino acid containing compositions useful in the treatment of vascular and inflammatory conditions. The invention further relates to the improvement of glutamine peptides useful in the treatment of diabetic, vascular and/or inflammatory conditions. The invention provides a Q- ER peptide, comprising a synthetic peptide or functional analogue thereof provided with at least one PG-domain amino acid motif xGxxPG or functional equivalent thereof, said PG- domain motif allowing targeting of said peptide to the elastin receptor complex (ER), wherein at least one amino acid at position x is selected from the group of amino acids alanine (in one letter code: A), glutamine (Q), glycine (G), valine (V), leucine (L), isoleucine (I), proline (P) and arginine, said peptide provided with at least one glutamine (Q).
The invention relates to means and methods for the treatment of diseases involving autophagy by cells, which process according to the invention is involved in mechanisms of tissue repair, vascular permeability and immune responses. The invention provides methods and means to target the elastin receptor complex specifically and to provide molecules and compositions comprising a specific targeting agent as well as amino acid compositions that are involved in the pathway of autophagy and the diseases related thereto. The disclosure also relates to peptide-drug development, in particular to (the improvement of) autophagy inhibiting amino acid containing peptides, more in particular glutamine-containing peptides and/or glutamine and other autophagy modulating amino acid containing compositions useful in the treatment of vascular and inflammatory conditions. The invention further relates to the improvement of glutamine peptides useful in the treatment of diabetic, vascular and/or inflammatory conditions. The invention provides a Q- ER peptide, comprising a synthetic peptide or functional analogue thereof provided with at least one PG-domain amino acid motif xGxxPG or functional equivalent thereof, said PG- domain motif allowing targeting of said peptide to the elastin receptor complex (ER), wherein at least one amino acid at position x is selected from the group of amino acids alanine (in one letter code: A), glutamine (Q), glycine (G), valine (V), leucine (L), isoleucine (I), proline (P) and arginine, said peptide provided with at least one glutamine (Q).
The invention shows that inflammation in metabolic syndrome is augmented by an hitherto overlooked lock- and-key activation of the elastin receptor, a protein involved in vascular (blood vessel) inflammation and elastin repair, with the C-peptide, a small protein that is produced in a 1:1 ratio alongside with widely known insulin. The elastin receptor is the lock that is activated by a key motif of amino acids (PG-domain) found in C-peptide and in breakdown products (PG-domain-fragments) thereof. Until now, no one has ever discovered this lock-and-key interaction between the two, now providing novel development of novel peptides for treatment of metabolic syndrome, exploiting the finding that not only the normal keys of the elastin receptor (elastin peptides), but also the C-peptide, a peptide we produce together with insulin every time glucose rises in our blood after a meal, interacts in a lock-and-key mode with the elastin receptor.
The invention shows that inflammation in metabolic syndrome is augmented by an hitherto overlooked lock- and-key activation of the elastin receptor, a protein involved in vascular (blood vessel) inflammation and elastin repair, with the C-peptide, a small protein that is produced in a 1:1 ratio alongside with widely known insulin. The elastin receptor is the lock that is activated by a key motif of amino acids (PG-domain) found in C-peptide and in breakdown products (PG-domain-fragments) thereof. Until now, no one has ever discovered this lock-and-key interaction between the two, now providing novel development of novel peptides for treatment of metabolic syndrome, exploiting the finding that not only the normal keys of the elastin receptor (elastin peptides), but also the C-peptide, a peptide we produce together with insulin every time glucose rises in our blood after a meal, interacts in a lock-and-key mode with the elastin receptor.
The invention relates to methods for determining whether a peptide is capable of modulating signalling via at least one Pattern Recognition Receptor (PRR) signalling pathway and/or G protein coupled receptor (GPCR) signalling pathway, the method comprising providing a cell susceptible to signalling through at least one of said pathways, contacting said cell with at least one dipeptide, contacting said cell with an agonistic or antagonistic compound of a PRR and/or a GPCR of said pathway, and determining the activity of said at least one signalling pathway in said cell. The invention further relates to use of peptides in therapeutic applications where modulation of at least one PRR and/or GPCR signalling pathway is desirable.
