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 …
strategy using small molecules to induce ubiquitin-dependent degradation of proteins. It has …
PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)
M He, C Cao, Z Ni, Y Liu, P Song, S Hao, Y He… - … and Targeted Therapy, 2022 - nature.com
Abstract PROteolysis TArgeting Chimeras (PROTACs) technology is a new protein-
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
degradation strategy that has emerged in recent years. It uses bifunctional small molecules …
Therapeutic targeting of “undruggable” MYC
V Llombart, MR Mansour - EBioMedicine, 2022 - thelancet.com
Summary c-MYC controls global gene expression and regulates cell proliferation, cell
differentiation, cell cycle, metabolism and apoptosis. According to some estimates, MYC is …
differentiation, cell cycle, metabolism and apoptosis. According to some estimates, MYC is …
A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models
Interactions between WD40 repeat domain protein 5 (WDR5) and its various partners such
as mixed lineage leukemia (MLL) and c-MYC are essential for sustaining oncogenesis in …
as mixed lineage leukemia (MLL) and c-MYC are essential for sustaining oncogenesis in …
KMT2A associates with PHF5A-PHF14-HMG20A-RAI1 subcomplex in pancreatic cancer stem cells and epigenetically regulates their characteristics
Pancreatic cancer (PC), one of the most aggressive and life-threatening human
malignancies, is known for its resistance to cytotoxic therapies. This is increasingly ascribed …
malignancies, is known for its resistance to cytotoxic therapies. This is increasingly ascribed …
Discovery of a dual WDR5 and Ikaros PROTAC degrader as an anti-cancer therapeutic
Abstract WD repeat domain 5 (WDR5), an integral component of the MLL/KMT2A lysine
methyltransferase complex, is critically involved in oncogenesis and represents an attractive …
methyltransferase complex, is critically involved in oncogenesis and represents an attractive …
Interaction of the oncoprotein transcription factor MYC with its chromatin cofactor WDR5 is essential for tumor maintenance
LR Thomas, CM Adams, J Wang… - Proceedings of the …, 2019 - National Acad Sciences
The oncoprotein transcription factor MYC is overexpressed in the majority of cancers. Key to
its oncogenic activity is the ability of MYC to regulate gene expression patterns that drive …
its oncogenic activity is the ability of MYC to regulate gene expression patterns that drive …
Small molecule targeting of chromatin writers in cancer
AR Conery, JL Rocnik, P Trojer - Nature Chemical Biology, 2022 - nature.com
More than a decade after the launch of DNA methyltransferase and histone deacetylase
inhibitors for the treatment of cancer, 2020 heralded the approval of the first histone …
inhibitors for the treatment of cancer, 2020 heralded the approval of the first histone …
Structure, function and inhibition of critical protein–protein interactions involving mixed lineage leukemia 1 and its fusion oncoproteins
Abstract Mixed lineage leukemia 1 (MLL1, also known as MLL or KMT2A) is an important
transcription factor and histone-H3 lysine-4 (H3K4) methyltransferase. It is a master …
transcription factor and histone-H3 lysine-4 (H3K4) methyltransferase. It is a master …
Unannotated microprotein EMBOW regulates the interactome and chromatin and mitotic functions of WDR5
The conserved WD40-repeat protein WDR5 interacts with multiple proteins both inside and
outside the nucleus. However, it is currently unclear whether and how the distribution of …
outside the nucleus. However, it is currently unclear whether and how the distribution of …