Small molecule NF-κB pathway inhibitors in clinic

V Ramadass, T Vaiyapuri, V Tergaonkar - International journal of …, 2020 - mdpi.com
Nuclear factor kappa B (NF-κB) signaling is implicated in all major human chronic diseases,
with its role in transcription of hundreds of gene well established in the literature. This has …

Small-molecule inhibitors of protein-protein interactions: progressing toward the reality

MR Arkin, Y Tang, JA Wells - Chemistry & biology, 2014 - cell.com
The past 20 years have seen many advances in our understanding of protein-protein
interactions (PPIs) and how to target them with small-molecule therapeutics. In 2004, we …

In vivo CRISPR screens identify the E3 ligase Cop1 as a modulator of macrophage infiltration and cancer immunotherapy target

X Wang, C Tokheim, SS Gu, B Wang, Q Tang, Y Li… - Cell, 2021 - cell.com
Despite remarkable clinical efficacy of immune checkpoint blockade (ICB) in cancer
treatment, ICB benefits for triple-negative breast cancer (TNBC) remain limited. Through …

TRIM8 modulates the EWS/FLI oncoprotein to promote survival in Ewing sarcoma

BKA Seong, NV Dharia, S Lin, KA Donovan, S Chong… - Cancer cell, 2021 - cell.com
Fusion-transcription factors (fusion-TFs) represent a class of driver oncoproteins that are
difficult to therapeutically target. Recently, protein degradation has emerged as a strategy to …

Snapshots and ensembles of BTK and cIAP1 protein degrader ternary complexes

J Schiemer, R Horst, Y Meng, JI Montgomery… - Nature Chemical …, 2021 - nature.com
Heterobifunctional chimeric degraders are a class of ligands that recruit target proteins to E3
ubiquitin ligases to drive compound-dependent protein degradation. Advancing from initial …

Absence of RIPK3 predicts necroptosis resistance in malignant melanoma

P Geserick, J Wang, R Schilling, S Horn, PA Harris… - Cell death & …, 2015 - nature.com
Acquired or intrinsic resistance to apoptotic and necroptotic stimuli is considered a major
hindrance of therapeutic success in malignant melanoma. Inhibitor of apoptosis proteins …

Inhibitor of apoptosis protein (IAP) antagonists in anticancer agent discovery: Current status and perspectives

H Cong, L Xu, Y Wu, Z Qu, T Bian… - Journal of Medicinal …, 2019 - ACS Publications
Apoptosis, an important form of programmed cell death (PCD), is a tightly regulated cellular
process to eliminate unwanted or damaged cells. Resistance of apoptosis is a hallmark of …

[HTML][HTML] Small molecules targeting protein–protein interactions for cancer therapy

D Wu, Y Li, L Zheng, H Xiao, L Ouyang, G Wang… - … Pharmaceutica Sinica B, 2023 - Elsevier
Protein–protein interactions (PPIs) are fundamental to many biological processes that play
an important role in the occurrence and development of a variety of diseases. Targeting the …

Molecular pathways: the balance between cancer and the immune system challenges the therapeutic specificity of targeting nuclear factor-κB signaling for cancer …

KP Zeligs, MK Neuman, CM Annunziata - Clinical Cancer Research, 2016 - AACR
The NF-κB signaling pathway is a complex network linking extracellular stimuli to cell
survival and proliferation. Cytoplasmic signaling to activate NF-κB can occur as part of the …

Therapeutic inducers of apoptosis in ovarian cancer

M Binju, MA Amaya-Padilla, G Wan, H Gunosewoyo… - Cancers, 2019 - mdpi.com
Ovarian cancers remain one of the most common causes of gynecologic cancer-related
death in women worldwide. The standard treatment comprises platinum-based …