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 …

The dawn of a new era: targeting the “undruggables” with antibody-based therapeutics

L Qian, X Lin, X Gao, RU Khan, JY Liao, S Du… - Chemical …, 2023 - ACS Publications
The high selectivity and affinity of antibodies toward their antigens have made them a highly
valuable tool in disease therapy, diagnosis, and basic research. A plethora of chemical and …

Therapeutic developments in pancreatic cancer

ZI Hu, EM O'Reilly - Nature Reviews Gastroenterology & Hepatology, 2024 - nature.com
Pancreatic ductal adenocarcinoma (PDAC) has a rising incidence and is one of the most
lethal human malignancies. Much is known regarding the biology and pathophysiology of …

Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation

MJ Bond, CM Crews - RSC chemical biology, 2021 - pubs.rsc.org
With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …

Molecular network of colorectal cancer and current therapeutic options

Z Huang, M Yang - Frontiers in oncology, 2022 - frontiersin.org
Colorectal cancer (CRC), a leading cause of cancer-related mortalities globally, results from
the accumulation of multiple genetic and epigenetic alterations in the normal colonic and …

[HTML][HTML] Targeting KRAS in non-small-cell lung cancer: recent progress and new approaches

M Reck, DP Carbone, M Garassino, F Barlesi - Annals of Oncology, 2021 - Elsevier
Rat sarcoma (RAS) is the most frequently mutated oncogene in human cancer, with Kirsten
rat sarcoma (KRAS) being the most commonly mutated RAS isoform. Overall, KRAS …

Strategies for targeting undruggable targets

G Zhang, J Zhang, Y Gao, Y Li, Y Li - Expert Opinion on Drug …, 2022 - Taylor & Francis
Introduction Undruggable targets refer to clinically meaningful therapeutic targets that are
'difficult to drug'or 'yet to be drugged'via traditional approaches. Featuring characteristics of …

Selective and noncovalent targeting of RAS mutants for inhibition and degradation

KW Teng, ST Tsai, T Hattori, C Fedele, A Koide… - Nature …, 2021 - nature.com
Activating mutants of RAS are commonly found in human cancers, but to date selective
targeting of RAS in the clinic has been limited to KRAS (G12C) through covalent inhibitors …

Proteome-scale discovery of protein degradation and stabilization effectors

J Poirson, H Cho, A Dhillon, S Haider, AZ Imrit… - Nature, 2024 - nature.com
Targeted protein degradation and stabilization are promising therapeutic modalities
because of their potency, versatility and their potential to expand the druggable target …

Opportunities and challenges of protein-based targeted protein degradation

F Shen, LMK Dassama - Chemical Science, 2023 - pubs.rsc.org
In the 20 years since the first report of a proteolysis targeting chimeric (PROTAC) molecule,
targeted protein degradation (TPD) technologies have attempted to revolutionize the fields …