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Targeting KRAS in cancer
RAS family variants—most of which involve KRAS—are the most commonly occurring
hotspot mutations in human cancers and are associated with a poor prognosis. For almost …
hotspot mutations in human cancers and are associated with a poor prognosis. For almost …
[HTML][HTML] Advances and challenges in the treatment of lung cancer
Y Li, B Yan, S He - Biomedicine & Pharmacotherapy, 2023 - Elsevier
Lung cancer accounts for a relatively high proportion of malignant tumors. As the most
prevalent type of lung cancer, non-small cell lung cancer (NSCLC) is characterized by high …
prevalent type of lung cancer, non-small cell lung cancer (NSCLC) is characterized by high …
Pan-KRAS inhibitor disables oncogenic signalling and tumour growth
D Kim, L Herdeis, D Rudolph, Y Zhao, J Böttcher… - Nature, 2023 - nature.com
KRAS is one of the most commonly mutated proteins in cancer, and efforts to directly inhibit
its function have been continuing for decades. The most successful of these has been the …
its function have been continuing for decades. The most successful of these has been the …
Single-Agent Divarasib (GDC-6036) in Solid Tumors with a KRAS G12C Mutation
A Sacher, P LoRusso, MR Patel… - … England Journal of …, 2023 - Mass Medical Soc
Abstract Background Divarasib (GDC-6036) is a covalent KRAS G12C inhibitor that was
designed to have high potency and selectivity. Methods In a phase 1 study, we evaluated …
designed to have high potency and selectivity. Methods In a phase 1 study, we evaluated …
Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy
M Holderfield, BJ Lee, J Jiang, A Tomlinson… - Nature, 2024 - nature.com
Abstract RAS oncogenes (collectively NRAS, HRAS and especially KRAS) are among the
most frequently mutated genes in cancer, with common driver mutations occurring at codons …
most frequently mutated genes in cancer, with common driver mutations occurring at codons …
Patient-derived xenograft models in cancer therapy: technologies and applications
Patient-derived xenograft (PDX) models, in which tumor tissues from patients are implanted
into immunocompromised or humanized mice, have shown superiority in recapitulating the …
into immunocompromised or humanized mice, have shown superiority in recapitulating the …
The current state of the art and future trends in RAS-targeted cancer therapies
Despite being the most frequently altered oncogenic protein in solid tumours, KRAS has
historically been considered 'undruggable'owing to a lack of pharmacologically targetable …
historically been considered 'undruggable'owing to a lack of pharmacologically targetable …
Molecular targeted therapy for anticancer treatment
HY Min, HY Lee - Experimental & Molecular Medicine, 2022 - nature.com
Since the initial clinical approval in the late 1990s and remarkable anticancer effects for
certain types of cancer, molecular targeted therapy utilizing small molecule agents or …
certain types of cancer, molecular targeted therapy utilizing small molecule agents or …
PROTACs: past, present and future
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules consisting of
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …
An allosteric pan-TEAD inhibitor blocks oncogenic YAP/TAZ signaling and overcomes KRAS G12C inhibitor resistance
The Hippo pathway is a key growth control pathway that is conserved across species. The
downstream effectors of the Hippo pathway, YAP (Yes-associated protein) and TAZ …
downstream effectors of the Hippo pathway, YAP (Yes-associated protein) and TAZ …