Compounds and use thereof to modify transport across cell membranes
AssigneeBiotransys Limited
InventorsRoy Harris, Paul O'Shea
Life of this patent
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Abstract
The invention provides the use of a compound capable of preferential interaction with plasma membrane lipid microdomains (PMLMs) as enhancers of transport processes across endothelial, epithelial and mesothelial membranes (ie including blood-brain-blood barrier and gastrointestinal mucosal membranes). When associated with therapeutic agents, the compounds act as transport vehicles. When the compounds interact with PMLMs in such a way as to inhibit transport across the membrane, the compounds function as anti-infective agents.
Claims22
The use of a compound which interacts preferentially with PMLMs to modify transport processes across an endothelial, epithelial or mesothelial membrane.
Use as claimed in any preceding claim, wherein the compound has the formula BVS-Gen1:
- BVS-Gen1:POS-Pol1-HYD-Pol2-NEG
- in which
- POS represents an amino acid residue including the N-terminal positive charge,
- Pol1 represents a short sequence of polar, possibly including positively charged, residues,
- HYD represents a hydrophobic amino acid sequence (ie more than one and typically up to five residues), optionally substituted or interrupted by one or more polar groups,
- Pol2 represents a short sequence of polar, possibly including positively charged, residues, and
- NEG represents a negatively charged amino acid residue including the carboxylate terminus.
A pharmaceutical composition comprising at least one therapeutically active agent and a compound capable of preferential interaction with PMLMs.
A conjugate of a therapeutically active agent with a compound capable of preferential interaction with PMLMs.
A method of enhancing transport across an endothelial, epithelial or mesothelial cellular membrane, which method comprises administering to the membrane a compound capable of preferential interaction with PMLMs.
A method of inhibiting infection by administering to the membrane a compound capable of preferential interaction with PMLMs so as to inhibit transport across the membrane.
A compound of the formula BVS-Gen1:
- BVS-Gen1:POS-Pol1-HYD-Pol2-NEG
- in which
- POS represents an amino acid residue including the N-terminal positive charge,
- Pol1 represents a short sequence of polar, possibly including positively charged, residues,
- HYD represents a hydrophobic amino acid sequence (ie more than one and typically up to five residues), optionally substituted or interrupted by one or more polar groups,
- Pol2 represents a short sequence of polar, possibly including positively charged, residues, and
- NEG represents a negatively charged amino acid residue including the carboxylate terminus.
A compound selected from the group consisting of
- 5 BVS3 GFLGFLAVVFLG BVS4 FVLGFVGLFLGA BVS5 GVFVLGLFGFLA BVS6 GVFVLFGLGFLA BVS7 GVAVLGALGFLA BVS8 GVAVLGFLGALA BVS9 GVFVLGFLGFLATAGS BVS10 GVFVLFLGFLATAGSAMGAASLTV BVS11 GVFVLGFLGFLATAGSAMGAASLT BVS12 GVFVLGFLGFLTTAGAAMGAASLT BVS13 GVLVLGFLGFLTTAGAAMGAASLT BVS14 AIGALFLGFLGAAG BVS15 AGALFLGFLGAAG BVS16 AGIGALFLGFLGAAG BVS17 GVFVGFLGFLTTAGAAMGAASLTL
Dependencies are inferred from the claim text.