Loss of proton‐sensing GPR4 reduces tumor progression in mouse models of colon cancer
G protein‐coupled receptor 4 (GPR4) is a pH‐sensing receptor activated by acidic pH. GPR4 expression is increased in patients with inflammatory bowel disease who are at high risk of developing colorectal cancer. In mouse models, loss of GPR4 attenuated tumor progression. This correlated with increased IL2 and natural killer cell activity.
Leonie Perren+16 more
wiley +1 more source
Buchbesprechung: Analytical Techniques in Combinatorial Chemistry. Von Michael E. Swartz. [PDF]
Jörg W. Metzger
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TRPM8 levels determine tumor vulnerability to channel agonists
TRPM8 is a Ca2+ permissive channel. Regardless of the amount of its transcript, high levels of TRPM8 protein mark different tumors, including prostate, breast, colorectal, and lung carcinomas. Targeting TRPM8 with channel agonists stimulates inward calcium currents followed by emptying of cytosolic Ca2+ stores in cancer cells.
Alessandro Alaimo+18 more
wiley +1 more source
Dynamic Combinatorial Chemistry of Ditellurides. [PDF]
Fisker CD+3 more
europepmc +1 more source
Book Review: Combinatorial Chemistry - A Practical Approach. Edited by Willi Bannwarth and Eduard Felder. Volume 9 in the series Methods and Principles in Medicinal Chemistry, edited by R. Mannhold, H. Kubinyi, H. Timmermann. [PDF]
Matthias Lormann, Stefan Bräse
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The pan‐HDAC inhibitor belinostat increases the expression of the pro‐apoptotic proteins Bim, Puma, and Noxa and induces apoptosis in ovarian cancer cell lines and patient‐derived tumor organoids when used at high concentrations. Moreover, inhibiting the anti‐apoptotic proteins Bcl‐xL or Mcl‐1 sensitizes these preclinical models to the cytotoxic effect
Cécilia Thomine+10 more
wiley +1 more source
Chirality Effects in Peptide-Based Dynamic Combinatorial Chemistry. [PDF]
Gable A+3 more
europepmc +1 more source
Template-guided selection of RNA ligands using imine-based dynamic combinatorial chemistry. [PDF]
Umuhire Juru A+3 more
europepmc +1 more source
Systematic profiling of cancer‐fibroblast interactions reveals drug combinations in ovarian cancer
Fibroblasts, cells in the tumor environment, support ovarian cancer cell growth and alter morphology and drug response. We used fibroblast and cancer cell co‐culture models to test 528 drugs and discovered new drugs for combination treatment. We showed that adding Vorinostat or Birinapant to standard chemotherapy may improve drug response, suggesting ...
Greta Gudoityte+10 more
wiley +1 more source