[HTML][HTML] Post-translational modification of GPX4 is a promising target for treating ferroptosis-related diseases

C Cui, F Yang, Q Li - Frontiers in Molecular Biosciences, 2022 - frontiersin.org
Glutathione peroxidase 4 (GPX4) is one of the most important antioxidant enzymes. As the
key regulator of ferroptosis, GPX4 has attracted considerable attention in the fields of cancer …

[HTML][HTML] Deubiquitinase-targeting chimeras for targeted protein stabilization

NJ Henning, L Boike, JN Spradlin, CC Ward… - Nature chemical …, 2022 - nature.com
Many diseases are driven by proteins that are aberrantly ubiquitinated and degraded. These
diseases would be therapeutically benefited by targeted protein stabilization (TPS). Here we …

Discovery of a covalent FEM1B recruiter for targeted protein degradation applications

NJ Henning, AG Manford, JN Spradlin… - Journal of the …, 2022 - ACS Publications
Proteolysis-targeting chimeras (PROTACs), heterobifunctional compounds that consist of
protein-targeting ligands linked to an E3 ligase recruiter, have arisen as a powerful …

[HTML][HTML] Cortex periplocae modulates the gut microbiota to restrict colitis and colitis-associated colorectal cancer via suppression of pathogenic Th17 cells

Z Lin, L Chen, M Cheng, F Zhu, X Yang, W Zhao… - Biomedicine & …, 2022 - Elsevier
Aberrant microbe-immune cell interaction is a predisposing factor in inflammatory bowel
disease (IBD) and colitis-associated cancer (CAC). Cortex Periplocae is a famous traditional …

[HTML][HTML] GPX4 suppresses ferroptosis to promote malignant progression of endometrial carcinoma via transcriptional activation by ELK1

S Wei, Z Yu, R Shi, L An, Q Zhang, Q Zhang, T Zhang… - BMC cancer, 2022 - Springer
Abstract Background Glutathione Peroxidase 4 (GPX4) is a key protein that inhibits
ferroptosis. However, its biological regulation and mechanism in endometrial cancer (EC) …

Discovery of Non-Cysteine-Targeting Covalent Inhibitors by Activity-Based Proteomic Screening with a Cysteine-Reactive Probe

Y Jung, N Noda, J Takaya, M Abo, K Toh… - ACS Chemical …, 2022 - ACS Publications
Covalent inhibitors of enzymes are increasingly appreciated as pharmaceutical seeds, yet
discovering non-cysteine-targeting inhibitors remains challenging. Herein, we report an …

[HTML][HTML] Biased holoenzyme assembly of protein phosphatase 2A (PP2A): From cancer to small molecules

TJ Haanen, CM O'Connor, G Narla - Journal of Biological Chemistry, 2022 - ASBMB
Protein phosphatase 2A (PP2A) is a family of serine threonine phosphatases responsible for
regulating protein phosphorylation, thus opposing the activity of cellular kinases. PP2A is …

[HTML][HTML] Withaferin A, a polyfunctional pharmacophore that includes covalent engagement of IPO5, is an inhibitor of influenza A replication

R Patouret, S Barluenga, N Winssinger - Bioorganic & Medicinal Chemistry, 2022 - Elsevier
Withaferin A, a natural steroidal lactone found in the extracts of Withania somnifera, is used
extensively in traditional medicine and part of an ancient remedy in ayurvedic medicine …

[图书][B] Chemoproteomics-enabled Discovery of Covalent Inhibitors and Novel Induced Proximity Platforms

L Boike - 2022 - search.proquest.com
Covalent drugs incorporate a mildly electrophilic functional group that reacts with protein
targets to confer additional affinity beyond the non-covalent interactions involved in drug …

Chemoproteomic target-class drug discovery against the deubiquitinating enzymes

WC Chan - 2022 - search.proquest.com
Modern small molecule drug discovery is dominated, and subsequently limited by a
paradigm of reversible non-covalent inhibitors. The deubiquitinating enzymes (DUBs) is a …