107658-43-5
Chemical Structure
GALA
- CAS No.: 107658-43-5
- Formula:C136H215N33O45
- Molecular Weight:3032.36
SMILES: OC([C@H](C)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](C)NC([C@H](CCC(O)=O)NC([C@H](CC(C)C)NC([C@H](C)NC([C@H](CCC(O)=O)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](C)NC([C@H](CCC(O)=O)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](CC1=CN=CN1)NC([C@H](CCC(O)=O)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](C)NC([C@H](CCC(O)=O)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](C)NC([C@H](CCC(O)=O)NC([C@H](C)NC([C@H](CC(C)C)NC([C@H](C)NC([C@H](C)NC([C@H](CCC(O)=O)NC([C@@H](N)CC2=CNC3=CC=CC=C23)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O
Biological Activity: GALA is a pH-responsive amphipathic peptide consisting of 30 amino acids, which acts as a lung endothelium-targeting ligand. GALA undergoes a conformational transition from random coil to α-helix in an acidic environment at pH 5.0, thereby inducing endosomal membrane destabilization and fusion. GALA-modified liposomes traverse lung endothelial cells via clathrin-dependent endocytosis and transcytosis, and specifically accumulate in the lungs after intravenous injection. GALA significantly promotes the cytosolic release of cargos carried by exosomes, plasmids and liposomes, effectively enhances gene transfection efficiency, and drives gene knockdown of functional macromolecules (such as siRNA) in alveolar epithelial cells (with no significant cytotoxicity at effective concentrations). GALA serves as a critical tool for studies on lung cancer metastasis (e.g., melanoma lung metastasis) and lung-targeted drug delivery systems[1][2][3].
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GALA | 98.01% | GALA is a pH-responsive amphipathic peptide consisting of 30 amino acids, which acts as a lung endothelium-targeting ligand. GALA undergoes a conformational transition from random coil to α-helix in an acidic environment at pH 5.0, thereby inducing endosomal membrane destabilization and fusion. GALA-modified liposomes traverse lung endothelial cells via clathrin-dependent endocytosis and transcytosis, and specifically accumulate in the lungs after intravenous injection. GALA significantly promotes the cytosolic release of cargos carried by exosomes, plasmids and liposomes, effectively enhances gene transfection efficiency, and drives gene knockdown of functional macromolecules (such as siRNA) in alveolar epithelial cells (with no significant cytotoxicity at effective concentrations). GALA serves as a critical tool for studies on lung cancer metastasis (e.g., melanoma lung metastasis) and lung-targeted drug delivery systems. | ||||||||||||||||||||
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- [1]. Santiwarangkool S, et al. A study of the endocytosis mechanism and transendothelial activity of lung-targeted GALA-modified liposomes. J Control Release. 2019;307:55-63. [Content Brief]
- [2]. Nakase I, et al. Combined treatment with a pH-sensitive fusogenic peptide and cationic lipids achieves enhanced cytosolic delivery of exosomes. Sci Rep. 2015;5:10112. Published 2015 May 26. [Content Brief]
- [3]. Futaki S, et al. Unique features of a pH-sensitive fusogenic peptide that improves the transfection efficiency of cationic liposomes. J Gene Med. 2005;7(11):1450-1458. [Content Brief]
Keywords
