Abstract: A peptide including a first peptide sequence of formula KLAKLAK (SEQ ID NO:11)in which K is lysine, L is leucine and A is alanine, and a second peptide sequence of formula (B) in which B is a peptide of 4 to 15 amino acids positively charged at neutral pH, including at least one peptide motif of formula ?xx? (SEQ ID NO:13)in which ? is a basic amino acid and X is any amino acid, and in which the first peptide sequence is repeated n times and the second peptide sequence is repeated m times, n and m being whole numbers between 1 and 5.
Abstract: The present invention relates to a method for the preparation of a compound of formula (I) or pharmaceutically acceptable salts thereof and intermediates thereof, comprising the steps of: a) halogenating a compound of formula (II), resulting in compound of formula (IIa), b) reacting a compound of formula (IIa) at its 14 position with the thiol moiety of a peptide of formula (III), optionally in the presence of a suitable linker, to obtain said compound of formula (I), wherein R1 represents OH, NH2 or NH-peptide; R2 represents H or —CO-peptide; R3 represents OCH3, OH or H; R4 represents H, or COCF3; R5 represents OH, O-tetrahydropyranyl or H; R6 represents OH or H; R7 represents H, OH, OCO(CH2)3CH3 or OCOCH(OC2H5)2; R8 represents OH or H; R9 represents OH or H; R10 represents a halogen and L is an optional suitable linker arm.
Type:
Application
Filed:
September 30, 2009
Publication date:
February 11, 2010
Applicants:
Universite Catholique de Louvain, Diatos S. A.
Abstract: The present invention relates to a novel compound of use in the improved delivery of therapeutic drug agents into target cells or tissues, composition comprising the same and uses thereof. The compound is more specifically a conjugate of a peptide moiety and a camptothecin, a derivative or analog thereof which provides numerous benefits, including enhancement in terms of aqueous solubility, pharmacokinetics and tissue distribution, enlargement of the therapeutic index, and limitation of the inter-patient metabolic variability, as well as improvement of delivery of the biologically active ingredient to the target cells or tissues.
Abstract: This invention relates to the field of antibody-drug conjugates, and more particularly antibody-drug conjugates that are intended for the treatment and/or diagnosis of diseases such as tumors and/or inflammatory reactions.
Abstract: The present invention relates to an amino acid sequence being able to facilitate penetration of a substance of interest inside cells and/or cell nuclei and having the following formula (I) [(X1)p [(X)o (B)nX B X X B]m (X2)q wherein X1 and X2 are amino acid sequences of 1 to 20 amino acids; p and q are whole numbers between 0 and 5; B is a basic amino acid; X is a non-basic, preferably hydrophobic amino acid, such as alanine, isoleucine, leucine, methionine, phenylalanine, tryptophan, valine or tyrosine; n is 2 or 3; m is 1 to 4; o is 0 or 1, between 0 and 5; B is a basic amino acid; X is a non-basic, preferably hydrophobic amino acid, such as alanine, isoleucine, leucine, methionine phenylalanine, tryptophan, valine or tyrosine; n is 2 or 3; m is 1 to 4; o is 0 or 1.
Abstract: The invention relates generally to chimeric peptides and compositions that facilitate the transport of insulin across biological membranes, methods for preparing the chimeric peptides, and a method for treating a subject suffering from diabetes.
Abstract: The invention relates generally to chimeric peptides and compositions that facilitate the transport of insulin across biological membranes, methods for preparing the chimeric peptides, and a method for treating a subject suffering from diabetes.
Abstract: A peptide including a first peptide sequence of formula KLAKLAK in which K is lysine, L is leucine and A is alanine, and a second peptide sequence of formula (B) in which B is a peptide of 4 to 15 amino acids positively charged at neutral pH, including at least one peptide motif of formula ?xx? in which ? is a basic amino acid and X is any amino acid, and in which the first peptide sequence is repeated n times and the second peptide sequence is repeated m times, n and m being whole numbers between 1 and 5.