The current state of the art and future trends in RAS-targeted cancer therapies

SR Punekar, V Velcheti, BG Neel… - Nature reviews Clinical …, 2022 - nature.com
Despite being the most frequently altered oncogenic protein in solid tumours, KRAS has
historically been considered 'undruggable'owing to a lack of pharmacologically targetable …

KRAS mutation: from undruggable to druggable in cancer

L Huang, Z Guo, F Wang, L Fu - Signal transduction and targeted …, 2021 - nature.com
Cancer is the leading cause of death worldwide, and its treatment and outcomes have been
dramatically revolutionised by targeted therapies. As the most frequently mutated oncogene …

Rational combinations of targeted cancer therapies: background, advances and challenges

H Jin, L Wang, R Bernards - Nature Reviews Drug Discovery, 2023 - nature.com
Over the past two decades, elucidation of the genetic defects that underlie cancer has
resulted in a plethora of novel targeted cancer drugs. Although these agents can initially be …

RAS-targeted therapies: is the undruggable drugged?

AR Moore, SC Rosenberg, F McCormick… - Nature reviews Drug …, 2020 - nature.com
Abstract RAS (KRAS, NRAS and HRAS) is the most frequently mutated gene family in
cancers, and, consequently, investigators have sought an effective RAS inhibitor for more …

Targeting KRAS mutant cancers: from druggable therapy to drug resistance

C Zhu, X Guan, X Zhang, X Luan, Z Song, X Cheng… - Molecular cancer, 2022 - Springer
Abstract Kirsten Rat Sarcoma Viral Oncogene Homolog (KRAS) is the most frequently
mutated oncogene, occurring in a variety of tumor types. Targeting KRAS mutations with …

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 …

BI-3406, a potent and selective SOS1–KRAS interaction inhibitor, is effective in KRAS-driven cancers through combined MEK inhibition

MH Hofmann, M Gmachl, J Ramharter, F Savarese… - Cancer Discovery, 2021 - AACR
KRAS is the most frequently mutated driver of pancreatic, colorectal, and non–small cell lung
cancers. Direct KRAS blockade has proved challenging, and inhibition of a key downstream …

Cancer cell-derived exosomal circUSP7 induces CD8+ T cell dysfunction and anti-PD1 resistance by regulating the miR-934/SHP2 axis in NSCLC

SW Chen, SQ Zhu, X Pei, BQ Qiu, D Xiong, X Long… - Molecular cancer, 2021 - Springer
Background CD8+ T cells play a critical role in the innate antitumour immune response.
Recently, CD8+ T cell dysfunction has been verified in various malignant cancers, including …

Molecular alterations and targeted therapy in pancreatic ductal adenocarcinoma

Y Qian, Y Gong, Z Fan, G Luo, Q Huang… - Journal of hematology & …, 2020 - Springer
Pancreatic ductal adenocarcinoma (PDAC) is a malignancy characterized by a poor
prognosis and high mortality rate. Genetic mutations and altered molecular pathways serve …

Pancreatic ductal adenocarcinoma: biological hallmarks, current status, and future perspectives of combined modality treatment approaches

M Orth, P Metzger, S Gerum, J Mayerle, G Schneider… - Radiation …, 2019 - Springer
Pancreatic ductal adenocarcinoma (PDAC) is a highly devastating disease with poor
prognosis and rising incidence. Late detection and a particularly aggressive biology are the …