Michael E. Jung
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View article: Discovery of an ApoE4-targeted small-molecule SirT1 enhancer for the treatment of Alzheimer’s disease
Discovery of an ApoE4-targeted small-molecule SirT1 enhancer for the treatment of Alzheimer’s disease Open
Decreased expression of sirtuin 1 (SirT1) has been implicated in Alzheimer’s disease (AD), and as we previously reported, is related to transcriptional repression by the major risk factor for sporadic AD, apolipoprotein E4 (ApoE4). Herein …
View article: Design and Biological Activity of a Novel Brain Penetrant Urea Compound Against Glioblastoma
Design and Biological Activity of a Novel Brain Penetrant Urea Compound Against Glioblastoma Open
Glioblastoma (GBM) remains the most lethal primary brain tumor, largely due to therapy-resistant glioma stem cells (GSCs) and the ability of non-stem cells to dedifferentiate under therapeutic pressure. We developed MXC-017, a novel urea-b…
View article: Large-scale discovery, analysis, and design of protein energy landscapes
Large-scale discovery, analysis, and design of protein energy landscapes Open
All folded proteins continuously fluctuate between their low-energy native structures and higher energy conformations that can be partially or fully unfolded. These rare states influence protein function, interactions, aggregation, and imm…
View article: Aster-dependent nonvesicular transport facilitates dietary cholesterol uptake
Aster-dependent nonvesicular transport facilitates dietary cholesterol uptake Open
Intestinal absorption is an important contributor to systemic cholesterol homeostasis. Niemann-Pick C1 Like 1 (NPC1L1) assists in the initial step of dietary cholesterol uptake, but how cholesterol moves downstream of NPC1L1 is unknown. We…
View article: EP021 Multi-center implementation of objective pain procedure assessment tools: Pain Procedure Rating System (PaPRS)
EP021 Multi-center implementation of objective pain procedure assessment tools: Pain Procedure Rating System (PaPRS) Open
Background and Aims Pain fellow performance evaluations have historically emphasized categories such as medical knowledge, communication skills, and professionalism. Objective evaluation of procedural skills, while extremely important, has…
View article: Development of a novel histone deacetylase inhibitor unveils the role of HDAC11 in alleviating depression by inhibition of microglial activation
Development of a novel histone deacetylase inhibitor unveils the role of HDAC11 in alleviating depression by inhibition of microglial activation Open
Histone deacetylases (HDACs) are key epigenetic regulators and classified into four subtypes. Despite the various roles of each HDAC isoform, the lack of selective HDAC inhibitors has limited the elucidation of their roles in biological sy…
View article: Aster-dependent non-vesicular transport facilitates dietary cholesterol uptake
Aster-dependent non-vesicular transport facilitates dietary cholesterol uptake Open
Intestinal cholesterol absorption is an important contributor to systemic cholesterol homeostasis. Niemann-Pick C1 Like 1 (NPC1L1), the target of the drug ezetimibe (EZ), assists in the initial step of dietary cholesterol uptake. However, …
View article: Data from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
Data from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Prior work indicates DEPTOR expression in multiple myeloma cells could be a therapeutic target. DEPTOR binds to mTOR via its PDZ domain and inhibits mTOR kinase activity. We previously identified a drug, which prevented mTOR–DEPTOR binding…
View article: Data from Golgi Acidification by NHE7 Regulates Cytosolic pH Homeostasis in Pancreatic Cancer Cells
Data from Golgi Acidification by NHE7 Regulates Cytosolic pH Homeostasis in Pancreatic Cancer Cells Open
abstractCancer cells reprogram their metabolism to meet elevated energy demands and favor glycolysis for energy production. This boost in glycolytic flux supports proliferation, but also generates acid in the form of hydrogen ions that mus…
View article: figure S7 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
figure S7 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Suppl fig 7: A: Examples of IHC staining of normal tissues for DEPTOR expression following daily injection of DMSO or drug 3g (10mg/kg x 21 days); B) Immunoblot analysis of heart tissue for DEPTOR expression
View article: Supplementary Figure 5 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i>
Supplementary Figure 5 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i> Open
PDF file - 322K, Figure S5. Levels of Rad51 transcript were higher in estrogen supplemented PTEN-null endometrial epithelia.
View article: Figure S2 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
Figure S2 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Suppl fig 2:A) Co-IP between DEPTOR & mTOR in 8226 treated with NSC126405 or 3g; B,C&D) Immunoblot of 8226 cells after 6 hrs incubation with drugs. Relative ex- pression below gels are means of 3 separate experiments; E) Bead pull-down ass…
View article: Figure S1 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
Figure S1 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Supplemental figure 1: A) Hematopoietic colony formation in marrow cells exposed to drug 3g for 14 days (assay as described in (3); Data represent % of control (0uM), mean+/-SD; B)8226 MM cells, PC3 prostate cancer cells, LLC Lewis lung ca…
View article: Supplementary Figure 4 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i>
Supplementary Figure 4 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i> Open
PDF file - 139K, Figure S4. Three-dimensional in vitro model for growth and treatment of PTEN-null epithelia co-cultured with WT endometrial stroma.
