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Preformulation Studies of a Stable PTEN-PDZ Lipopeptide Able to Cross an In Vitro Blood-Brain-Barrier Model as a Potential Therapy for Alzheimer's Disease
(Springer, 2020-08-04)
PurposeAmyloid beta (A beta) drives the accumulation of excess Phosphatase and Tensin Homolog Deleted on Chromosome 10 (PTEN) at synapses, inducing synaptic depression and perturbing memory. This recruitment of PTEN to ...
Manipulating the fluorescence lifetime at the sub-cellular scale via photo-switchable barcoding
(Nature, 2020-05-18)
Fluorescent barcoding is a pivotal technique for the investigation of the microscale world, from information storage to the monitoring of dynamic biochemical processes. Using fluorescence lifetime as the readout modality ...
Manganese-Catalyzed Multicomponent Synthesis of Tetrasubstituted Propargylamines: System Development and Theoretical Study
(Wiley-VCH, 2020-07-20)
The importance of multicomponent reactions as an efficient tool in organic synthesis is widely recognized, as the need for sustainable, practical, atom- and step-economic methodologies is becoming a crucial concept in ...
Reduced Graphene Oxide/Polymer Monolithic Materials for Selective CO2 Capture
(MDPI, 2020-04-17)
Polymer composite materials with hierarchical porous structure have been advancing in many different application fields due to excellent physico-chemical properties. However, their synthesis continues to be a highly ...
Site-Selective Aqueous C–H Acylation of Tyrosine-Containing Oligopeptides with Aldehydes
(RSC, 2020-10-06)
The development of useful synthetic tools to label amino acids within a peptide framework for the ultimate modification of proteins in a late-stage fashion is a challenging task of utmost importance within chemical biology. ...
Site-Selective Trifluoromethylation Reactions of Oligopeptides
(Wiley, 2020-06-08)
Site-selective chemical modifications that target proteinogenic amino acid residues complement the methods entailing genetic manipulation, thereby allowing straightforward and rapid access to engineered proteins. The ...
Cu-Catalyzed Site-Selective C(sp2)–H Radical Trifluoromethylation of Tryptophan Containing Peptides
(ACS Publications, 2020-02-13)
Site-selective functionalization of C–H bonds within a peptide framework poses a challenging task of paramount synthetic relevance. Herein, we report an operationally simple C(sp2)–H trifluoromethylation of tryptophan ...
Towards a more precise therapy in cancer: Exploring epigenetic complexity
(Elsevier, 2020-08)
A plethora of preclinical evidences suggests that pharmacological targeting of epigenetic dysregulation is a potent strategy to combat human diseases. Nevertheless, the implementation of epidrugs in clinical practice is ...
Fused 1,5-Naphthyridines: Synthetic Tools and Applications
(MDPI, 2020-07-31)
Heterocyclic nitrogen compounds, including fused 1,5-naphthyridines, have versatile applications in the fields of synthetic organic chemistry and play an important role in the field of medicinal chemistry, as many of them ...
Synthetic Strategies, Reactivity and Applications of 1,5-Naphthyridines
(MDPI, 2020-07-16)
This review covers the synthesis and reactivity of 1,5-naphthyridine derivatives published in the last 18 years. These heterocycles present a significant importance in the field of medicinal chemistry because many of them ...