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发表于

Article title

Covalent adduct Grob fragmentation underlies LSD1 demethylase-specific inhibitor mechanism of action and resistance

LSD1 inhibitors utilize Grob fragmentation to exhibit different mechanism of action
LSD1 inhibitors utilize Grob fragmentation to exhibit different mechanism of action

Journal

Nature Communications

Tags

Inhibitor mode of action; LSD1 inhibitor; covalent drug

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Article title

A PARP2 active site helix melts to permit DNA damage-induced enzymatic activation

PARP2 utilizes an active site helix to permit DNA-induced activation
PARP2 utilizes an active site helix to permit DNA-induced activation

Journal

Molecular Cell

Tags

ADP-ribosylation; Allosteric activation; HDX-MS

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Article title

Bidirectional histone monoaminylation dynamics regulate neural rhythmicity

Histone monoaminylation shows dynamic and regulates neural rhythmicity
Histone monoaminylation shows dynamic and regulates neural rhythmicity

Journal

Nature

Tags

Histone PTMs; Metabolic PTMs; Genetics

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Article title

Human HDAC6 senses valine abundancy to regulate DNA damage

Human HDAC6 senses valine abundancy to regulate DNA damage
HDAC is a sensor of valine leading to DNA damage and potent cancer treatment

Journal

Nature

Tags

Small molecule metabolites; DNA damage; Novel cellular pathways

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Article title

Structure-guided discovery of bile acid derivatives for treating liver diseases without causing itch

Structure-guided discovery of bile acid molecules for liver diseases without itch
Discover liver disease-targeting small molecule without itch adverse effect

Journal

Cell

Tags

Cryo-EM structure, Drug rational design

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Article title

Targeting cancer with small-molecule pan-KRAS degraders

Targeting cancer with pan-KRAS PROTAC molecule
Targeting cancer with pan-KRAS PROTAC molecule

Journal

Science

Tags

PROTAC, Drug screening

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Article title

Cancer-associated DNA hypermethylation of Polycomb targets requires DNMT3A dual recognition of histone H2AK119 ubiquitination and the nucleosome acidic patch

Cryo-EM structure of DNMT3A1 UDR domain with H2A119Ub NCP
Cryo-EM structure of DNMT3A1 UDR domain with H2A119Ub NCP

Journal

Science Advances

Tags

DNA methylation; Ubiquitinated nucleosome complex; Genetics

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