G01N 33/50 - Analyse chimique de matériau biologique, p. ex. de sang ou d'urineTest par des méthodes faisant intervenir la formation de liaisons biospécifiques par ligandsTest immunologique
G01N 33/569 - Tests immunologiquesTests faisant intervenir la formation de liaisons biospécifiquesMatériaux à cet effet pour micro-organismes, p. ex. protozoaires, bactéries, virus
A61K 31/00 - Préparations médicinales contenant des ingrédients actifs organiques
Methods of treating radiation injury of a subject in need thereof comprising administering to the subject a peptide consisting of an amino acid molecule selected from the group consisting of VVC, LAG, AQG, LQGV, QVVC, MTRV, LAGV, LQAV, PGCP, VGQL, RVLQ, EMFQ, AVAL, FVLS, NMWD, LCFL, FSYA, FWVD, AFTV, LGTL, QLLG, YAIT, APSL, ITTL, QALG, GVLC, NLIN, SPIE, LNTI, LHNL, CPVQ, EVVR, MTEV, EALE, EPPE, LGTL, VGGI, RLPG, LQGA, LCFL, TLAVE, VEGNL, LNEAL, CPRGVNP, MGGTWA, LTCDDP, VCNYRDV, QPLAPLVG, and DINGFLPAL. The invention provides for administration of the peptide prior to and following exposure of the subject to a source of radiation.
The invention relates generally to biotechnology, and more specifically to in silico methods of identifying lead molecules that have an increased probability of becoming an approved medicament, and business methods of identifying molecules such that they have an increased probability of becoming an approved medicament. Provided is a method for identifying a biologically active peptide consisting of two to seven amino acid residues, comprising the steps of providing a database comprising a plurality of naturally occurring polypeptide sequences; defining at least one peptide motif that satisfies certain defined criteria; and determining for the defined peptide motif its frequency of occurrence among the polypeptide sequences in the database and correlating the frequency with the biological activity of the peptide.
G06F 19/22 - pour la comparaison de séquences impliquant des nucléotides ou des acides aminés, p.ex. recherche d'homologie, identification de motifs ou de polymorphismes de nucléotides simples [SNP] ou alignement de séquences
G06F 19/18 - pour la génomique ou la protéomique fonctionnelle, p.ex. associations génotype-phénotype, déséquilibre de liaison, mutagénèse, génotypage ou annotation génomique, interactions protéines-protéines ou interactions protéines-acides nucléiques
G06F 19/28 - pour la programmation d'outils ou de systèmes de bases de données, p.ex. ontologies, intégration de données hétérogènes, entreposage de données ou architectures informatiques
27.
INHIBITION OF RENAL ISCHEMIA REPERFUSION INJURY BY SYNTHETIC OLIGOPEPTIDES
The invention relates to the field of medicine. In particular, it relates to the therapeutic use of synthetic oligopeptides capable of inducing cell regeneration, for instance in the treatment of ischemic renal injury. Provided is the use of the peptide AQGV for the preparation of a medicament for the treatment of a subject in need of cell regeneration. Also provided is a method for the treatment of a subject in need of cell regeneration, comprising administering to said subject a therapeutically effective dose of the peptide AQGV together with a pharmaceutically acceptable carrier.
Described are methods and associate means for treating a subject, such as a mammal, experiencing or thought to be at risk for hemorrhagic shock. Such methods include administering, to the subject in a medically acceptable manner, a short oligopeptide such as AQGV and/or LQGV.
Methods of treating radiation injury of a subject in need thereof comprising administering to the subject a peptide consisting of the amino acid sequence AQGV. The invention provides for administration of the amino acid composition prior to and following exposure of the subject to a source of radiation.
brevets
