ACS Medicinal Chemistry Letters

Journal: ACS Medicinal Chemistry Letters

Abbreviation

ACS Med. Chem. Lett.

Publisher

American Chemical Society

ISSN

1948-5875

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Publications 1 - 7 of 7

Discovery and Design of First Benzylamine-Based Ligands Binding to an Unlocked Conformation of the Complement Factor D
Vulpetti, Anna; Ostermann, Nils; Randl, Stefan; et al. (2018)
ACS Medicinal Chemistry Letters
Discovery of New Binders for DCAF1, an Emerging Ligase Target in the Targeted Protein Degradation Field
Vulpetti, Anna; Holzer, Philipp; Schmiedeberg, Niko; et al. (2023)
ACS Medicinal Chemistry Letters
In this study, we describe the rapid identification ofpotent bindersfor the WD40 repeat domain (WDR) of DCAF1. This was achieved by tworounds of iterative focused screening of a small set of compoundsselected on the basis of internal WDR domain knowledge followed byhit expansion. Subsequent structure-based design led to nanomolarpotency binders with a clear exit vector enabling DCAF1-based bifunctionaldegrader exploration.
Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series
Rudolph, Joachim; Aliagas, Ignacio; Crawford, James J.; et al. (2015)
ACS Medicinal Chemistry Letters
1,5-Disubstituted 1,2,3-Triazoles as Amide Bond Isosteres Yield Novel Tumor-Targeting Minigastrin Analogs
Grob, Nathalie; Schibli, Roger; Behe, Martin; et al. (2021)
ACS Medicinal Chemistry Letters
1,5-Disubstituted 1,2,3-triazoles (1,5-Tz) are considered bioisosteres of cis-amide bonds. However, their use for enhancing the pharmacological properties of peptides or proteins is not yet well established. Aiming to illustrate their utility, we chose the peptide conjugate [Nle15]MG11 (DOTA-dGlu-Ala-Tyr-Gly-Trp-Nle-Asp-Phe-NH2) as a model compound since it is known that the cholecystokinin-2 receptor (CCK2R) is able to accommodate turn conformations. Analogs of [Nle15]MG11 incorporating 1,5-Tz in the backbone were synthesized and radiolabeled with lutetium-177, and their pharmacological properties (cell internalization, receptor binding affinity and specificity, plasma stability, and biodistribution) were evaluated and compared with [Nle15]MG11 as well as their previously reported analogs bearing 1,4-disubstituted 1,2,3-triazoles. Our investigations led to the discovery of novel triazole-modified analogs of [Nle15]MG11 with nanomolar CCK2R-binding affinity and 2-fold increased tumor uptake. This study illustrates that substitution of amides by 1,5-disubstituted 1,2,3-triazoles is an effective strategy to enhance the pharmacological properties of biologically active peptides.
Kinase Inhibition by Deoxy Analogues of the Resorcylic Lactone L-783277
Liniger, Marc; Neuhaus, Christian; Hofmann, Tatjana; et al. (2011)
ACS Medicinal Chemistry Letters
Synthesis and Antimycobacterial Activity of 2,1 -Dihydropyridomycins
Horlacher, Oliver P.; Hartkoorn, Ruben C.; Cole, Stewart T.; et al. (2013)
ACS Medicinal Chemistry Letters
Structural Elucidation and Antimicrobial Characterization of Novel Diterpenoids from Fabiana densa var. ramulosa
Quaglio, Deborah; Corradi, Silvia; Erazo, Silvia; et al. (2020)
ACS Medicinal Chemistry Letters

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Journal: ACS Medicinal Chemistry Letters

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