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US 2021/0061883 A1Published application
Protease-activated receptor-2 modulators
AssigneeOasis Pharmaceuticals, LLC
InventorRichard J. Looby
Life of this patent
Estimating the term…
Abstract
Provided herein are peptides comprising a mutated fragment of a wild-type protease-activated receptor-2 (PAR2). The peptides comprising a hydrophobic moiety can penetrate the cell membrane and act as an antagonist of PAR2. Also provided herein are compositions and cells comprising the peptides and methods of using the peptides.
Claims29
A peptide comprising a sequence of:
- (SEQ ID NO:
- 42)
- X4X5X6X7X8X9X10X11X12X13X14X15X16X17X18X19X20,
- wherein:
- X4 is absent, A, G, P, or an N-terminal linker;
- X5 is M, G, P, I, L, V, norleucine (J), methionine sulfoxide (M(SO)), or methionine sulfone (M(SO2)), or absent when X4 is absent;
- X6 is D, E, H, or absent when X4 to X5 are absent;
- X7 is D, E, H, or absent when X4 to X6 are absent;
- X8 is N, D, or E;
- X9 is any amino acid;
- X10 is any amino acid;
- X11 is any amino acid or D-amino acid thereof, 2-aminoisobutyric acid (B), hydroxyproline (Hyp), P, a proline homolog , G, or rigidifier/helix-breaker moiety;
- X12 is K, R, P or absent;
- X13 is any amino acid or citrulline (Cit);
- X14 is K or any amino acid that makes the peptide bond between X13 and X14 uncleavable, or any amino acid that reduces positive charge;
- X15 is any amino acid, or beta-A;
- X16 is A, S, T, G, Q, beta-A, 2-aminoisobutyric acid (B), or absent;
- X17 is I, A, L, or V;
- X18 is K, I, or F;
- and
- X19 is a hydrophobic amino acid, a D-amino acid thereof, or absent.
18 more elements
2-59. (canceled)
A peptide comprising a sequence of SEQ ID NO:
- 41, wherein the amino acid sequence comprises a mutation at positions X5 and X15;
- and wherein the peptide is at least 15 amino acids in length.
A peptide comprising a sequence of SEQ ID NO:
- 41, wherein the amino acid sequence comprises a mutation at positions X5 and X15, and additional amino acids at X19 and X20, wherein X19 and X20 are independently a hydrophobic amino acid or a D-amino acid.
(canceled)
73-133. (canceled)
135-143. (canceled)
145-161. (canceled)
163-164. (canceled)
167-168. (canceled)
(canceled)
172-177. (canceled)
Dependencies are inferred from the claim text.