View article: figure S4 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
figure S4 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Suppl fig 4: A) Mice were challenged with 8226 cells (admixed with Matrigel) SC and, when tumor size was 300mm3, mice were randomized to receive drug 3g at 5 mg/kg IP daily (X) for 9 days or DMSO (o); Results shown are mean +/- SD tumor vo…
View article: figure S3 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
figure S3 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Supplemental figure 3: Mice were challenged SQ with 8226 MM cells and, when tumors were 500mm3 mice were treated with DMSO(control) or drug 3g at 20mg/kg by daily IP injection (4 mice/group). Data are tumor volume at days 2, 3 or 4 after s…
View article: Figure S1 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
Figure S1 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Supplemental figure 1: A) Hematopoietic colony formation in marrow cells exposed to drug 3g for 14 days (assay as described in (3); Data represent % of control (0uM), mean+/-SD; B)8226 MM cells, PC3 prostate cancer cells, LLC Lewis lung ca…
View article: figure S5 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
figure S5 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Suppl fig 5: A) Mice (4/group) bearing SQ 8226 xenografts were in- Jected IP with DMSO (control (C)) or drug 3g at 20 mg/kg and tumors were excised 24, 48 or 72 hrs later. Tumors were stained for DEPTOR expression. Data are number of DEPTO…
View article: figure S7 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
figure S7 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Suppl fig 7: A: Examples of IHC staining of normal tissues for DEPTOR expression following daily injection of DMSO or drug 3g (10mg/kg x 21 days); B) Immunoblot analysis of heart tissue for DEPTOR expression
View article: Data from Macropinocytosis in Cancer-Associated Fibroblasts Is Dependent on CaMKK2/ARHGEF2 Signaling and Functions to Support Tumor and Stromal Cell Fitness
Data from Macropinocytosis in Cancer-Associated Fibroblasts Is Dependent on CaMKK2/ARHGEF2 Signaling and Functions to Support Tumor and Stromal Cell Fitness Open
Although pancreatic ductal adenocarcinoma (PDAC) cells are exposed to a nutrient-depleted tumor microenvironment, they can acquire nutrients via macropinocytosis, an endocytic form of protein scavenging that functions to support cancer met…
View article: Data from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
Data from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Prior work indicates DEPTOR expression in multiple myeloma cells could be a therapeutic target. DEPTOR binds to mTOR via its PDZ domain and inhibits mTOR kinase activity. We previously identified a drug, which prevented mTOR–DEPTOR binding…
View article: Supplementary Figure 3 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i>
Supplementary Figure 3 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i> Open
PDF file - 80K, Figure S3. Decreased levels of Cyp3A4 were detected in estrogen depleted mice.
View article: figure S5 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
figure S5 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Suppl fig 5: A) Mice (4/group) bearing SQ 8226 xenografts were in- Jected IP with DMSO (control (C)) or drug 3g at 20 mg/kg and tumors were excised 24, 48 or 72 hrs later. Tumors were stained for DEPTOR expression. Data are number of DEPTO…
View article: Supplementary Figure 2 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i>
Supplementary Figure 2 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i> Open
PDF file - 409K, Figure S2. The histology of Olaparib treated estrogen deprived PTEN-null tumors was similar to vehicle treated counterparts and resembled human endometrioid endometrial carcinoma.
View article: Supplementary Figure 5 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i>
Supplementary Figure 5 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i> Open
PDF file - 322K, Figure S5. Levels of Rad51 transcript were higher in estrogen supplemented PTEN-null endometrial epithelia.
View article: figure S3 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
figure S3 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Supplemental figure 3: Mice were challenged SQ with 8226 MM cells and, when tumors were 500mm3 mice were treated with DMSO(control) or drug 3g at 20mg/kg by daily IP injection (4 mice/group). Data are tumor volume at days 2, 3 or 4 after s…
View article: figure S8 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
figure S8 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Supplemental figure 8: Representative sections of liver obtained from control (DMSO) mice or mice injected IP daily with drug 3g at 20mg/kg. Magnification=100x
View article: Supplementary Figure 2 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i>
Supplementary Figure 2 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i> Open
PDF file - 409K, Figure S2. The histology of Olaparib treated estrogen deprived PTEN-null tumors was similar to vehicle treated counterparts and resembled human endometrioid endometrial carcinoma.
View article: Supplementary Figure 1 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i>
Supplementary Figure 1 from Low Levels of Circulating Estrogen Sensitize PTEN-Null Endometrial Tumors to PARP Inhibition <i>In Vivo</i> Open
PDF file - 422K, Figure S1. Despite Olaparib therapy, PTEN-null endometrial tumors persisted and resembled human endometrial endometrioid cancers.
View article: figure S4 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity
figure S4 from A Novel Therapeutic Induces DEPTOR Degradation in Multiple Myeloma Cells with Resulting Tumor Cytotoxicity Open
Suppl fig 4: A) Mice were challenged with 8226 cells (admixed with Matrigel) SC and, when tumor size was 300mm3, mice were randomized to receive drug 3g at 5 mg/kg IP daily (X) for 9 days or DMSO (o); Results shown are mean +/- SD tumor vo…