Chemistries of bifunctional PROTAC degraders

C Cao, M He, L Wang, Y He, Y Rao - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis targeting chimeras (PROTACs) technology is a novel and promising therapeutic
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …

Tumor cell plasticity in targeted therapy-induced resistance: mechanisms and new strategies

ZD Shi, K Pang, ZX Wu, Y Dong, L Hao… - … and Targeted Therapy, 2023 - nature.com
Despite the success of targeted therapies in cancer treatment, therapy-induced resistance
remains a major obstacle to a complete cure. Tumor cells evade treatments and relapse via …

The E-cadherin and N-cadherin switch in epithelial-to-mesenchymal transition: signaling, therapeutic implications, and challenges

CY Loh, JY Chai, TF Tang, WF Wong, G Sethi… - Cells, 2019 - mdpi.com
Epithelial-to-Mesenchymal Transition (EMT) has been shown to be crucial in tumorigenesis
where the EMT program enhances metastasis, chemoresistance and tumor stemness. Due …

PROTACs: great opportunities for academia and industry

X Sun, H Gao, Y Yang, M He, Y Wu, Y Song… - Signal transduction and …, 2019 - nature.com
Although many kinds of therapies are applied in the clinic, drug-resistance is a major and
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …

PROTAC: an effective targeted protein degradation strategy for cancer therapy

SM Qi, J Dong, ZY Xu, XD Cheng, WD Zhang… - Frontiers in …, 2021 - frontiersin.org
Proteolysis targeting chimeric (PROTAC) technology is an effective endogenous protein
degradation tool developed in recent years that can ubiquitinate the target proteins through …

JAK-STAT signaling: a double-edged sword of immune regulation and cancer progression

KL Owen, NK Brockwell, BS Parker - Cancers, 2019 - mdpi.com
Janus kinase-signal transducer and activator of transcription (JAK-STAT) signaling mediates
almost all immune regulatory processes, including those that are involved in tumor cell …

EZH2 inhibition activates a dsRNA–STING–interferon stress axis that potentiates response to PD-1 checkpoint blockade in prostate cancer

KL Morel, AV Sheahan, DL Burkhart, SC Baca… - Nature cancer, 2021 - nature.com
Prostate cancers are considered to be immunologically 'cold'tumors given the very few
patients who respond to checkpoint inhibitor (CPI) therapy. Recently, enrichment of …

Enhancers in disease: molecular basis and emerging treatment strategies

A Claringbould, JB Zaugg - Trends in molecular medicine, 2021 - cell.com
Enhancers are genomic sequences that play a key role in regulating tissue-specific gene
expression levels. An increasing number of diseases are linked to impaired enhancer …

Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges

S Zeng, W Huang, X Zheng, Z Zhang, J Wang… - European journal of …, 2021 - Elsevier
Proteolysis targeting chimera (PROTAC), hijacking protein of interest (POI) and recruiting E3
ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug …

Aberrant chromatin reorganization in cells from diseased fibrous connective tissue in response to altered chemomechanical cues

SJ Heo, S Thakur, X Chen, C Loebel, B Xia… - Nature biomedical …, 2023 - nature.com
Abstract Changes in the micro-environment of fibrous connective tissue can lead to
alterations in the phenotypes of tissue-resident cells, yet the underlying mechanisms are …