[HTML][HTML] 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 …
dramatically revolutionised by targeted therapies. As the most frequently mutated oncogene …
[HTML][HTML] PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)
M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
[HTML][HTML] Signaling pathways and therapeutic interventions in gastric cancer
Gastric cancer (GC) ranks fifth in global cancer diagnosis and fourth in cancer-related death.
Despite tremendous progress in diagnosis and therapeutic strategies and significant …
Despite tremendous progress in diagnosis and therapeutic strategies and significant …
The clinical KRAS (G12C) inhibitor AMG 510 drives anti-tumour immunity
J Canon, K Rex, AY Saiki, C Mohr, K Cooke, D Bagal… - Nature, 2019 - nature.com
KRAS is the most frequently mutated oncogene in cancer and encodes a key signalling
protein in tumours,. The KRAS (G12C) mutant has a cysteine residue that has been …
protein in tumours,. The KRAS (G12C) mutant has a cysteine residue that has been …
[HTML][HTML] RAS proteins and their regulators in human disease
DK Simanshu, DV Nissley, F McCormick - Cell, 2017 - cell.com
RAS proteins are binary switches, cycling between ON and OFF states during signal
transduction. These switches are normally tightly controlled, but in RAS-related diseases …
transduction. These switches are normally tightly controlled, but in RAS-related diseases …
Targeted Degradation of Oncogenic KRASG12C by VHL-Recruiting PROTACs
KRAS is mutated in∼ 20% of human cancers and is one of the most sought-after targets for
pharmacological modulation, despite having historically been considered “undruggable.” …
pharmacological modulation, despite having historically been considered “undruggable.” …
Targeting alterations in the RAF–MEK pathway
R Yaeger, RB Corcoran - Cancer discovery, 2019 - AACR
The MAPK pathway is one of the most commonly mutated oncogenic pathways in cancer.
Although RAS mutations are the most frequent MAPK alterations, less frequent alterations in …
Although RAS mutations are the most frequent MAPK alterations, less frequent alterations in …
Drugging an undruggable pocket on KRAS
D Kessler, M Gmachl, A Mantoulidis… - Proceedings of the …, 2019 - National Acad Sciences
The 3 human RAS genes, KRAS, NRAS, and HRAS, encode 4 different RAS proteins which
belong to the protein family of small GTPases that function as binary molecular switches …
belong to the protein family of small GTPases that function as binary molecular switches …
Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design
JML Ostrem, KM Shokat - Nature reviews Drug discovery, 2016 - nature.com
KRAS is the most frequently mutated oncogene in human cancer. In addition to holding this
distinction, unsuccessful attempts to target this protein have led to the characterization of …
distinction, unsuccessful attempts to target this protein have led to the characterization of …
[HTML][HTML] Exploring targeted degradation strategy for oncogenic KRASG12C
KRAS is the most frequently mutated oncogene found in pancreatic, colorectal, and lung
cancers. Although it has been challenging to identify targeted therapies for cancers …
cancers. Although it has been challenging to identify targeted therapies for cancers …