摘要:
The present invention relates to proteins and polypeptides that (i) have the formula A - [Wm - A]n where each A is independently a peptide of formula XXXXRXPXXXX where each X is independently any amino acid, R is arginine, and P is proline; each W is independently a linker; m is 1 or 2; and n is any number from 1 through 5; (ii) consist essentially of the formula XnRXPXm where each X is independently any amino acid, R is arginine, P is proline, n is any number from zero to fifteen, m is any number from zero to fifteen, and the sum of n and m is any number from eight to fifteen; (iii) have the formula A - An where each A is independently a peptide of formula XXXXRXPXXXX where each X is independently any amino acid, R is arginine, and P is proline; and n is any number from 1 through 5; or (iv) consist essentially of the formula XnRXPXm where each X is independently any amino acid, R is arginine, P is proline, n is any number from zero to seven, m is any number from zero to seven, and the sum of n and m is any number from zero to seven. Methods using these proteins and polypeptides to: identify the location of an RXP -binding domain of Cx43CT, modulate a Cx43 gap junction channel, screen for compounds that modulate Cx43CT, and measure Cx43CT-binding affinity of a compound that binds to Cx43CT, are also disclosed.
摘要:
The invention describes peptide analogues of a-melanocyte-stimulating hormone (a-MSH), which posses an increased efficay compared to the native α-MSH peptide. The α-MSH analogues exhibit increased anti-inflammatory effects and increased capability to prevent ischemic conditions compared to α-MSH. The invention further discloses use of the peptides for the manufacture of pharmaceutical compositions for the treatment or prophylaxis of a condition in the tissue of one or more organs of a mammal, and moreover pharmaceutical compositions.
摘要:
N- or C-terminally modified small peptides having antiarrhythmic properties are disclosed, and in particular to small peptides that possess improved pharmacokinetic properties such as have a reduced tendency to inhibit the activity of isozyme 3A4 of cytochrome P 450 oxidase. The invention further relates to uses of said compounds in the preparation of a medicament, and to pharmaceutical compositions comprising said compounds.
摘要:
Disclosed are novel peptides including antiarrhythmic peptides that have improved stability. Further disclosed are compositions that include such peptides and methods of using the compositions particularly as medicaments.
摘要:
Disclosed are novel peptides including antiarrhythmic peptides that have improved stability. Further disclosed are compositions that include such peptides and methods of using the compositions particularly as medicaments.
摘要:
Peptides X-AA1-AA2...AAn-Y, wherein AA is an L- or D-amino acid residue, X is hydrogen or an amino protective group, Y is OH, NH2 or an amino acid sequence comprising from 3 to 9 amino acid residues and n is an integer greater than 2, are prepared by solid phase synthesis, preferably using Fmoc-chemistry, the improvement consisting in that the C-terminal part attached to the solid phase comprises a pre-sequence comprising from 3 to 9, preferably from 5 to 7, amino acid residues independently selected from native L-amino acids having a side chain functionality which is suitably protected during the coupling steps and having a propensity factor P alpha > 0.57 and a propensity factor P beta > 1.10, preferably Lys and/or Glu, or the corresponding D-amino acids and said pre-sequence is optionally cleaved from the formed peptide.
摘要:
The invention provides materials and methods for promoting weight loss or preventing weight gain, and in the treatment of diabetes, metablic syndrome and associated disorders. In particular, the invention provides novel glucagon analogue peptides effective in such methods. The peptides may mediate their effect by having increased selectivity for the GLP-1 receptor as compared to human glucagon.
摘要:
Disclosed are peptides that facilitate the intercellular communication mediated by gap junctions. The invention has a wide spectrum of useful applications including use in the treatment of diseases associated with impaired gap junction intracellular communication (GJIC).
摘要:
The present invention relates to proteins and polypeptides that (i) have the formula A - [Wm - A]n where each A is independently a peptide of formula XXXXRXPXXXX where each X is independently any amino acid, R is arginine, and P is proline; each W is independently a linker; m is 1 or 2; and n is any number from 1 through 5; (ii) consist essentially of the formula X n RXPX m where each X is independently any amino acid, R is arginine, P is proline, n is any number from zero to fifteen, m is any number from zero to fifteen, and the sum of n and m is any number from eight to fifteen; (iii) have the formula A - A n where each A is independently a peptide of formula XXXXRXPXXXX where each X is independently any amino acid, R is arginine, and P is proline; and n is any number from 1 through 5; or (iv) consist essentially of the formula X n RXPX m where each X is independently any amino acid, R is arginine, P is proline, n is any number from zero to seven, m is any number from zero to seven, and the sum of n and m is any number from zero to seven. Methods using these proteins and polypeptides to: identify the location of an RXP -binding domain of Cx43CT, modulate a Cx43 gap junction channel, screen for compounds that modulate Cx43CT, and measure Cx43CT-binding affinity of a compound that binds to Cx43CT, are also disclosed.
摘要:
Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed.