E3 ligase ligands for PROTACs: how they were found and how to discover new ones

T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …

Recent insight into the role of FBXW7 as a tumor suppressor

K Yumimoto, KI Nakayama - Seminars in cancer biology, 2020 - Elsevier
FBXW7 (also known as Fbw7, Sel10, hCDC4, or hAgo) is a tumor suppressor and the most
frequently mutated member of the F-box protein family in human cancers. FBXW7 functions …

A role for APP in Wnt signalling links synapse loss with β-amyloid production

C Elliott, AI Rojo, E Ribe, M Broadstock, W Xia… - Translational …, 2018 - nature.com
In Alzheimer's disease (AD), the canonical Wnt inhibitor Dickkopf-1 (Dkk1) is induced by β-
amyloid (Aβ) and shifts the balance from canonical towards non-canonical Wnt signalling …

Cryo-EM structure of C9ORF72–SMCR8–WDR41 reveals the role as a GAP for Rab8a and Rab11a

D Tang, J Sheng, L Xu, X Zhan, J Liu… - Proceedings of the …, 2020 - National Acad Sciences
A massive intronic hexanucleotide repeat (GGGGCC) expansion in C9ORF72 is a genetic
origin of amyotrophic lateral sclerosis (ALS) and frontotemporal dementia (FTD). Recently …

The ubiquitin proteasome system and schizophrenia

S Luza, CM Opazo, CA Bousman, C Pantelis… - The Lancet …, 2020 - thelancet.com
The ubiquitin-proteasome system is a master regulator of neural development and the
maintenance of brain structure and function. It influences neurogenesis, synaptogenesis …

Germline variants in tumor suppressor FBXW7 lead to impaired ubiquitination and a neurodevelopmental syndrome

SEM Stephenson, G Costain, LER Blok, MA Silk… - The American Journal of …, 2022 - cell.com
Neurodevelopmental disorders are highly heterogenous conditions resulting from
abnormalities of brain architecture and/or function. FBXW7 (F-box and WD-repeat-domain …

Exploiting the cullin E3 ligase adaptor protein SKP1 for targeted protein degradation

SH Hong, A Divakaran, A Osa, OW Huang… - ACS chemical …, 2024 - ACS Publications
Targeted protein degradation with proteolysis targeting chimeras (PROTACs) is a powerful
therapeutic modality for eliminating disease-causing proteins through targeted ubiquitination …

F-box proteins and cancer

K Yumimoto, Y Yamauchi, KI Nakayama - Cancers, 2020 - mdpi.com
Controlled protein degradation is essential for the operation of a variety of cellular processes
including cell division, growth, and differentiation. Identification of the relations between …

Global identification of phospho-dependent SCF substrates reveals a FBXO22 phosphodegron and an ERK-FBXO22-BAG3 axis in tumorigenesis

P Liu, X Cong, S Liao, X Jia, X Wang, W Dai… - Cell Death & …, 2022 - nature.com
Abstract SKP1-CUL1-F-box (SCF) ubiquitin ligases play fundamental roles in cellular
functions. Typically, substrate phosphorylation is required for SCF recognition and …

Implications of FBXW7 in neurodevelopment and neurodegeneration: molecular mechanisms and therapeutic potential

Y Yang, X Zhou, X Liu, R Song, Y Gao… - Frontiers in Cellular …, 2021 - frontiersin.org
The ubiquitin-proteasome system (UPS) mediated protein degradation is crucial to maintain
quantitive and functional homeostasis of diverse proteins. Balanced cellular protein …