Jaeki Min
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View article: Discovery of a VHL molecular glue degrader of GEMIN3 by Picowell RNA-seq
Discovery of a VHL molecular glue degrader of GEMIN3 by Picowell RNA-seq Open
Targeted protein degradation (TPD) is an emerging therapeutic modality in which small molecules are used to recruit targets to the natural protein degradation machinery of the cell. Molecular glue degraders (MGD) are monovalent small molec…
View article: Data from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i>
Data from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i> Open
Despite improvement in the treatment of medulloblastoma over the last years, numerous patients with MYC- and MYCN-driven tumors still fail current therapies. Medulloblastomas have an intact retinoblastoma protein RB, suggesting that CDK4/6…
View article: Supplementary Table S2 from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Table S2 from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i> Open
Supplementary Table S2
View article: Supplementary Table S4 from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Table S4 from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i> Open
Supplementary Table S4
View article: Supplementary Table S1 from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Table S1 from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i> Open
Supplementary Table S1
View article: Supplementary Table S4 from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Table S4 from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i> Open
Supplementary Table S4
View article: Data from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i>
Data from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i> Open
Despite improvement in the treatment of medulloblastoma over the last years, numerous patients with MYC- and MYCN-driven tumors still fail current therapies. Medulloblastomas have an intact retinoblastoma protein RB, suggesting that CDK4/6…
View article: Supplementary Table S2 from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Table S2 from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i> Open
Supplementary Table S2
View article: Supplementary Methods, Figures and Tables from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Methods, Figures and Tables from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i> Open
Supplementary Methods, Figures S1-S9 and Tables S3, S5-S7
View article: Supplementary Methods, Figures and Tables from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Methods, Figures and Tables from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i> Open
Supplementary Methods, Figures S1-S9 and Tables S3, S5-S7
View article: Supplementary Table S1 from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i>
Supplementary Table S1 from Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i> Open
Supplementary Table S1
View article: Protein–protein interfaces in molecular glue-induced ternary complexes: classification, characterization, and prediction
Protein–protein interfaces in molecular glue-induced ternary complexes: classification, characterization, and prediction Open
This review surveys molecular glue-induced ternary complexes in the PDB and provides an overview of computational methods that can be utilized to predict them.
View article: Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i>
Combination of Ribociclib with BET-Bromodomain and PI3K/mTOR Inhibitors for Medulloblastoma Treatment <i>In Vitro</i> and <i>In Vivo</i> Open
Despite improvement in the treatment of medulloblastoma over the last years, numerous patients with MYC- and MYCN-driven tumors still fail current therapies. Medulloblastomas have an intact retinoblastoma protein RB, suggesting that CDK4/6…
View article: Preclinical evaluation of proteolytic targeting of LCK as a therapeutic approach in T cell acute lymphoblastic leukemia
Preclinical evaluation of proteolytic targeting of LCK as a therapeutic approach in T cell acute lymphoblastic leukemia Open
T cell acute lymphoblastic leukemia (T-ALL) is an aggressive hematological malignancy, and there is an unmet need for targeted therapies, especially for patients with relapsed disease. We have recently identified pre–T cell receptor and ly…
View article: Development of Potent and Selective Janus Kinase 2/3 Directing PG–PROTACs
Development of Potent and Selective Janus Kinase 2/3 Directing PG–PROTACs Open
Aberrant activation of the JAK-STAT signaling pathway has been implicated in the pathogenesis of a range of hematological malignancies and autoimmune disorders. Here we describe the design, synthesis, and characterization of JAK2/3 PROTACs…
View article: CCDC 2113324: Experimental Crystal Structure Determination
CCDC 2113324: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2113322: Experimental Crystal Structure Determination
CCDC 2113322: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Phenyl‐Glutarimides: Alternative Cereblon Binders for the Design of PROTACs
Phenyl‐Glutarimides: Alternative Cereblon Binders for the Design of PROTACs Open
Targeting cereblon (CRBN) is currently one of the most frequently reported proteolysis‐targeting chimera (PROTAC) approaches, owing to favorable drug‐like properties of CRBN ligands, immunomodulatory imide drugs (IMiDs). However, IMiDs are…
View article: Degradation of Janus kinases in <i>CRLF2</i>-rearranged acute lymphoblastic leukemia
Degradation of Janus kinases in <i>CRLF2</i>-rearranged acute lymphoblastic leukemia Open
CRLF2-rearranged (CRLF2r) acute lymphoblastic leukemia (ALL) accounts for more than half of Philadelphia chromosome-like (Ph-like) ALL and is associated with a poor outcome in children and adults. Overexpression of CRLF2 results in activat…
View article: Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators
Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators Open
Whereas the PROTAC approach to target protein degradation greatly benefits from rational design, the discovery of small-molecule degraders relies mostly on phenotypic screening and retrospective target identification efforts. Here, we desc…
View article: BRAF inhibition protects against hearing loss in mice
BRAF inhibition protects against hearing loss in mice Open
Dabrafenib, an FDA-approved oral anticancer drug, prevents cisplatin- and noise-induced hearing loss in animal models.
View article: Development of BODIPY FL Thalidomide As a High-Affinity Fluorescent Probe for Cereblon in a Time-Resolved Fluorescence Resonance Energy Transfer Assay
Development of BODIPY FL Thalidomide As a High-Affinity Fluorescent Probe for Cereblon in a Time-Resolved Fluorescence Resonance Energy Transfer Assay Open
Ligands for cereblon, a component of a functional E3 ligase complex that targets proteins for proteolysis, are critical for developing molecular glues and proteolysis-targeting chimeras (PROTACs), which have therapeutic implications for va…
View article: PDTM-02. TARGETING THE RB PATHWAY IN MEDULLOBLASTOMA
PDTM-02. TARGETING THE RB PATHWAY IN MEDULLOBLASTOMA Open
Medulloblastoma (MB), the most common malignant pediatric brain tumor, is classified into four major molecularly and histopathologically distinct subgroups, among which MYC-driven Group 3 MBs confer a poor prognosis. The Cyclin D/CDK4/CDK6…
View article: Discovery of Novel Pyrazolo-pyridone DCN1 Inhibitors Controlling Cullin Neddylation
Discovery of Novel Pyrazolo-pyridone DCN1 Inhibitors Controlling Cullin Neddylation Open
Chemical control of cullin neddylation is attracting increased attention based largely on the successes of the NEDD8-activating enzyme (E1) inhibitor pevonedistat. Recently reported chemical probes enable selective and time-dependent inhib…
View article: Ventromorphins: A New Class of Small Molecule Activators of the Canonical BMP Signaling Pathway
Ventromorphins: A New Class of Small Molecule Activators of the Canonical BMP Signaling Pathway Open
Here,\nwe describe three new small-molecule activators of BMP signaling\nfound by high throughput screening of a library of ∼600 000\nsmall molecules. Using a cell-based luciferase assay in the BMP4-responsive\nhuman cervical carcinoma clo…