Patents

US10208098: Recombinant protein-based method for the delivery of silencer RNA to target the brain

The invention relates to the design and development of recombinant protein for the delivery of silencer RNA complex to mediate RNA interference since it represents a novel therapeutic approach to modulate several neurodegenerative disease-related genes across the Blood-Brain Barrier (BBB). To overcome challenges due to this barrier for biologics and other biological complex, the invention describes a method wherein peptide having sequence GGGGHLNILSTLWKYRC represented by SEQ ID NO. 9 known to target specific gangliosides was linked to a double-stranded RNA binding protein to bind and deliver silencer RNA to the brain parenchyma. The designed fusion protein comprising a double-stranded RNA-binding domain (dsRBD) of human Trans Activation Response element (TAR) RNA Binding Protein (TARBP2) and a brain targeting peptide sequence that binds GM1. Conformation-specific binding of TARBP2 domain to silencer RNA results in the formation of homogenous serum-stable complex with GM1 targeting potential. Uptake of the complex in neural cells reveals selective requirement of GM1 for entry. Remarkably, the invention pertains to the systemic delivery of the complex comprising TARBP-BTP and silencer RNA in A?PP-PS1 mouse model of Alzheimer's disease (AD) led to distinctive localization primarily in the cerebral hemisphere in the hippocampus and brain cortex and in principle can work across other mammalian CNS targets. Further, the delivery of silencer-RNA mediated by brain targeting peptide fusion led to significant knockdown of BACE1, a therapeutic protease target in both A?PP-PS1 and wild type C57BL/6 mice. The invention establishes the emergent importance of fusion proteins in delivering therapeutic siRNA as a simple complex to brain tissues to treat neurodegenerative diseases besides Alzheimer's disease (AD). The complex is also useful to study gene function of hitherto unidentified genes/interplay of genes in mammalian systems and central nervous system. 

Filing Date: 16-09-2015

Issue Date: 19-02-2019

Applicant: CSIR–Centre for Cellular and Molecular Biology (CSIR-CCMB), Hyderabad

Patent No: US10208098

Application No: 15/266642

Inventor(s): Gopal Vijaya; Ghulam Hassan Dar

IPC Classification: C07K 14/47, A61K 47/42, A61K 47/34, A61K 31/7105, C12N 15/113, C12N 15/87, C12N 15/11

Country: United States of America

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