Targeting RNA structures with small molecules
JL Childs-Disney, X Yang, QMR Gibaut… - Nature Reviews Drug …, 2022 - nature.com
RNA adopts 3D structures that confer varied functional roles in human biology and
dysfunction in disease. Approaches to therapeutically target RNA structures with small …
dysfunction in disease. Approaches to therapeutically target RNA structures with small …
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 …
historically been considered 'undruggable'owing to a lack of pharmacologically targetable …
[HTML][HTML] Single-Agent Divarasib (GDC-6036) in Solid Tumors with a KRAS G12C Mutation
A Sacher, P LoRusso, MR Patel… - … England Journal of …, 2023 - Mass Medical Soc
Abstract Background Divarasib (GDC-6036) is a covalent KRAS G12C inhibitor that was
designed to have high potency and selectivity. Methods In a phase 1 study, we evaluated …
designed to have high potency and selectivity. Methods In a phase 1 study, we evaluated …
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] Small molecules in targeted cancer therapy: advances, challenges, and future perspectives
L Zhong, Y Li, L Xiong, W Wang, M Wu… - Signal transduction and …, 2021 - nature.com
Due to the advantages in efficacy and safety compared with traditional chemotherapy drugs,
targeted therapeutic drugs have become mainstream cancer treatments. Since the first …
targeted therapeutic drugs have become mainstream cancer treatments. Since the first …
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 …
treatment of solid tumors. However, when compared to KRASG12C, selective inhibition of …
Cystine transporter SLC7A11/xCT in cancer: ferroptosis, nutrient dependency, and cancer therapy
The cystine/glutamate antiporter SLC7A11 (also commonly known as xCT) functions to
import cystine for glutathione biosynthesis and antioxidant defense and is overexpressed in …
import cystine for glutathione biosynthesis and antioxidant defense and is overexpressed in …
Recent advances in the development of protein–protein interactions modulators: mechanisms and clinical trials
H Lu, Q Zhou, J He, Z Jiang, C Peng, R Tong… - Signal transduction and …, 2020 - nature.com
Protein–protein interactions (PPIs) have pivotal roles in life processes. The studies showed
that aberrant PPIs are associated with various diseases, including cancer, infectious …
that aberrant PPIs are associated with various diseases, including cancer, infectious …
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 …
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 …
mutated oncogene, occurring in a variety of tumor types. Targeting KRAS mutations with …