A06 tri-complex inhibitors of the oncogenic, GTP-bound form of KRASG12C overcome RTK-mediated escape mechanisms and drive tumor regressions in preclinical …
R Nichols, C Schulze, A Bermingham, T Choy… - Journal of Thoracic …, 2020 - jto.org
… expression and site of SMARCA4 mutations, we describe two … -mutant tumors and the class
of mutations associated with … KEAP1, STK11, and KRAS mutations in patient with NSCLC, …
of mutations associated with … KEAP1, STK11, and KRAS mutations in patient with NSCLC, …
Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism
… KRAS mutants are thought to exist in a “constitutively” active (GTP-bound) state in cancer cells
(13). Thus, inhibition of KRAS… to KRAS G12C inhibition, were treated with inhibitors of RTK …
(13). Thus, inhibition of KRAS… to KRAS G12C inhibition, were treated with inhibitors of RTK …
Mechanisms of response and tolerance to active RAS inhibition in KRAS-mutant NSCLC
HA Araujo, X Pechuan-Jorge, T Zhou, MT Do, X Hu… - Cancer Discovery - AACR
… On-treatment feedback reactivation of the RAS-MAPK pathway, as a result of synthesis
and GTP-loading of new KRASG12C and/or RTK-driven activation of wild-type RAS, (KRAS, …
and GTP-loading of new KRASG12C and/or RTK-driven activation of wild-type RAS, (KRAS, …
[HTML][HTML] Selective KRAS G12C inhibitors in non-small cell lung cancer: chemistry, concurrent pathway alterations, and clinical outcomes
G Palma, F Khurshid, K Lu, B Woodward… - NPJ Precision …, 2021 - nature.com
… KRAS mutations occur in approximately one in four patients diagnosed with non-small …
KRAS G12C mutant lung cell lines. KRAS G12C inhibition in combination with the RTK inhibitors …
KRAS G12C mutant lung cell lines. KRAS G12C inhibition in combination with the RTK inhibitors …
Targeting KRAS: Crossroads of Signaling and Immune Inhibition
S Kato, Y Fujiwara, DS Hong - Journal of Immunotherapy …, 2022 - meridian.allenpress.com
… of cancer with KRAS mutation; successful development of the KRAS G12C inhibitor and its
… in GTP-bound KRAS G12C activation, suppression of RTK-mediated MAPK reactivation, …
… in GTP-bound KRAS G12C activation, suppression of RTK-mediated MAPK reactivation, …
MEK inhibitors for the treatment of NRAS mutant melanoma
S Sarkisian, D Davar - Drug Design, Development and Therapy, 2018 - Taylor & Francis
… initiation of receptor tyrosine kinase (RTK) on the cell surface … reported to be additive in
KRAS mutant tumor cell lines and … AKT inhibitor MK-2206 in KRAS mutant cancers, Citation101 …
KRAS mutant tumor cell lines and … AKT inhibitor MK-2206 in KRAS mutant cancers, Citation101 …
[HTML][HTML] The Therapeutic Landscape for KRAS-Mutated Colorectal Cancers
SM Tria, ME Burge, VLJ Whitehall - Cancers, 2023 - mdpi.com
… Signaling is initiated by the binding of a ligand to its receptor tyrosine kinase (RTK) such as
… This study revealed that while these inhibitors are developed for very specific KRAS mutants…
… This study revealed that while these inhibitors are developed for very specific KRAS mutants…
[HTML][HTML] Targeting oncogenic KRAS in non-small-cell lung cancer
N Sunaga, Y Miura, N Kasahara, R Sakurai - Cancers, 2021 - mdpi.com
… of resistance to KRAS G12C inhibitors and possible … the current understanding of KRAS
mutations regarding the … to complement each other to activate RTK-RAS signaling pathways to …
mutations regarding the … to complement each other to activate RTK-RAS signaling pathways to …
[HTML][HTML] Targeted therapies for KRAS-mutant non-small cell lung cancer: from preclinical studies to clinical development—a narrative review
M Santarpia, G Ciappina, CC Spagnolo… - Translational Lung …, 2023 - ncbi.nlm.nih.gov
… describe KRAS mutations and the biology of KRAS-mutant tumors … on KRAS inhibitors in
NSCLC patients with KRAS G12C … RTK feedback signaling in response to MEK inhibition. Upon …
NSCLC patients with KRAS G12C … RTK feedback signaling in response to MEK inhibition. Upon …
[HTML][HTML] KRAS secondary mutations that confer acquired resistance to KRAS G12C inhibitors, sotorasib and adagrasib, and overcoming strategies: insights from in …
T Koga, K Suda, T Fujino, S Ohara, A Hamada… - Journal of Thoracic …, 2021 - Elsevier
… In this study, we searched for secondary KRAS mutations that would confer resistance to the
KRAS … and SHP2 inhibitor) or RTK inhibitors (cetuximab and afatinib) upstream and a MEK …
KRAS … and SHP2 inhibitor) or RTK inhibitors (cetuximab and afatinib) upstream and a MEK …