[HTML][HTML] Role of oncogenic KRAS in the prognosis, diagnosis and treatment of colorectal cancer

G Zhu, L Pei, H Xia, Q Tang, F Bi - Molecular cancer, 2021 - Springer
Colorectal cancer (CRC) is a heterogeneous disease at the cellular and molecular levels.
Kirsten rat sarcoma (KRAS) is a commonly mutated oncogene in CRC, with mutations in …

[HTML][HTML] Recent advances in the development of protein–protein interactions modulators: mechanisms and clinical trials

H Lu, Q Zhou, J He, Z Jiang, C Peng, R Tong… - Signal transduction and …, 2020 - nature.com
Protein–protein interactions (PPIs) have pivotal roles in life processes. The studies showed
that aberrant PPIs are associated with various diseases, including cancer, infectious …

[HTML][HTML] Chemical acylation of an acquired serine suppresses oncogenic signaling of K-Ras (G12S)

Z Zhang, KZ Guiley, KM Shokat - Nature chemical biology, 2022 - nature.com
Drugs that directly impede the function of driver oncogenes offer exceptional efficacy and a
therapeutic window. The recently approved mutant selective small-molecule cysteine …

[HTML][HTML] Emerging strategies to target RAS signaling in human cancer therapy

K Chen, Y Zhang, L Qian, P Wang - Journal of hematology & oncology, 2021 - Springer
Abstract RAS mutations (HRAS, NRAS, and KRAS) are among the most common
oncogenes, and around 19% of patients with cancer harbor RAS mutations. Cells harboring …

Emerging and re-emerging warheads for targeted covalent inhibitors: applications in medicinal chemistry and chemical biology

M Gehringer, SA Laufer - Journal of medicinal chemistry, 2018 - ACS Publications
Targeted covalent inhibitors (TCIs) are designed to bind poorly conserved amino acids by
means of reactive groups, the so-called warheads. Currently, targeting noncatalytic cysteine …

Pharmacological targeting of RAS: recent success with direct inhibitors

JP O'Bryan - Pharmacological research, 2019 - Elsevier
RAS has long been viewed as undruggable due to its lack of deep pockets for binding of
small molecule inhibitors. However, recent successes in the development of direct RAS …

GTP-state-selective cyclic peptide ligands of K-Ras (G12D) block its interaction with Raf

Z Zhang, R Gao, Q Hu, H Peacock… - ACS central …, 2020 - ACS Publications
We report the identification of three cyclic peptide ligands of K-Ras (G12D) using an
integrated in vitro translation–mRNA display selection platform. These cyclic peptides show …

Drug target identification in tissues by thermal proteome profiling

A Mateus, N Kurzawa, J Perrin… - Annual Review of …, 2022 - annualreviews.org
Drug target deconvolution can accelerate the drug discovery process by identifying a drug's
targets (facilitating medicinal chemistry efforts) and off-targets (anticipating toxicity effects or …

[HTML][HTML] Therapeutic targeting of RAS: New hope for drugging the “undruggable”

I Khan, JM Rhett, JP O'Bryan - … et Biophysica Acta (BBA)-Molecular Cell …, 2020 - Elsevier
RAS is the most frequently mutated oncogene in cancer and a critical driver of oncogenesis.
Therapeutic targeting of RAS has been a goal of cancer research for more than 30 years …

[HTML][HTML] KRasG12C inhibitors in clinical trials: a short historical perspective

L Goebel, MP Müller, RS Goody, D Rauh - RSC medicinal chemistry, 2020 - pubs.rsc.org
KRas is the most frequently mutated oncogene in human cancer, and even 40 years after
the initial discovery of Ras oncogenes in 1982, no approved drug directly targets Ras in Ras …