Development of potent isoflavone-based formyl peptide receptor 1 (FPR1) antagonists and their effects in gastric cancer cell models; European Journal of Medicinal Chemistry; Vol. 261
| Parent link: | European Journal of Medicinal Chemistry.— .— Amsterdam: Elsevier Science Publishing Company Inc. Vol. 261.— 2023.— Article number 115854, 18 p. |
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| مؤلفون آخرون: | , , , , , , , , , , , |
| الملخص: | Title screen Formyl peptide receptor-1 (FPR1) is a G protein-coupled chemoattractant receptor that plays a crucial role in the trafficking of leukocytes into the sites of bacterial infection and inflammation. Recently, FPR1 was shown to be expressed in different types of tumor cells and could play a significant role in tumor growth and invasiveness. Starting from the previously reported FPR1 antagonist 4, we have designed a new series of 4H-chromen-2-one derivatives that exhibited a substantial increase in FPR1 antagonist potency. Docking studies identified the key interactions for antagonist activity. The most potent compounds in this series (24a and 25b) were selected to study the effects of the pharmacological blockade of FPR1 in NCl–N87 and AGS gastric cancer cells. Both compounds potently inhibited cell growth through a combined effect on cell proliferation and apoptosis and reduced cell migration, while inducing an increase in angiogenesis, thus suggesting that FPR1 could play a dual role as oncogene and onco-suppressor Текстовый файл AM_Agreement |
| اللغة: | الإنجليزية |
| منشور في: |
2023
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| الموضوعات: | |
| الوصول للمادة أونلاين: | https://doi.org/10.1016/j.ejmech.2023.115854 |
| التنسيق: | الكتروني فصل الكتاب |
| KOHA link: | https://koha.lib.tpu.ru/cgi-bin/koha/opac-detail.pl?biblionumber=680406 |
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| 200 | 1 | |a Development of potent isoflavone-based formyl peptide receptor 1 (FPR1) antagonists and their effects in gastric cancer cell models |f Fabio Francavilla, Federica Sarcina, Igor A. Schepetkin [et al.] | |
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| 300 | |a Title screen | ||
| 320 | |a References: 39 tit | ||
| 330 | |a Formyl peptide receptor-1 (FPR1) is a G protein-coupled chemoattractant receptor that plays a crucial role in the trafficking of leukocytes into the sites of bacterial infection and inflammation. Recently, FPR1 was shown to be expressed in different types of tumor cells and could play a significant role in tumor growth and invasiveness. Starting from the previously reported FPR1 antagonist 4, we have designed a new series of 4H-chromen-2-one derivatives that exhibited a substantial increase in FPR1 antagonist potency. Docking studies identified the key interactions for antagonist activity. The most potent compounds in this series (24a and 25b) were selected to study the effects of the pharmacological blockade of FPR1 in NCl–N87 and AGS gastric cancer cells. Both compounds potently inhibited cell growth through a combined effect on cell proliferation and apoptosis and reduced cell migration, while inducing an increase in angiogenesis, thus suggesting that FPR1 could play a dual role as oncogene and onco-suppressor | ||
| 336 | |a Текстовый файл | ||
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| 461 | 1 | |t European Journal of Medicinal Chemistry |c Amsterdam |n Elsevier Science Publishing Company Inc. | |
| 463 | 1 | |t Vol. 261 |v Article number 115854, 18 p. |d 2023 | |
| 610 | 1 | |a FPR1 | |
| 610 | 1 | |a Gastric cancer | |
| 610 | 1 | |a 4H-chromen-2-one derivatives | |
| 610 | 1 | |a Docking studies | |
| 610 | 1 | |a Cell growth | |
| 610 | 1 | |a электронный ресурс | |
| 610 | 1 | |a труды учёных ТПУ | |
| 701 | 1 | |a Francavilla |b F. |g Fabio | |
| 701 | 1 | |a Sarcina |b F. |g Federica | |
| 701 | 1 | |a Schepetkin (Shchepyotkin) |b I. A. |c doctor-biophysicist |c leading researcher of Tomsk Polytechnic University, candidate of medical science |f 1962- |g Igor Aleksandrovich |9 20276 | |
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