[HTML] nih.gov

SHP2 inhibition diminishes KRASG12C cycling and promotes tumor microenvironment remodeling

C Fedele, S Li, KW Teng, CJR Foster, D Peng… - Journal of Experimental …, 2020 - rupress.org
KRAS is the most frequently mutated human oncogene, and KRAS inhibition has been a
longtime goal. Recently, inhibitors were developed that bind KRASG12C-GDP and react …
被引用次数：174 相关文章 所有 8 个版本

SHP2 inhibition overcomes RTK-mediated pathway reactivation in KRAS-mutant tumors treated with MEK inhibitors

H Lu, C Liu, R Velazquez, H Wang, LM Dunkl… - Molecular cancer …, 2019 - AACR
FGFR1 was recently shown to be activated as part of a compensatory response to prolonged
treatment with the MEK inhibitor trametinib in several KRAS-mutant lung and pancreatic …
被引用次数：80 相关文章 所有 8 个版本
[PDF] aacrjournals.org

Allosteric inhibition of SHP2 stimulates antitumor immunity by transforming the immunosuppressive environment

E Quintana, CJ Schulze, DR Myers, TJ Choy, K Mordec… - Cancer research, 2020 - AACR
The protein tyrosine phosphatase SHP2 binds to phosphorylated signaling motifs on
regulatory immunoreceptors including PD-1, but its functional role in tumor immunity is …
被引用次数：80 相关文章 所有 3 个版本
[HTML] nih.gov

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 …
被引用次数：57 相关文章 所有 7 个版本
[PDF] aacrjournals.org

Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C

A Weiss, E Lorthiois, L Barys, KS Beyer… - Cancer discovery, 2022 - AACR
Covalent inhibitors of KRASG12C have shown antitumor activity against
advanced/metastatic KRASG12C-mutated cancers, though resistance emerges and …
被引用次数：64 相关文章 所有 5 个版本

KRASG12D inhibition reprograms the microenvironment of early and advanced pancreatic cancer to promote FAS-mediated killing by CD8+ T cells

KK Mahadevan, KM McAndrews, VS LeBleu, S Yang… - Cancer Cell, 2023 - cell.com
Summary The KRAS G12D mutation is present in nearly half of pancreatic adenocarcinomas
(PDAC). We investigated the effects of inhibiting the KRAS G12D mutant protein with …
被引用次数：42 相关文章 所有 7 个版本
[PDF] aacrjournals.org

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 …
被引用次数：336 相关文章 所有 8 个版本
[PDF] frontiersin.org

Targeting KRAS: the elephant in the room of epithelial cancers

V Merz, M Gaule, C Zecchetto, A Cavaliere… - Frontiers in …, 2021 - frontiersin.org
Mutations of the proto-oncogene KRAS are the most frequent gain-of-function alterations
found in cancer. KRAS is mutated in about 30% of all human tumors, but it could reach more …
被引用次数：59 相关文章 所有 7 个版本
[PDF] ciberonc.es

Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase

DA Ruess, GJ Heynen, KJ Ciecielski, J Ai… - Nature medicine, 2018 - nature.com
The ubiquitously expressed non-receptor protein tyrosine phosphatase SHP2, encoded by
PTPN11, is involved in signal transduction downstream of multiple growth factor, cytokine …
被引用次数：352 相关文章 所有 12 个版本
[HTML] nih.gov

The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients

J Hallin, LD Engstrom, L Hargis, A Calinisan, R Aranda… - Cancer discovery, 2020 - AACR
Despite decades of research, efforts to directly target KRAS have been challenging.
MRTX849 was identified as a potent, selective, and covalent KRASG12C inhibitor that …
被引用次数：1018 相关文章 所有 6 个版本