scholarly journals Tuning of endosomal escape and gene expression by functional groups, molecular weight and transfection medium: a structure–activity relationship study

2020 ◽  
Vol 8 (23) ◽  
pp. 5026-5041 ◽  
Author(s):  
Friederike Richter ◽  
Liam Martin ◽  
Katharina Leer ◽  
Elisabeth Moek ◽  
Franziska Hausig ◽  
...  
Keyword(s):  
Gene Expression ◽  
Molecular Weight ◽  
Gene Delivery ◽  
Functional Groups ◽  
Endosomal Escape ◽  
Specific Lipids ◽  
Structure Activity ◽  
Transfection Medium ◽  
Relationship Study ◽  
Endosomal Release

A library of cationic polyacrylamide homopolymers was synthesized and their gene delivery, endosomal release, and interaction with endosome-specific lipids were investigated. The guanidinium-containing polymers were most efficient.

scholarly journals Cyclodextrin- and calixarene-based polycationic amphiphiles as gene delivery systems: a structure–activity relationship study

2015 ◽  
Vol 13 (6) ◽  
pp. 1708-1723 ◽  
Author(s):  
Laura Gallego-Yerga ◽  
Michela Lomazzi ◽  
Valentina Franceschi ◽  
Francesco Sansone ◽  
Carmen Ortiz Mellet ◽  
...  
Keyword(s):  
Gene Delivery ◽  
Structure Activity Relationship ◽  
Delivery Systems ◽  
Activity Relationship ◽  
Structure Activity ◽  
Relationship Study

Multi-head/multi-tail facial amphiphiles built on cyclodextrin (CD) and calixarene (CA) scaffolds are paradigmatic examples of monodisperse gene delivery systems.

Enhanced gene expression and reduced toxicity in mice using polyplexes of low-molecular-weight poly(ethylene imine) for pulmonary gene delivery

2009 ◽  
Vol 17 (8) ◽  
pp. 638-651 ◽  
Author(s):  
Elke Kleemann ◽  
Norman Jekel ◽  
Lea Ann Dailey ◽  
Susanne Roesler ◽  
Ludger Fink ◽  
...  
Keyword(s):  
Gene Expression ◽  
Molecular Weight ◽  
Gene Delivery ◽  
Low Molecular Weight ◽  
Ethylene Imine ◽  
Poly Ethylene ◽  
Reduced Toxicity

Naldemedine: Peripherally Acting Opioid Receptor Antagonist for Treating Opioid-induced Adverse Effects

2020 ◽  
Vol 20 (31) ◽  
pp. 2830-2842
Author(s):  
Masanao Inagaki ◽  
Toshiyuki Kanemasa ◽  
Takaaki Yokota
Keyword(s):  
Adverse Effects ◽  
Adverse Events ◽  
Severe Pain ◽  
Lead Compound ◽  
Inhibitory Effects ◽  
Pharmacokinetic Profiles ◽  
Structure Activity ◽  
The Usa ◽  
Relationship Study ◽  
The Eu

Opioids are widely used for pain management in moderate-to-severe pain. However, opioids are associated with adverse events, such as constipation and emesis/vomiting. To reduce these undesired effects, a structure–activity relationship study of morphinan derivatives was conducted, and a promising lead compound with inhibitory effects on opioid receptors was obtained. Further improvement in the potency and pharmacokinetic profiles of the lead compound led to the discovery of naldemedine, which showed anti-constipation and anti-emetic effects against these adverse events that were induced by morphine without influencing morphine’s analgesic effect. Naldemedine was launched in Japan and the USA in 2017 and in the EU in 2019, for treating opioid-induced constipation.

scholarly journals Insight into the bZIP Gene Family in Solanum tuberosum: Genome and Transcriptome Analysis to Understand the Roles of Gene Diversification in Spatiotemporal Gene Expression and Function

2020 ◽  
Vol 22 (1) ◽  
pp. 253
Author(s):  
Venura Herath ◽  
Jeanmarie Verchot
Keyword(s):  
Gene Expression ◽  
Gene Family ◽  
Functional Groups ◽  
Leucine Zipper ◽  
Expression Profiles ◽  
Crop Improvement ◽  
Potato Virus X ◽  
Tissue Growth ◽  
Abiotic Stress Response ◽  
Sequence Alignments

The basic region-leucine zipper (bZIP) transcription factors (TFs) form homodimers and heterodimers via the coil–coil region. The bZIP dimerization network influences gene expression across plant development and in response to a range of environmental stresses. The recent release of the most comprehensive potato reference genome was used to identify 80 StbZIP genes and to characterize their gene structure, phylogenetic relationships, and gene expression profiles. The StbZIP genes have undergone 22 segmental and one tandem duplication events. Ka/Ks analysis suggested that most duplications experienced purifying selection. Amino acid sequence alignments and phylogenetic comparisons made with the Arabidopsis bZIP family were used to assign the StbZIP genes to functional groups based on the Arabidopsis orthologs. The patterns of introns and exons were conserved within the assigned functional groups which are supportive of the phylogeny and evidence of a common progenitor. Inspection of the leucine repeat heptads within the bZIP domains identified a pattern of attractive pairs favoring homodimerization, and repulsive pairs favoring heterodimerization. These patterns of attractive and repulsive heptads were similar within each functional group for Arabidopsis and S. tuberosum orthologs. High-throughput RNA-seq data indicated the most highly expressed and repressed genes that might play significant roles in tissue growth and development, abiotic stress response, and response to pathogens including Potato virus X. These data provide useful information for further functional analysis of the StbZIP gene family and their potential applications in crop improvement.

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