Jian Jin

Development of a S-adenosylmethionine analog that intrudes the RNA-cap binding site of Zika methyltransferase.

Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia.

Selective inhibitors of protein methyltransferases.

Chemical probes of histone lysine methyltransferases.

A chromatin activity-based chemoproteomic approach reveals a transcriptional repressome for gene-specific silencing.

EZH2 inhibition enhances the efficacy of an EGFR inhibitor in suppressing colon cancer cells.

Structure-activity relationship studies of SETD8 inhibitors.

The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs.

A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3).

Targeting EZH2 and PRC2 dependence as novel anticancer therapy.

Non-canonical Bromodomain within DNA-PKcs Promotes DNA Damage Response and Radioresistance through Recognizing an IR-Induced Acetyl-Lysine on H2AX.

Effects of β-Arrestin-Biased Dopamine D2 Receptor Ligands on Schizophrenia-Like Behavior in Hypoglutamatergic Mice.

The promise and peril of chemical probes.

A Role for Widely Interspaced Zinc Finger (WIZ) in Retention of the G9a Methyltransferase on Chromatin.

A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases.

Genome-wide profiling of histone H3 lysine 27 and lysine 4 trimethylation in multiple myeloma reveals the importance of Polycomb gene targeting and highlights EZH2 as a potential therapeutic target.

Identification of a small-molecule ligand of the epigenetic reader protein Spindlin1 via a versatile screening platform.

Novel Therapeutics Targeting Epigenetics: New Molecules, New Methods.

Topoisomerase 1 inhibition suppresses inflammatory genes and protects from death by inflammation.

Structure-Activity Relationship Studies for Enhancer of Zeste Homologue 2 (EZH2) and Enhancer of Zeste Homologue 1 (EZH1) Inhibitors.

Non-Substrate Based, Small Molecule Inhibitors of the Human Isoprenylcysteine Carboxyl Methyltransferase.

Discovery of a Potent, Selective, and Cell-Active Dual Inhibitor of Protein Arginine Methyltransferase 4 and Protein Arginine Methyltransferase 6.

Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase.

Discovery of G Protein-Biased D2 Dopamine Receptor Partial Agonists.

Distinct cortical and striatal actions of a β-arrestin-biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties.

Targeting the histone methyltransferase G9a activates imprinted genes and improves survival of a mouse model of Prader-Willi syndrome.

EZH2 inhibition in multiple myeloma downregulates myeloma associated oncogenes and upregulates microRNAs with potential tumor suppressor functions.

Epigenetic siRNA and Chemical Screens Identify SETD8 Inhibition as a Therapeutic Strategy for p53 Activation in High-Risk Neuroblastoma.

Discovery of Potent and Selective Inhibitors for G9a-Like Protein (GLP) Lysine Methyltransferase.

Hsp90 inhibition destabilizes Ezh2 protein in alloreactive T cells and reduces graft-versus-host disease in mice.

An Oral Selective Alpha-1A Adrenergic Receptor Agonist Prevents Doxorubicin Cardiotoxicity.

In silico design of novel probes for the atypical opioid receptor MRGPRX2.

Inhibitors of Protein Methyltransferases and Demethylases.

Dual Inhibition of EZH2 and EZH1 Sensitizes PRC2-Dependent Tumors to Proteasome Inhibition.

Recent progress in developing selective inhibitors of protein methyltransferases.

Structure-activity relationship studies of G9a-like protein (GLP) inhibitors.

Report and Application of a Tool Compound Data Set.

Targeted Gene Repression Using Novel Bifunctional Molecules to Harness Endogenous Histone Deacetylation Activity.

Structure-inspired design of β-arrestin-biased ligands for aminergic GPCRs.

VE-Cadherin-Mediated Epigenetic Regulation of Endothelial Gene Expression.

Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3).

The polycomb group protein BMI-1 inhibitor PTC-209 is a potent anti-myeloma agent alone or in combination with epigenetic inhibitors targeting EZH2 and the BET bromodomains.

Discovery of Bisubstrate Inhibitors of Nicotinamide N-Methyltransferase (NNMT).

Inhibition of the G9a/GLP histone methyltransferase complex modulates anxiety-related behavior in mice.

Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK).

Structural determinants of 5-HT receptor activation and biased agonism.

Influenza virus infection causes global RNAPII termination defects.