Uptake mechanism of essential lysophospholipids into the brain and inhibition by endogenous-retroviral envelope protein
OwnerNicolas REYES, Maria MARTINEZ-MOLLEDOinventors
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Abstract
The disclosure provides the structure of an MFSD2A-SYNC2 complex together with functional data that revealed important molecular aspects of MFSD2A transport cycle, receptor-mediated cell-cell fusion, and pharmacology and resulted in the identification of two novel allosteric modulators of MFSD2A, which are two soluble fragments of SYNC2, namely SYNC2su-co and SYNC2su-co-2, representing first-in-class molecules to inhibit MFSD2A LPCs uptake and increase transcytosis rate.
Claims18
1-23. (canceled)
A polypeptide-drug conjugate comprising a polypeptide covalently linked to a drug, directly or through a linker, wherein the drug is a small molecule, an antibody, a DNA, or a RNA, a liposome, or a nanoparticle, and wherein the polypeptide comprises an isolated syncytin 2 (SYNC2) polypeptide fragment.
A method of transiently inhibiting MFSD2 Å transport function in the blood brain barrier (BBB) or transiently increasing vesicular transcytosis across BBB endothelium in a subject in need thereof, comprising administering to the subject an effective dose of an isolated syncytin 2 (SYNC2) polypeptide fragment.
A method of transiently increasing BBB permeability to deliver therapeutic small-compounds, macromolecules in particular antibodies, nanomaterials in particular liposomes or gene therapy, into the brain of a subject in need thereof, comprising administering to the subject an effective dose of an isolated syncytin 2 (SYNC2) polypeptide fragment.
Dependencies are inferred from the claim text.