التفاصيل البيبلوغرافية
| العنوان: |
Design and synthesis of potent and orally active GPR4 antagonists with modulatory effects on nociception, inflammation, and angiogenesis. |
| المؤلفون: |
Miltz, Wolfgang1 wolfgang.miltz@novartis.com, Velcicky, Juraj1, Dawson, Janet2, Littlewood-Evans, Amanda2, Ludwig, Marie-Gabrielle3, Seuwen, Klaus3, Feifel, Roland4, Oberhauser, Berndt1, Meyer, Arndt1, Gabriel, Daniela3, Nash, Mark5, Loetscher, Pius2 |
| المصدر: |
Bioorganic & Medicinal Chemistry. Aug2017, Vol. 25 Issue 16, p4512-4525. 14p. |
| مصطلحات موضوعية: |
*G protein coupled receptors, *CELL receptors, *MEMBRANE proteins, *ACIDOSIS, *NEOVASCULARIZATION |
| مستخلص: |
GPR4, a G-protein coupled receptor, functions as a proton sensor being activated by extracellular acidic pH and has been implicated in playing a key role in acidosis associated with a variety of inflammatory conditions. An orally active GPR4 antagonist 39c was developed, starting from a high throughput screening hit 1 . The compound shows potent cellular activity and is efficacious in animal models of angiogenesis, inflammation and pain. [ABSTRACT FROM AUTHOR] |
| قاعدة البيانات: |
Academic Search Index |
