| Yazarlar (8) |
Şevki Adem
Çankırı Karatekin Üniversitesi, Türkiye |
|
Abdulselam Aslan
Giresun Üniversitesi, Türkiye |
|
Ishtıaq Ahmed
Türkiye |
|
Karsten Krohn
Türkiye |
|
Çağlar Güler
Türkiye |
|
Veysal Çomaklı
Ağrı İbrahim Çeçen Üniversitesi, Türkiye |
|
Ramazan Demirdağ
Ağrı İbrahim Çeçen Üniversitesi, Türkiye |
Prof. Dr. Müslüm KUZU
Ağrı İbrahim Çeçen Üniversitesi, Türkiye |
| Özet |
| Pyruvate kinase isoenzyme M2 (PKM2) is expressed excessively in many different cancer types and it plays an important role in the control of glucose metabolism. Thus, it is evaluated as an important target in the development of medication for cancer. The flavonoids comprise a large group of natural products with variable phenolic structures and occur mainly in plants. They are of great interest due to their biological properties. In this study, the effects of various flavonoid derivatives on the PKM2 enzyme activity were analyzed in vitro. The flavonoid derivatives 1 and 2 showed inhibition effect with IC50 values of <60 μM. IC50 values of compounds 3-8 were calculated as 134, 415, 145, 163, 295 μM, and 3.5 mM, respectively. The molecules 9-12 showed an activation effect with values of AC50 of less than 90 μM. The IC50 values of the derivatives 13-17 were calculated as 115, 150, 200, 221, and 275 μM, respectively. The results show that catechin derivatives can be probably used as lead compounds for the design of PKM2 enzyme activators and inhibitors. |
| Anahtar Kelimeler |
| Cancer | Enzyme activation | Enzyme inhibition | Flavonoid derivatives | Pyruvate kinase isoenzyme M2 |
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale |
| Dergi Adı | ARCHIV DER PHARMAZIE |
| Dergi ISSN | 0365-6233 Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI |
| Makale Dili | İngilizce |
| Basım Tarihi | 02-2016 |
| Cilt No | 349 |
| Sayı | 2 |
| Sayfalar | 132 / 136 |
| Doi Numarası | 10.1002/ardp.201500357 |
| Makale Linki | http://doi.wiley.com/10.1002/ardp.201500357 |
| Atıf Sayıları | |
| WoS | 13 |
| Google Scholar | 13 |
