KRAS mutation in pancreatic cancer

J Luo - Seminars in oncology, 2021 - Elsevier
Pancreatic cancer is a recalcitrant cancer with one of the lowest 5-year survival rates. A
hallmark of pancreatic cancer is the prevalence of oncogenic mutation in the KRAS gene …

A comprehensive review of SHP2 and its role in cancer

MD Asmamaw, XJ Shi, LR Zhang, HM Liu - Cellular Oncology, 2022 - Springer
Src homology 2-containing protein tyrosine phosphatase 2 (SHP2) is a non-receptor protein
tyrosine phosphatase ubiquitously expressed mainly in the cytoplasm of several tissues …

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 …

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 …

Endothelial deletion of SHP2 suppresses tumor angiogenesis and promotes vascular normalization

Z Xu, C Guo, Q Ye, Y Shi, Y Sun, J Zhang… - Nature …, 2021 - nature.com
SHP2 mediates the activities of multiple receptor tyrosine kinase signaling and its function in
endothelial processes has been explored extensively. However, genetic studies on the role …

Combinations with allosteric SHP2 inhibitor TNO155 to block receptor tyrosine kinase signaling

C Liu, H Lu, H Wang, A Loo, X Zhang, G Yang… - Clinical Cancer …, 2021 - AACR
Purpose: SHP2 inhibitors offer an appealing and novel approach to inhibit receptor tyrosine
kinase (RTK) signaling, which is the oncogenic driver in many tumors or is frequently …

Molecular pathways and mechanisms of BRAF in cancer therapy

PI Poulikakos, RJ Sullivan, R Yaeger - Clinical Cancer Research, 2022 - AACR
With the identification of activating mutations in BRAF across a wide variety of malignancies,
substantial effort was placed in designing safe and effective therapeutic strategies to target …

Recent advances of SHP2 inhibitors in cancer therapy: current development and clinical application

X Yuan, H Bu, J Zhou, CY Yang… - Journal of medicinal …, 2020 - ACS Publications
SHP2 (Src homology-2 domain-containing protein tyrosine phosphatase-2) is a non-
receptor protein tyrosine phosphatase that removes tyrosine phosphorylation. Functionally …

BRAF—A tumour-agnostic drug target with lineage-specific dependencies

AJ Hanrahan, Z Chen, N Rosen, DB Solit - Nature Reviews Clinical …, 2024 - nature.com
In June 2022, the FDA granted Accelerated Approval to the BRAF inhibitor dabrafenib in
combination with the MEK inhibitor trametinib for the treatment of adult and paediatric …

SHP2 inhibition sensitizes diverse oncogene-addicted solid tumors to re-treatment with targeted therapy

A Drilon, MR Sharma, ML Johnson, TA Yap, S Gadgeel… - Cancer discovery, 2023 - AACR
Rationally targeted therapies have transformed cancer treatment, but many patients develop
resistance through bypass signaling pathway activation. PF-07284892 (ARRY-558) is an …