A5042471970- Immune cells in cancer
- Immune Cell Function and Interaction
- Acute Myeloid Leukemia Research
- IL-33, ST2, and ILC Pathways
- T-cell and B-cell Immunology
- Psoriasis: Treatment and Pathogenesis
- Kruppel-like factors research
- Synthesis and Catalytic Reactions
- Metabolism, Diabetes, and Cancer
- Peptidase Inhibition and Analysis
- Cancer-related Molecular Pathways
- Cancer, Hypoxia, and Metabolism
- Epigenetics and DNA Methylation
- Ubiquitin and proteasome pathways
- Asthma and respiratory diseases
- Catalytic C–H Functionalization Methods
- Fibroblast Growth Factor Research
- Protein Degradation and Inhibitors
- Cancer Immunotherapy and Biomarkers
- Radical Photochemical Reactions
Bristol-Myers Squibb (United States)
2020-2023
This paper describes an intermolecular cross-selective [2 + 2] photocycloaddition reaction of exocyclic arylidene oxetanes, azetidines, and cyclobutanes with simple electron-deficient alkenes. The takes place under mild conditions using a commercially available Ir(III) photosensitizer upon blue light irradiation. transformation provides access to range polysubstituted 2-oxaspiro[3.3]heptane, 2-azaspiro[3.3]heptane, spiro[3.3]heptane motifs, which are prime interest in medicinal chemistry as...
Many cellular processes and pathways are mediated by the regulation of protein–protein complexes. For example, E3 ubiquitin ligases recruit substrate proteins transfer a tag to target those for destruction proteasome. It has now been shown that this process protein can be redirected small molecules in both laboratory clinical settings. This presents new paradigm drug discovery, enabling rapid removal linked disease. In Innovations review, we will describe work done on cereblon as case study...
Hepatocellular carcinoma (HCC) accounts for a majority of primary liver cancer and is one the most common forms worldwide. Aberrant signaling FGF19-FGFR4 pathway leads to HCC in mice hypothesized be driver FGF19 amplified humans. Multiple small molecule inhibitors have been pursued as targeted therapies recent years, including several selective FGFR4 that are currently being evaluated clinical trials. Herein, we report novel series highly selective, covalent...
CaMKK2 signals through AMPK-dependent and AMPK-independent pathways to trigger cellular outputs including proliferation, differentiation, migration, resulting in changes metabolism, bone mass accrual, neuronal function, hematopoiesis, immunity. CAMKK2 is upregulated tumors hepatocellular carcinoma, prostate, breast, gastric cancer, genetic deletion myeloid cells results increased antitumor immunity several syngeneic models. Validation of the biological roles has relied on or small molecule...
Abstract Calcium/calmodulin-dependent protein kinase 2 (CaMKK2) is a key regulator of energy homeostasis in several cell types. Expression this enzyme tumor cells promotes proliferation and migration, expression tumor-associated immune facilitates M2 macrophage polarization the development myeloid-derived suppressor cells. Thus, there has been interest developing CaMKK2 inhibitors as potential anticancer therapeutics. One impediment to clinical these agents that roles other cellular...
Retinoic acid receptor-related orphan nuclear receptor (ROR) γt is a member of the RORC hormone family transcription factors. RORγt functions as critical regulator thymopoiesis and immune responses. expressed in multiple cell populations including Th17 cells, where its primary function regulation responses to bacteria fungi through IL-17A production. However, excessive production has been linked numerous autoimmune diseases. Moreover, cells have shown elicit both pro- anti-tumor effects....
<p>Supplementary Figures and Tables: 5 figures, 3 tables</p>
<div>Abstract<p>Calcium/calmodulin-dependent protein kinase 2 (CaMKK2) is a key regulator of energy homeostasis in several cell types. Expression this enzyme tumor cells promotes proliferation and migration, expression tumor-associated immune facilitates M2 macrophage polarization the development myeloid-derived suppressor cells. Thus, there has been interest developing CaMKK2 inhibitors as potential anticancer therapeutics. One impediment to clinical these agents that roles...
<p>Supplementary Figures and Tables: 5 figures, 3 tables</p>
<div>Abstract<p>Calcium/calmodulin-dependent protein kinase 2 (CaMKK2) is a key regulator of energy homeostasis in several cell types. Expression this enzyme tumor cells promotes proliferation and migration, expression tumor-associated immune facilitates M2 macrophage polarization the development myeloid-derived suppressor cells. Thus, there has been interest developing CaMKK2 inhibitors as potential anticancer therapeutics. One impediment to clinical these agents that roles...
ABSTRACT Calcium/calmodulin-dependent protein kinase 2 (CaMKK2) is a key regulator of energy homeostasis in several cell types. Expression this enzyme tumor cells promotes proliferation and migration, expression tumor-associated immune facilitates M2 macrophage polarization the development myeloid-derived suppressor cells. Thus, there has been considerable interest developing CaMKK2 inhibitors as potential cancer therapeutics. However, roles other cellular compartments within environment...
Abstract Retinoic acid receptor-related orphan nuclear receptor (ROR) γt is a member of the RORC hormone family transcription factors. RORγt functions as critical regulator thymopoiesis and immune responses. expressed in multiple cell populations including Th17 cells, where its primary function regulation responses to bacteria fungi through IL-17A production. However, excessive production has been linked numerous autoimmune diseases. Moreover, cells have shown elicit both pro- anti-tumor...