A Dimension of Sound

Wissner, Reba A.

doi:10.2307/j.ctv1qv307

Cited by 2 publications

(3 citation statements)

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“…The synthesis starts with Fmoc-protected amino acids, which are commercially available in most cases, with typical yields of 40% over the three steps. So far, thioamide versions of 15 of the 20 canonical amino acids (Ala, 130 Arg, 131 Asp, 132 Cys, 131 Glu, 133 Gly, 131 Ile, 134 Leu, 135 Lys, 131 Phe, 136 Pro, 136 Ser, 131 Trp, 131 Tyr, 134 and Val 137 ), as well as hydroxyproline, 134 have been reported.…”

Section: Chemical Synthesis Of Thioamide-containing Peptidesmentioning

confidence: 99%

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Biosynthesis and Chemical Applications of Thioamides

et al. 2019

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Thioamidation as a posttranslational modification is exceptionally rare, with only a few reported natural products and exactly one known protein example (methyl-coenzyme M reductase from methane-metabolizing archaea). Recently, there has been significant progress in elucidating the biosynthesis and function of several thioamide-containing natural compounds. Separate developments in the chemical installation of thioamides into peptides and proteins have enabled cell biology and biophysical studies that advance the current understanding of natural thioamides. This review highlights the various strategies used by Nature to install thioamides in peptidic scaffolds and the potential functions of this rare but important modification. We also discuss synthetic methods used for the site-selective incorporation of thioamides into polypeptides with a brief discussion of the physicochemical implications. This account will serve as a foundation for further study of thioamides in natural products and their various applications.

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Section: Chemical Synthesis Of Thioamide-containing Peptidesmentioning

confidence: 99%

“…With the possibility of incorporating thioamides as spectroscopic probes into full-length proteins 136 , the question of their influence on protein stability has emerged. Due to their increased size and altered hydrogen bonding properties, they can stabilize or destabilize protein folds.…”

Section: Thioamide Effects In Full Length Proteinsmentioning

confidence: 99%

Biosynthesis and Chemical Applications of Thioamides

et al. 2019

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“…In contrast, activation of HER-2 occurs mainly by overexpression, which leads to spontaneous homodimerization and activation of downstream signaling events in a ligand-independent manner. 23,24 Figure1: EGFR pathway This review is originated from the literature survey on the quinazoline and other important heterocyclic moiety [25][26][27][28][29][30][31][32][33][34][35][36][37][38][39][40][41] which shows the good EGFR/VEGFR inhibitory activity.…”

Section: Introductionmentioning

confidence: 99%

Epidermal Growth Factor Receptor (EGFR) Inhibitors for Tumor Anti-angiogenesis Activity

Bairagi¹,

Ladhha²,

Lohiya³

et al. 2012

Proceedings of the 16th International Electronic Conference on Synthetic Organic Chemistry

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The EGFR family plays an essential role in normal organ development by mediating morphogenesis and differentiation through effects on cell proliferation, differentiation, apoptosis, invasion, and angiogenesis. Unlike normal cells that have tight regulatory mechanisms controlling EGFR pathways, tumor cells often have dysregulated EGFR signaling, allowing them to proliferate under adverse conditions, invade surrounding tissues, and increase angiogenesis. Epidermal growth factor receptor (EGFR) is a transmembrane receptor tyrosine kinase that belongs to the Human epidermal receptor (HER) family of receptors. Receptor protein tyrosine kinases play a key role in signal transduction pathways that regulate cell division and differentiation. Among the growth factor receptor kinases that have been identified as being important in cancer is epidermal growth factor receptor (EGFR) kinase (also known as erb-B1 or HER-1) and the related human epidermal growth factor receptor HER-2 (also known as erbB-2). The quinazoline and other heterocyclic skeletons are of great importance to chemists as well as biologists as it is available in a large variety of naturally occurring compounds. In this article we are emphasizing on various heterocycles such as Quinazoline, pyrrolotriazines etc. as promising anticancer agents. These heterocycles showed the anticancer activity through the inhibition of EGFR enzyme. Attempt will be taken to provide details information on the said topic in the benefit of medicinal chemist.

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A Dimension of Sound

Cited by 2 publications

References 0 publications

Biosynthesis and Chemical Applications of Thioamides

Biosynthesis and Chemical Applications of Thioamides

Epidermal Growth Factor Receptor (EGFR) Inhibitors for Tumor Anti-angiogenesis Activity

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