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Solid Phase Synthesis and Self ‐Assembly of Higher‐Order siRNAs and their Bioconjugates
This article is protected by copyright. All rights reserved.
Source: Chemical Biology and Drug Design - November 27, 2018 Category: Biology Authors: Christopher N. Cultrara, Sunil Shah, Stephen D. Kozuch, Mayurbhai R. Patel, David Sabatino Tags: Special Issue Article Source Type: research

Nonsteroidal estrogen receptor isoform ‐selective biphenyls
Estrogen receptor (ER) has been a therapeutic target to treat ER‐positive breast cancer, most notably by agents known as selective estrogen receptor modulators (SERMs). However, resistance and severe adverse effects of known drugs gave impetus to the search for newer agents with better therapeutic profile. ERα and ERβ are two isoforms sharing 56% identity and having different physiological functions and expressions in various tissues. Only two residues differ in the active sites of the two isoforms motivating us to design isoform‐selective ligands. Guided by computational docking and molecular dynamics simulations, w...
Source: Chemical Biology and Drug Design - November 10, 2017 Category: Biology Authors: Seema Bhatnagar, Anjali Soni, Swati Kaushik, Megha Rikhi, Thankayyan Retnabai Santhoshkumar, Bhyravabhotla Jayaram Tags: RESEARCH ARTICLE Source Type: research

Non ‐steroidal Estrogen Receptor Isoform Selective Biphenyls
This article is protected by copyright. All rights reserved. Novel substituted biphenyl‐2,6‐diethanones are designed and synthesized targeting ERα isoform. MD simulations along with MM‐GBSA accounted for the binding selectivity of 3b towards ERα over ERβ. Co‐treatment and E‐screen studies indicated the ERα selective nature of 3b and anti‐estrogenicity. ERα siRNA silencing experiments further confirmed the isoform selectivity.
Source: Chemical Biology and Drug Design - October 20, 2017 Category: Biology Authors: Seema Bhatnagar, Anjali Soni, Swati Kaushik, Megha Rikhi, T R Santhosh Kumar, B. Jayaram Tags: Research Article Source Type: research

Amphiphilic small peptides for delivery of plasmid DNAs and siRNAs
This article is protected by copyright. All rights reserved. As novel nucleic acid carriers, linear and branched amphiphilic peptides were prepared. Each peptide was compared in terms of SNALP size, stability, and delivery activities for plasmid DNA (pDNA) and siRNA. Among the five peptides, a linear peptide H‐RCL was an effective delivery carrier for both siRNA and pDNA. Introduction of a benzoyl group to H‐RCL significantly enhanced siRNA delivery, but greatly reduced pDNA delivery. These demonstrated that a small structural modification of the peptides can modulate their delivery properties.
Source: Chemical Biology and Drug Design - October 20, 2017 Category: Biology Authors: Eun ‐Kyoung Bang, Hanna Cho, Sean S‐H Jeon, Na Ly Tran, Dong‐Kwon Lim, Wooyoung Hur, Taebo Sim Tags: Research Article Source Type: research

Therapeutic potential of chemically modified siRNA: Recent trends
This article is protected by copyright. All rights reserved. Ribose Modifications Phosphate Backbone Modifications Nucleobase Modifications Modification to the Termini and Conjugate groups siRNA Binding
Source: Chemical Biology and Drug Design - April 5, 2017 Category: Biology Authors: Chelliah Selvam, Daniel Mutisya, Sandhya Prakash, Kasturi Ranganna, Ramasamy Thilagavathi Tags: Review Source Type: research

siRNA ‐loaded liposomes: inhibition of encystment of Acanthamoeba and toxicity on the eye surface
This article is protected by copyright. All rights reserved. Glycogen phosphorilase, a key enzyme for encystment of Acanthamoeba,was silenced PEGylated cationic liposomes were used as carriers for siRNA delivery Ther was a significant reduction in the encystment of AP2 trophozoties
Source: Chemical Biology and Drug Design - January 29, 2017 Category: Biology Authors: Kathrin Faber, Giovanni K. Zorzi, Nathaly T. Brazil, Marilise B. Rott, Helder F. Teixeira Tags: Research Article Source Type: research

In Vivo RNAi Efficacy of Palmitic Acid‐Conjugated Dicer‐Substrate siRNA in a Subcutaneous Tumor Mouse Model
This article is protected by copyright. All rights reserved. We designed palmitic acid‐conjugated Dicer‐substrate 27‐nt siRNAs (C16‐Dsi27RNAs) and investigated their in vivo RNAi effects in a subcutaneous tumor mouse model. C16‐Dsi27RNAs had potent gene silencing activity against both eGFP and VEGF as target genes in a subcutaneous tumor mouse model generated from GCIY‐eGFP cells administered by intratumoral injection.
Source: Chemical Biology and Drug Design - January 23, 2016 Category: Biology Authors: Takanori Kubo, Kazuyoshi Yanagihara, Toshio Seyama Tags: Research Article Source Type: research

Systematic Comparisons of Formulations of Linear Oligolysine Peptides with siRNA and Plasmid DNA
This article is protected by copyright. All rights reserved. Linear oligolysine peptides with 16 or more lysines can effectively encapsulate plasmid DNA (pDNA) into monodisperse nanoparticles for gene transfer into the cells. However, the linear oligolysine peptides are not capable of forming monodisperse complexes with siRNA, hence they are ineffective in siRNA delivery into cells. Since the linear peptides have a limited rotation freedom, they are more suitable for cellular delivery of pDNA which has a higher rotation freedom than the more physically rigid siRNA.
Source: Chemical Biology and Drug Design - December 18, 2015 Category: Biology Authors: Albert Kwok, David McCarthy, Stephen L. Hart, Aristides D. Tagalakis Tags: Research Article Source Type: research

A Bifurcated Proteoglycan Binding Small Molecule Carrier for siRNA delivery
This article is protected by copyright. All rights reserved. A bifurcated guanidylated small molecule is modelled to access different clusters of sulphate esters in proteoglycans bound to the cell surface. Modular synthesis gives ready access to these molecules which have potential for the delivery of siRNA.
Source: Chemical Biology and Drug Design - January 28, 2014 Category: Biology Authors: Matt Gooding, Derick Adigbli, A. W. Edith Chan, Roberta J. Melander, Alexander J. MacRobert, David L. Selwood Tags: Research Article Source Type: research