Protein degraders enter the clinic—a new approach to cancer therapy

D Chirnomas, KR Hornberger, CM Crews - Nature Reviews Clinical …, 2023 - nature.com
Heterobifunctional protein degraders, such as PROteolysis TArgeting Chimera (PROTAC)
protein degraders, constitute a novel therapeutic modality that harnesses the cell's natural …

Epigenetic modifications of histones in cancer

Z Zhao, A Shilatifard - Genome biology, 2019 - Springer
The epigenetic modifications of histones are versatile marks that are intimately connected to
development and disease pathogenesis including human cancers. In this review, we will …

The BioGRID database: A comprehensive biomedical resource of curated protein, genetic, and chemical interactions

R Oughtred, J Rust, C Chang, BJ Breitkreutz… - Protein …, 2021 - Wiley Online Library
Abstract The BioGRID (Biological General Repository for Interaction Datasets, thebiogrid.
org) is an open‐access database resource that houses manually curated protein and …

The BioGRID interaction database: 2019 update

R Oughtred, C Stark, BJ Breitkreutz, J Rust… - Nucleic acids …, 2019 - academic.oup.com
Abstract The Biological General Repository for Interaction Datasets (BioGRID:
https://thebiogrid. org) is an open access database dedicated to the curation and archival …

Emerging strategies to overcome resistance to third-generation EGFR inhibitors

K Shi, G Wang, J Pei, J Zhang, J Wang… - Journal of Hematology & …, 2022 - Springer
Epidermal growth factor receptor (EGFR), the receptor for members of the epidermal growth
factor family, regulates cell proliferation and signal transduction; moreover, EGFR is related …

Overcoming resistance to tumor-targeted and immune-targeted therapies

M Aldea, F Andre, A Marabelle, S Dogan, F Barlesi… - Cancer Discovery, 2021 - AACR
Resistance to anticancer therapies includes primary resistance, usually related to lack of
target dependency or presence of additional targets, and secondary resistance, mostly …

Targeted protein degradation: elements of PROTAC design

SL Paiva, CM Crews - Current opinion in chemical biology, 2019 - Elsevier
Targeted protein degradation using Proteolysis Targeting Chimeras (PROTACs) has
emerged as a novel therapeutic modality in drug discovery. PROTACs mediate the …

Bromodomains: a new target class for drug development

AG Cochran, AR Conery, RJ Sims III - Nature Reviews Drug Discovery, 2019 - nature.com
Less than a decade ago, it was shown that bromodomains, acetyl lysine 'reader'modules
found in proteins with varied functions, were highly tractable small-molecule targets. This is …

An overview of PROTACs: a promising drug discovery paradigm

Z Liu, M Hu, Y Yang, C Du, H Zhou, C Liu, Y Chen… - Molecular …, 2022 - Springer
Proteolysis targeting chimeras (PROTACs) technology has emerged as a novel therapeutic
paradigm in recent years. PROTACs are heterobifunctional molecules that degrade target …

Targeting the estrogen receptor for the treatment of breast cancer: recent advances and challenges

RK Rej, JE Thomas, RK Acharyya… - Journal of Medicinal …, 2023 - ACS Publications
Estrogen receptor alpha (ERα) is a well-established therapeutic target for the treatment of
ER-positive (ER+) breast cancers. Despite the tremendous successes achieved with …