Beyond 20 in the 21st century: prospects and challenges of non-canonical amino acids in peptide drug discovery
JL Hickey, D Sindhikara, SL Zultanski… - ACS Medicinal …, 2023 - ACS Publications
Life is constructed primarily using a toolbox of 20 canonical amino acids─ relying upon
these building blocks for the assembly of proteins and peptides that regulate nearly every …
these building blocks for the assembly of proteins and peptides that regulate nearly every …
Side-Selective Solid-Phase Metallaphotoredox N(in)-Arylation of Peptides
Postsynthetic diversification of peptides through selective modification of endogenous amino
acid side chains has enabled significant advances in peptide drug discovery while …
acid side chains has enabled significant advances in peptide drug discovery while …
One-Pot Synthesis of Cereblon Proteolysis Targeting Chimeras via Photoinduced C(sp2)–C(sp3) Cross Coupling and Amide Formation for Proteolysis Targeting …
CM Arndt, J Bitai, J Brunner, T Opatz… - Journal of Medicinal …, 2023 - ACS Publications
In this study, a one-pot synthesis via photoinduced C (sp2)–C (sp3) coupling followed by
amide formation to access proteolysis targeting chimeras (PROTACs) was developed. The …
amide formation to access proteolysis targeting chimeras (PROTACs) was developed. The …
Pd (I)-catalyzed ring-opening arylation of cyclopropyl-α-aminoamides: Access to α-ketoamide peptidomimetics
Y Sun, L Yang, Y Cheng, G An, G Li - Chinese Chemical Letters, 2024 - Elsevier
We report the unprecedent Pd (I) catalyzed ring-opening arylation of cyclopropyl-α-
aminoamides. This protocol allows facile access to biologically important α-ketoamide …
aminoamides. This protocol allows facile access to biologically important α-ketoamide …
Peptide Boronic Acids by Late‐Stage Hydroboration on the Solid Phase
M Werner, J Brinkhofer, L Hammermüller… - Advanced …, 2024 - Wiley Online Library
Organoboron compounds have a wide range of applications in numerous research fields,
and metmhods to incorporate them in biomolecules are much sought after. Here, on‐resin …
and metmhods to incorporate them in biomolecules are much sought after. Here, on‐resin …
High-throughput experimentation for medicinal chemistry: state of the art, challenges, and opportunities
D Kalyani, M Uehling, M Wleklinski - The Power of High …, 2022 - ACS Publications
This chapter details strategies toward developing library amenable reactions with a lens
toward accessing a diverse array of medicinal chemistry targets using microscale or …
toward accessing a diverse array of medicinal chemistry targets using microscale or …
Leveraging HTE in Non-canonical Amino Acid Synthesis and Peptide Ligation
NR Patel, D Schultz - … : Case Studies from Drug Discovery, Drug …, 2022 - ACS Publications
Peptide therapeutics have been termed the “Goldilocks” modality, possessing the target
selectivity of a biologic coupled with the pharmacokinetics and biopharmaceutical properties …
selectivity of a biologic coupled with the pharmacokinetics and biopharmaceutical properties …
One-pot synthesis of CRBN PROTACs via photoinduced C (sp2)–C (sp3) cross coupling and amide formation for PROTAC library synthesis
CM Arndt, J Bitai, J Brunner, T Opatz, P Martinelli… - 2023 - chemrxiv.org
In this study, a one-pot synthesis via photoinduced C (sp2)–C (sp3) coupling followed by
amide formation to access proteolysis targeting chimeras (PROTACs) was developed. The …
amide formation to access proteolysis targeting chimeras (PROTACs) was developed. The …