Concepedia

Accelerated Identification of Cell Active KRAS Inhibitory Macrocyclic Peptides using Mixture Libraries and Automated Ligand Identification System (ALIS) Technology

Michael Garrigou, Bérengère Sauvagnat, Ruchia Duggal, Nicole Boo, Pooja Gopal, Jennifer M. Johnston, Anthony W. Partridge, Tomi K. Sawyer, Kaustav Biswas, N. Boyer

Journal of Medicinal Chemistry · 2022 · 28 citations · 26 references

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Concepts

Abstract

that inhibited pERK activity in a pancreatic cancer cell line. More broadly, this methodology offers an efficient alternative to accelerate the fastidious hit-to-lead optimization of PPI peptide inhibitors.

References

26

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

J.M. Ostrem, Ulf Peters, Martin L. Sos et al. · Nature · 2013 · 2.5K citations · Full text

, , +14

The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

Jude Canon, Karen Rex, Anne Y. Saiki et al. · Nature · 2019 · 2.3K citations

, , +14

Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS <sup>G12D</sup> Inhibitor

Xiaolun Wang, Shelley Allen, James F. Blake et al. · Journal of Medicinal Chemistry · 2021 · 708 citations · Full text

, , +14

Identification of the Clinical Development Candidate <b>MRTX849</b>, a Covalent KRAS<sup>G12C</sup> Inhibitor for the Treatment of Cancer

Jay B. Fell, John P. Fischer, Brian R. Baer et al. · Journal of Medicinal Chemistry · 2020 · 594 citations · Full text

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Nanoscale synthesis and affinity ranking

Nathan J. Gesmundo, Bérengère Sauvagnat, Patrick J. Curran et al. · Nature · 2018 · 214 citations

, , +13