| Title |
An Enzyme‐Directed Imidazoquinoline for Cancer Immunotherapy
|
|---|---|
| Published in |
ChemMedChem, October 2016
|
| DOI | 10.1002/cmdc.201600443 |
| Pubmed ID | |
| Authors | |
| Abstract |
Herein we report the synthesis and activity of an enzyme-directed immunostimulant with immune cell activation mediated by β-galactosidase, either exogenously added, or on B16 melanoma cells. Covalent attachment of a β-galactopyranoside to an imidazoquinoline immunostimulant at a position critical for activity resulted in a pro-immunostimulant that could be selectively converted by β-galactosidase into an active immunostimulant. The pro-immunostimulant exhibited β-galactosidase-directed immune cell activation as measured by NF-κB transcription in RAW-Blue macrophages or cytokine production (TNF, IL-6, IL-12) in JAWSII monocytes. Conversion of the pro-immunostimulant into an active immunostimulant was also found to occur using β-galactosidase-enriched B16 melanoma cells. In co-culture experiments with either immune cell line, β-galactosidase-enriched B16 cells effected activation of bystander immune cells. |
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X Demographics
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Germany | 1 | 50% |
| United States | 1 | 50% |
Demographic breakdown
| Type | Count | As % |
|---|---|---|
| Scientists | 2 | 100% |
Mendeley demographics
Geographical breakdown
| Country | Count | As % |
|---|---|---|
| Unknown | 31 | 100% |
Demographic breakdown
| Readers by professional status | Count | As % |
|---|---|---|
| Student > Doctoral Student | 5 | 16% |
| Student > Ph. D. Student | 4 | 13% |
| Researcher | 3 | 10% |
| Professor > Associate Professor | 3 | 10% |
| Lecturer | 2 | 6% |
| Other | 6 | 19% |
| Unknown | 8 | 26% |
| Readers by discipline | Count | As % |
|---|---|---|
| Chemistry | 13 | 42% |
| Chemical Engineering | 2 | 6% |
| Biochemistry, Genetics and Molecular Biology | 2 | 6% |
| Pharmacology, Toxicology and Pharmaceutical Science | 1 | 3% |
| Agricultural and Biological Sciences | 1 | 3% |
| Other | 2 | 6% |
| Unknown | 10 | 32% |