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 …

Targeting KRAS in pancreatic cancer: new drugs on the horizon

SF Bannoura, MH Uddin, M Nagasaka, F Fazili… - Cancer and Metastasis …, 2021 - Springer
Abstract Kirsten Rat Sarcoma (KRAS) is a master oncogene involved in cellular proliferation
and survival and is the most commonly mutated oncogene in all cancers. Activating KRAS …

Identification of MRTX1133, a Noncovalent, Potent, and Selective KRASG12D Inhibitor

X Wang, S Allen, JF Blake, V Bowcut… - Journal of medicinal …, 2021 - ACS Publications
KRASG12D, the most common oncogenic KRAS mutation, is a promising target for the
treatment of solid tumors. However, when compared to KRASG12C, selective inhibition of …

Development of orally bioavailable peptides targeting an intracellular protein: from a hit to a clinical KRAS inhibitor

M Tanada, M Tamiya, A Matsuo… - Journal of the …, 2023 - ACS Publications
Cyclic peptides as a therapeutic modality are attracting a lot of attention due to their potential
for oral absorption and accessibility to intracellular tough targets. Here, starting with a drug …

Selection of Nucleotide-Encoded Mass Libraries of Macrocyclic Peptides for Inaccessible Drug Targets

K Colas, D Bindl, H Suga - Chemical Reviews, 2024 - ACS Publications
Technological advances and breakthrough developments in the pharmaceutical field are
knocking at the door of the “undruggable” fortress with increasing insistence. Notably, the …

Tackling undruggable targets with designer peptidomimetics and synthetic biologics

CS Swenson, G Mandava, DM Thomas… - Chemical …, 2024 - ACS Publications
The development of potent, specific, and pharmacologically viable chemical probes and
therapeutics is a central focus of chemical biology and therapeutic development. However, a …

KRAS mutation: The booster of pancreatic ductal adenocarcinoma transformation and progression

Z Zhang, H Zhang, X Liao, H Tsai - Frontiers in Cell and …, 2023 - frontiersin.org
Pancreatic ductal adenocarcinoma (PDAC) is the most common type of pancreatic cancer. It
has a poor response to conventional therapy and has an extremely poor 5-year survival rate …

[HTML][HTML] Strategies to tackle RAS-mutated metastatic colorectal cancer

G Patelli, F Tosi, A Amatu, G Mauri, A Curaba… - ESMO open, 2021 - Elsevier
The RAS oncogene is among the most commonly mutated in cancer. RAS mutations are
identified in about half of patients diagnosed with metastatic colorectal cancer (mCRC) …

Targeting small GTPases: emerging grasps on previously untamable targets, pioneered by KRAS

G Yin, J Huang, J Petela, H Jiang, Y Zhang… - Signal transduction and …, 2023 - nature.com
Abstract Small GTPases including Ras, Rho, Rab, Arf, and Ran are omnipresent molecular
switches in regulating key cellular functions. Their dysregulation is a therapeutic target for …

Targeting intracellular protein–protein interactions with macrocyclic peptides

M Buyanova, D Pei - Trends in pharmacological sciences, 2022 - cell.com
Intracellular protein–protein interactions (PPIs) are challenging targets for traditional drug
modalities. Macrocyclic peptides (MPs) prove highly effective PPI inhibitors in vitro and can …