Advancing targeted protein degradation for cancer therapy
The human proteome contains approximately 20,000 proteins, and it is estimated that more
than 600 of them are functionally important for various types of cancers, including nearly 400 …
than 600 of them are functionally important for various types of cancers, including nearly 400 …
Myricetin: biological activity related to human health
KS Park, Y Chong, MK Kim - Applied Biological Chemistry, 2016 - Springer
Myricetin (3,5,7,3′,4′,5′-hexahydroxyflavone) is one of the natural flavonols from fruit,
vegetable, tea, and medicinal plants. A great deal of attention has been paid to this compound …
vegetable, tea, and medicinal plants. A great deal of attention has been paid to this compound …
EZH2 noncanonically binds cMyc and p300 through a cryptic transactivation domain to mediate gene activation and promote oncogenesis
Canonically, EZH2 serves as the catalytic subunit of PRC2, which mediates H3K27me3
deposition and transcriptional repression. Here, we report that in acute leukaemias, EZH2 has …
deposition and transcriptional repression. Here, we report that in acute leukaemias, EZH2 has …
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 …
Harnessing the E3 ligase KEAP1 for targeted protein degradation
J Wei, F Meng, KS Park, H Yim, J Velez… - Journal of the …, 2021 - ACS Publications
Proteolysis targeting chimeras (PROTACs) represent a new class of promising therapeutic
modalities. PROTACs hijack E3 ligases and the ubiquitin-proteasome system (UPS), leading …
modalities. PROTACs hijack E3 ligases and the ubiquitin-proteasome system (UPS), leading …
Discovery of a first-in-class EZH2 selective degrader
The enhancer of zeste homolog 2 (EZH2) is the main enzymatic subunit of the PRC2
complex, which catalyzes trimethylation of histone H3 lysine 27 (H3K27me3) to promote …
complex, which catalyzes trimethylation of histone H3 lysine 27 (H3K27me3) to promote …
Bridged proteolysis targeting chimera (PROTAC) enables degradation of undruggable targets
Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for degrading
disease-causing proteins. While many PROTACs have been developed for numerous …
disease-causing proteins. While many PROTACs have been developed for numerous …
In vitro solubility, stability and permeability of novel quercetin–amino acid conjugates
In order to discover a quercetin prodrug with improved bioavailability, we synthesized nine
quercetin–amion acid conjugates and estimated their pharmacokinetic properties including …
quercetin–amion acid conjugates and estimated their pharmacokinetic properties including …
Discovery of the first-in-class G9a/GLP covalent inhibitors
The highly homologous protein lysine methyltransferases G9a and GLP, which catalyze mono-
and dimethylation of histone H3 lysine 9 (H3K9), have been implicated in various human …
and dimethylation of histone H3 lysine 9 (H3K9), have been implicated in various human …
Targeting triple-negative breast cancer by a novel proteolysis targeting chimera degrader of enhancer of zeste homolog 2
B Dale, C Anderson, KS Park… - ACS Pharmacology & …, 2022 - ACS Publications
Enhancer of zeste homolog 2 (EZH2), a catalytic subunit of polycomb repressive complex 2 (PRC2),
is overexpressed in triple-negative breast cancer (TNBC), correlating with poor …
is overexpressed in triple-negative breast cancer (TNBC), correlating with poor …