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• W2912853931 abstract "The safe and effective intracellular delivery of functional biopharmaceuticals remains amajor concern for the pharmaceutical industries. The main aim of this thesis is to develop improvedpeptide based molecular transporters for intracellular delivery of small molecule and largebiopharmaceutical based cargos, in functional form in breast cancer cells. Chapter 1 reviews thecurrent literature of the structural and functional features of molecular transporters and theirlimitations. This introductory chapter provides a framework for designing peptide based moleculartransporters for developing next generation therapeutics. Chapter 2 describes membrane activepeptide gramicidin-inspired designed alternating L,D-peptides for delivering hydrophilic andhydrophobic drugs in breast cancer cells. Chapter 3-5 describe natural TAT-peptide inspireddesigned arginine rich molecular transporters for intracellular delivery of biopharmaceuticals.Here, we have examined the proteolytically stable backbone structures of library of moleculartransporters and evaluated their efficacies. In Chapter 3, we have designed protease-resistantarginine-rich facial peptides (SPP8, SPP16 and SPP9) having arginine-sarcosine-arginine (Arg-Sar-Arg) template as molecular transporters. Interestingly, our designed lipopeptide (SPP9) havingtwo stearyl moieties exhibited significantly higher cellular internalization of cargo with only sixL-arginine residues compared to linear oligoarginine peptide, R9 and stearylated oligo-nonaarginine(stearyl-R9) peptide. To further enhance the cytosolic cargo internalization, we designedand examined the efficacy of cyclic molecular transporters. In Chapter 4, we have engineeredcyclic peptide based molecular transporters (SPP5, SPP10, SPP13 and SPP18) having Arg-Sar-Arg template. Our designed cyclic lipopeptide SPP18 showed better internalization of siRNA thancyclic-Arg9 peptide and commercial transfection agent Hiperfect. However, SPP18 and its linearcounterpart, SPP9, showed similar siRNA internalization and exhibited significant gene silencingefficiency as evidenced by RT-PCR experiment. To facilitate the release of cargo from endosomalentrapment and improve the cargo internalization, we examined the effect of insertion of both LandD-histidine residues in designed cyclic peptide backbone. In Chapter 5, we have designedand studied cyclic peptide based molecular transporters (SPP22, SPP21, SPP14 and SPP23) havingarginine-(L/D)histidine-arginine (Arg-L/D-His-Arg) motif. We also examined the insertion oflinoleic acids as lipophilic moiety in our designed lipopeptide. Interestingly, our designed lipopeptide based molecular transporters, SPP21, SPP22, SPP14 and SPP23 showed higher siRNAdelivery efficiency in MDA-MB-231 cell lines than commercially available transfection agentHiperfect or cyclic-Arg9 peptide. RT-PCR data suggests SPP21, SPP14 and Hiperfect exhibitsignificant gene silencing inferring functional delivery of siRNA. Double lipidated peptides SPP21and SPP14 having Arg-D-His-Arg motif exhibited significant cytosolic delivery of cargocompared to double stearylated peptide SPP23 having Arg-L-His-Arg motif. The proteolyticinstability of SPP23 probably contributes to reduced cytosolic delivery. We anticipate that cyclicpeptides SPP18 and SPP21 and linear peptide SPP9 might be translated into clinics to developsiRNA based nanotherapeutics." @default.
• W2912853931 created "2019-02-21" @default.
• W2912853931 creator A5020086176 @default.
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• W2912853931 date "2018-04-01" @default.
• W2912853931 modified "2023-09-24" @default.
• W2912853931 title "Nature-Inspired Designed NanostructuredPeptides as Molecular Transporters" @default.
• W2912853931 hasPublicationYear "2018" @default.
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