Sustainability challenges in peptide synthesis and purification: from R&D to production

A Isidro-Llobet, MN Kenworthy… - The Journal of …, 2019 - ACS Publications
In recent years, there has been a growing interest in therapeutic peptides within the
pharmaceutical industry with more than 50 peptide drugs on the market, approximately 170 …

Macrocyclization strategies for cyclic peptides and peptidomimetics

C Bechtler, C Lamers - RSC Medicinal Chemistry, 2021 - pubs.rsc.org
Peptides are a growing therapeutic class due to their unique spatial characteristics that can
target traditionally “undruggable” protein–protein interactions and surfaces. Despite their …

Advances in chemical protein modification

O Boutureira, GJL Bernardes - Chemical reviews, 2015 - ACS Publications
Chemical protein modification has emerged as an invaluable tool for the development of
modified proteins. The complementary use of both genetic and chemical methods has …

Click chemistry in complex mixtures: bioorthogonal bioconjugation

CS McKay, MG Finn - Chemistry & biology, 2014 - cell.com
The selective chemical modification of biological molecules drives a good portion of modern
drug development and fundamental biological research. While a few early examples of …

[HTML][HTML] Macrocyclization reactions: the importance of conformational, configurational, and template-induced preorganization

V Marti-Centelles, MD Pandey, MI Burguete… - Chemical …, 2015 - ACS Publications
Macrocyclic structures are common synthetic targets in drug discovery,(1, 2) and therefore,
interest in their study is continuously increasing in this field.(3, 4) A classic example is …

Chemical protein modification through cysteine

SB Gunnoo, A Madder - ChemBioChem, 2016 - Wiley Online Library
The modification of proteins with non‐protein entities is important for a wealth of
applications, and methods for chemically modifying proteins attract considerable attention …

Arylation chemistry for bioconjugation

C Zhang, EV Vinogradova… - Angewandte Chemie …, 2019 - Wiley Online Library
Bioconjugation chemistry has been used to prepare modified biomolecules with functions
beyond what nature intended. Central to these techniques is the development of highly …

Peptide therapeutics: targeting the undruggable space

N Tsomaia - European journal of medicinal chemistry, 2015 - Elsevier
Rapid advancements in genomics have brought a better understanding of molecular
mechanisms for various pathologies and identified a number of highly attractive target …

π-Clamp-mediated cysteine conjugation

C Zhang, M Welborn, T Zhu, NJ Yang, MS Santos… - Nature …, 2016 - nature.com
Site-selective functionalization of complex molecules is one of the most significant
challenges in chemistry. Typically, protecting groups or catalysts must be used to enable the …

Functionalised staple linkages for modulating the cellular activity of stapled peptides

YH Lau, P De Andrade, ST Quah, M Rossmann… - Chemical …, 2014 - pubs.rsc.org
Stapled peptides are a promising class of alpha-helix mimetic inhibitors for protein–protein
interactions. We report the divergent synthesis of “functionalised” stapled peptides via an …