208655-83-8Relevant articles and documents
Novel glycosylated endomorphin-2 analog produces potent centrally-mediated antinociception in mice after peripheral administration
Fichna, Jakub,Mazur, Marzena,Grzywacz, Daria,Kamysz, Wojciech,Perlikowska, Renata,Piekielna, Justyna,Sobczak, Marta,Salaga, MacIej,Toth, Geza,Janecka, Anna,Chen, Chunqiu,Olczak, Jacek
, p. 6673 - 6676 (2013)
We report the synthesis and pharmacological characterization of a novel glycosylated analog of a potent and selective endogenous μ-opioid receptor (MOP) agonist, endomorphin-2 (Tyr-Pro-Phe-Phe-NH2, EM-2), obtained by the introduction in positio
Simplified Novel Muraymycin Analogues; using a Serine Template Strategy for Linking Key Pharmacophores
Patel, Bhautikkumar,Kerr, Rachel V,Malde, Alpeshkumar K,Zunk, Matthew,Bugg, Timothy D. H.,Grant, Gary,Rudrawar, Santosh
supporting information, p. 1429 - 1438 (2020/06/17)
The present status of antibiotic research requires the urgent invention of novel agents that act on multidrug-resistant bacteria. The World Health Organization has classified antibiotic-resistant bacteria into critical, high and medium priority according to the urgency of need for new antibiotics. Naturally occurring uridine-derived “nucleoside antibiotics” have shown promising activity against numerous priority resistant organisms by inhibiting the transmembrane protein MraY (translocase I), which is yet to be explored in a clinical context. The catalytic activity of MraY is an essential process for bacterial cell viability and growth including that of priority organisms. Muraymycins are one subclass of naturally occurring MraY inhibitors. Despite having potent antibiotic properties, the structural complexity of muraymycins advocates for simplified analogues as potential lead structures. Herein, we report a systematic structure-activity relationship (SAR) study of serine template-linked, simplified muraymycin-type analogues. This preliminary SAR lead study of serine template analogues successfully revealed that the complex structure of naturally occurring muraymycins could be easily simplified to afford bioactive scaffolds against resistant priority organisms. This study will pave the way for the development of novel antibacterial lead compounds based on a simplified serine template.
ANTIBODY-COUPLED CYCLIC PEPTIDE TYROSINE TYROSINE COMPOUNDS AS MODULATORS OF NEUROPEPTIDE Y RECEPTORS
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Paragraph 0387-0388, (2018/05/17)
The present invention comprises conjugates comprising a monoclonal antibody conjugated to a cyclic PYY peptide. The invention also relates to pharmaceutical compositions and methods for use thereof. The novel conjugates are useful for preventing, treating or ameliorating diseases and disorders disclosed herein.