Discovery of small molecule ligands for the von Hippel-Lindau (VHL) E3 ligase and their use as inhibitors and PROTAC degraders

CJ Diehl, A Ciulli - Chemical Society Reviews, 2022 - pubs.rsc.org
The von Hippel-Lindau (VHL) Cullin RING E3 ligase is an essential enzyme in the ubiquitin-
proteasome system that recruits substrates such as the hypoxia inducible factor for …

PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy

JM Kelm, DS Pandey, E Malin, H Kansou, S Arora… - Molecular Cancer, 2023 - Springer
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …

FAK in cancer: from mechanisms to therapeutic strategies

HH Chuang, YY Zhen, YC Tsai, CH Chuang… - International journal of …, 2022 - mdpi.com
Focal adhesion kinase (FAK), a non-receptor tyrosine kinase, is overexpressed and
activated in many cancer types. FAK regulates diverse cellular processes, including growth …

Driving E3 ligase substrate specificity for targeted protein degradation: lessons from nature and the laboratory

AD Cowan, A Ciulli - Annual review of biochemistry, 2022 - annualreviews.org
Methods to direct the degradation of protein targets with proximity-inducing molecules that
coopt the cellular degradation machinery are advancing in leaps and bounds, and diverse …

FAK in cancer: mechanistic findings and clinical applications

FJ Sulzmaier, C Jean, DD Schlaepfer - Nature reviews cancer, 2014 - nature.com
Focal adhesion kinase (FAK) is a cytoplasmic protein tyrosine kinase that is overexpressed
and activated in several advanced-stage solid cancers. FAK promotes tumour progression …

FAK signaling in human cancer as a target for therapeutics

BY Lee, P Timpson, LG Horvath, RJ Daly - Pharmacology & therapeutics, 2015 - Elsevier
Focal adhesion kinase (FAK) is a key regulator of growth factor receptor-and integrin-
mediated signals, governing fundamental processes in normal and cancer cells through its …

Discovery and characterisation of highly cooperative FAK‐degrading PROTACs

RP Law, J Nunes, C Chung… - Angewandte Chemie …, 2021 - Wiley Online Library
Focal adhesion kinase (FAK) is a key mediator of tumour progression and metastasis. To
date, clinical trials of FAK inhibitors have reported disappointing efficacy for oncology …

Emerging roles of focal adhesion kinase in cancer

YL Tai, LC Chen, TL Shen - BioMed research international, 2015 - Wiley Online Library
Focal adhesion kinase (FAK) is a cytoplasmic nonreceptor tyrosine kinase that enables
activation by growth factor receptors or integrins in various types of human cancers. The …

Targeting focal adhesion kinase (FAK) in cancer therapy: A recent update on inhibitors and PROTAC degraders

X Wang, N Li, YH Liu, J Wu, QG Liu, JB Niu… - European Journal of …, 2024 - Elsevier
Focal adhesion kinase (FAK) is considered as a pivotal intracellular non-receptor tyrosine
kinase, and has garnered significant attention as a promising target for anticancer drug …

Focal adhesion kinase: from biological functions to therapeutic strategies

X Tan, Y Yan, B Song, S Zhu, Q Mei, K Wu - Experimental Hematology & …, 2023 - Springer
Focal adhesion kinase (FAK), a nonreceptor cytoplasmic tyrosine kinase, is a vital
participant in primary cellular functions, such as proliferation, survival, migration, and …