Direct GDP-KRASG12C inhibitors and mechanisms of resistance: the tip of the iceberg

JC Rosen, A Sacher, MS Tsao - Therapeutic Advances in …, 2023 - journals.sagepub.com
Kirsten rat sarcoma viral oncogene homolog mutations are observed in 25% of lung
adenocarcinoma and 40% of these are G12C mutations. Historically, no approved targeted …

Research progress on small molecule inhibitors targeting KRAS G12C with acrylamide structure and the strategies for solving KRAS inhibitor resistance

Z Jiang, Y Li, X Zhou, J Wen, P Zheng, W Zhu - Bioorganic & Medicinal …, 2024 - Elsevier
KRAS (Kirsten-RAS) is a highly mutated gene in the RAS (rat sarcoma) gene family that acts
as a critical switch in intracellular signaling pathways, regulating cell proliferation …

Markov state models and molecular dynamics simulations reveal the conformational transition of the intrinsically disordered hypervariable region of K-Ras4B to the …

H Zhang, D Ni, J Fan, M Li, J Zhang… - Journal of Chemical …, 2022 - ACS Publications
K-Ras4B, the most frequently mutated Ras isoform in human tumors, plays a vital part in cell
growth, differentiation, and survival. Its tail, the C-terminal hypervariable region (HVR), is …

Molecular docking and molecular dynamics simulations reveal the clinical resistance of the gatekeeper mutation V564F of FGFR2 against Infigratinib

G Zheng, W Liu, Q Zhang, T Shen, J Zhang… - Journal of …, 2023 - Taylor & Francis
Fibroblast growth factor receptor 2 (FGFR2), as a transmembrane receptor tyrosine kinase,
is implicated in a plethora of human cancers, including intrahepatic cholangiocarcinomas …

Structural perspectives on recent breakthrough efforts toward direct drugging of RAS and acquired resistance

JS Lokhandwala, TB Smalley, TH Tran - Frontiers in Oncology, 2024 - frontiersin.org
The Kirsten rat sarcoma viral oncoprotein homolog (KRAS) is currently a primary focus of
oncologists and translational scientists, driven by exciting results with KRAS-targeted …

Mechanistic insights into the role of calcium in the allosteric regulation of the calmodulin-regulated death-associated protein kinase

X Li, B Li, J Li, M Yang, Y Bai, K Chen… - Frontiers in Molecular …, 2022 - frontiersin.org
Calcium (Ca2+) signaling plays an important role in the regulation of many cellular
functions. Ca2+-binding protein calmodulin (CaM) serves as a primary effector of calcium …

Computational revealing Infigratinib resistance to the FGFR2 N549H and N549K mutations

G Xu, B Wu, W Liang, J Zhang, S Xu, T Du… - Journal of …, 2025 - Taylor & Francis
Fibroblast growth factor receptor 2 (FGFR2) is a receptor tyrosine kinase that is involved in
many human cancers such as intrahepatic cholangiocarcinomas and hepatocellular …