Multifaceted roles of disulfide bonds. Peptides as therapeutics
M Gongora-Benitez, J Tulla-Puche… - Chemical Reviews, 2014 - ACS Publications
In the last century, small-molecule natural products were the main inspiration for most drug
discovery programs based either on high-throughput screening (HTS) or rational design …
discovery programs based either on high-throughput screening (HTS) or rational design …
Impact of non-proteinogenic amino acids in the discovery and development of peptide therapeutics
Y Ding, JP Ting, J Liu, S Al-Azzam, P Pandya, S Afshar - Amino Acids, 2020 - Springer
With the development of modern chemistry and biology, non-proteinogenic amino acids
(NPAAs) have become a powerful tool for develo** peptide-based drug candidates. Drug …
(NPAAs) have become a powerful tool for develo** peptide-based drug candidates. Drug …
Strategic approaches to optimizing peptide ADME properties
L Di - The AAPS journal, 2015 - Springer
Abstract Development of peptide drugs is challenging but also quite rewarding. Five
blockbuster peptide drugs are currently on the market, and six new peptides received first …
blockbuster peptide drugs are currently on the market, and six new peptides received first …
Methods to enhance the metabolic stability of peptide-based PET radiopharmaceuticals
The high affinity and specificity of peptides towards biological targets, in addition to their
favorable pharmacological properties, has encouraged the development of many peptide …
favorable pharmacological properties, has encouraged the development of many peptide …
Improving oral bioavailability of peptides by multiple N‐methylation: somatostatin analogues
E Biron, J Chatterjee, O Ovadia… - Angewandte Chemie …, 2008 - Wiley Online Library
Low bioavailability of peptides following oral administration is attributed to their inactivation
in the gastro–intestinal tract through enhanced enzymatic degradation in the gut wall by a …
in the gastro–intestinal tract through enhanced enzymatic degradation in the gut wall by a …
Peptides as therapeutics with enhanced bioactivity
D Goodwin, P Simerska, I Toth - Current medicinal chemistry, 2012 - ingentaconnect.com
The development of techniques for efficient peptide production renewed interest in peptides
as therapeutics. Numerous modifications for improving stability, transport and affinity profiles …
as therapeutics. Numerous modifications for improving stability, transport and affinity profiles …
Click chemistry as a macrocyclization tool in the solid-phase synthesis of small cyclic peptides
Despite the vast number of techniques developed for the cyclization of small peptides,
cyclization efficiency remains problematic in peptides that lack turn-promoting structures …
cyclization efficiency remains problematic in peptides that lack turn-promoting structures …
Translation of DNA into a Library of 13 000 Synthetic Small-Molecule Macrocycles Suitable for in Vitro Selection
DNA-templated organic synthesis enables the translation, selection, and amplification of
DNA sequences encoding synthetic small-molecule libraries. Previously we described the …
DNA sequences encoding synthetic small-molecule libraries. Previously we described the …
To protect peptide pharmaceuticals against peptidases
R Rink, A Arkema-Meter, I Baudoin, E Post… - … of pharmacological and …, 2010 - Elsevier
Introduction: The major hurdle in the application and delivery of peptide pharmaceuticals is
their rapid in vivo breakdown. Methods: We here combined two approaches to stabilize …
their rapid in vivo breakdown. Methods: We here combined two approaches to stabilize …
A Comprehensive Review of Non-Covalent Radiofluorination Approaches Using Aluminum [18F]fluoride: Will [18F]AlF Replace 68Ga for Metal Chelate Labeling?
Due to its ideal physical properties, fluorine-18 turns out to be a key radionuclide for positron
emission tomography (PET) imaging, for both preclinical and clinical applications. However …
emission tomography (PET) imaging, for both preclinical and clinical applications. However …