Vertical Pathway Inhibition Overcomes Adaptive Feedback Resistance to KRASG12C Inhibition
MB Ryan, F Fece de la Cruz, S Phat, DT Myers… - Clinical cancer …, 2020 - AACR
Purpose: Although KRAS represents the most commonly mutated oncogene, it has long
been considered an “undruggable” target. Novel covalent inhibitors selective for the …
been considered an “undruggable” target. Novel covalent inhibitors selective for the …
Clinical Acquired Resistance to KRASG12C Inhibition through a Novel KRAS Switch-II Pocket Mutation and Polyclonal Alterations Converging on RAS–MAPK …
Mutant-selective KRASG12C inhibitors, such as MRTX849 (adagrasib) and AMG 510
(sotorasib), have demonstrated efficacy in KRAS G12C-mutant cancers, including non–small …
(sotorasib), have demonstrated efficacy in KRAS G12C-mutant cancers, including non–small …
Cell Type–specific Adaptive Signaling Responses to KRASG12C Inhibition
HS Solanki, EA Welsh, B Fang, V Izumi, L Darville… - Clinical Cancer …, 2021 - AACR
Purpose: Covalent inhibitors of KRASG12C specifically target tumors driven by this form of
mutant KRAS, yet early studies show that bypass signaling drives adaptive resistance …
mutant KRAS, yet early studies show that bypass signaling drives adaptive resistance …
KRASG12C-independent feedback activation of wild-type RAS constrains KRASG12C inhibitor efficacy
Although KRAS has long been considered undruggable, direct KRAS G12C inhibitors have
shown promising initial clinical efficacy. However, the majority of patients still fail to respond …
shown promising initial clinical efficacy. However, the majority of patients still fail to respond …
Selective inhibition of oncogenic KRAS output with small molecules targeting the inactive state
MP Patricelli, MR Janes, LS Li, R Hansen, U Peters… - Cancer discovery, 2016 - AACR
KRAS gain-of-function mutations occur in approximately 30% of all human cancers. Despite
more than 30 years of KRAS-focused research and development efforts, no targeted therapy …
more than 30 years of KRAS-focused research and development efforts, no targeted therapy …
Mechanisms of Resistance to KRASG12C-Targeted Therapy
NS Akhave, AB Biter, DS Hong - Cancer discovery, 2021 - AACR
KRAS mutations are among the most common drivers of human carcinogenesis, and are
associated with poor prognosis and an aggressive disease course. With the advent of …
associated with poor prognosis and an aggressive disease course. With the advent of …
More to the RAS Story: KRASG12C Inhibition, Resistance Mechanisms, and Moving Beyond KRASG12C
CD Lietman, ML Johnson, F McCormick… - American Society of …, 2022 - ascopubs.org
Despite the discovery of RAS oncogenes in human tumor DNA 40 years ago, the
development of effective targeted therapies directed against RAS has lagged behind those …
development of effective targeted therapies directed against RAS has lagged behind those …
Pharmacological induction of RAS-GTP confers RAF inhibitor sensitivity in KRAS mutant tumors
I Yen, F Shanahan, M Merchant, C Orr, T Hunsaker… - Cancer Cell, 2018 - cell.com
Targeting KRAS mutant tumors through inhibition of individual downstream pathways has
had limited clinical success. Here we report that RAF inhibitors exhibit little efficacy in KRAS …
had limited clinical success. Here we report that RAF inhibitors exhibit little efficacy in KRAS …
Overcoming resistance to drugs targeting KRASG12C mutation
D Jiao, S Yang - The Innovation, 2020 - cell.com
Activating KRAS mutations are present in 25% of human cancer. Although oncogenic Ras
was deemed" undruggable" in the past, recent efforts led to the development of …
was deemed" undruggable" in the past, recent efforts led to the development of …
[HTML][HTML] Precision oncology provides opportunities for targeting KRAS-inhibitor resistance
Novel inhibitors targeting Kirsten rat sarcoma virus homolog (KRAS) KRAS G12C in various
cancers have shown good initial efficacy, but therapy-related drug resistance eventually …
cancers have shown good initial efficacy, but therapy-related drug resistance eventually …
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