Találati lista | Tudóstér

001-es BibID:	BIBFORM059983
Első szerző:	Docsa Tibor (vegyész, biokémikus)
Cím:	Insulin sensitivity is modified by a glycogen phosphorylase inhibitor : glucopyranosylidene-spiro-thiohydantoin in streptozotocin-induced diabetic rats / Tibor Docsa, Balázs Marics, József Németh, Csaba Hüse, László Somsák, Pál Gergely, Barna Peitl
Dátum:	2015
ISSN:	1568-0266
Megjegyzések:	The major role of liver glycogen is to supply glucose to the circulation maintaining the normal blood glucose level. In muscle and liver the accumulation and breakdown of glycogen are regulated by the reciprocal activities of glycogen phosphorylase and glycogen synthase. Glycogen phosphorylase catalyses the key step of glycogen degradation and its activity can be inhibited by glucose and its analogues. Obviously, any readily accessible inhibitor of glycogen phosphorylase can be used as a potential therapy of non-insulin-dependent or type 2 diabetes. Hepatic glycogen phosphorylase has been identified as a new target for drugs that control blood glucose concentration. In our experiments glucopyranosylidene-spirothiohydantoin (TH) was tested on the insulin sensitivity and blood glucose level of control and streptozotocin-treated rats. The streptozotocin-treated rats failed to gain weight and exhibited stable hyperglycemia (4.7 ± 0.5 mmol/L glucose in control vs. 7.8 ± 0.5 mmol/L) and low plasma insulin levels (9.6 ± 1.9 [mű]IU/mL in control vs. 3.2 ± 2.2 [mű]IU/mL). When insulin supplementation with slow-release implants (2 IU/day) was started 8 weeks after streptozotocin injection, blood glucose concentration remained suppressed, plasma insulin level dramatically increased and the insulin sensitivity restored. TH administration significantly reduced the high blood glucose concentration and restored the insulin sensitivity of STZtreated rats.
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban Blood glucose glycogen phosphorylase inhibitor insulin implant streptozotocin Type 2 diabetes
Megjelenés:	Current Topics In Medicinal Chemistry 15 : 23 (2015), p. 2390-2394. -
További szerzők:	Marics Balázs (1986-) (okleveles táplálkozástudományi szakember, dietetikus) Németh József (1954-) (vegyész, analitikus) Hüse Csaba Somsák László (1954-) (vegyész) Gergely Pál (1947-) (biokémikus) Peitl Barna (1972-) (orvos, farmakológus)
Pályázati támogatás:	OTKA-109450 OTKA
Internet cím:	Intézményi repozitóriumban (DEA) tárolt változat
Borító:
Saját polcon:

001-es BibID:	BIBFORM006384
Első szerző:	Somsák László (vegyész)
Cím:	New inhibitors of glycogen phosphorylase as potential antidiabetic agents / L. Somsák, K. Czifrák, M. Tóth, É. Bokor, E. D. Chrysina, K.-M. Alexacou, J. M. Hayes, C. Tiraidis, E. Lazoura, D. D. Leonidas, S. E. Zographos, N. G. Oikonomakos
Dátum:	2008
ISSN:	0929-8673
Megjegyzések:	The protein glycogen phosphorylase has been linked to type 2 diabetes, indicating the importance of this target to human health. Hence, the search for potent and selective inhibitors of this enzyme, which may lead to antihyperglycaemic drugs, has received particular attention. Glycogen phosphorylase is a typical allosteric protein with five different ligand binding sites, thus offering multiple opportunities for modulation of enzyme activity. The present survey is focused on recent new molecules, potential inhibitors of the enzyme. The biological activity can be modified by these molecules through direct binding, allosteric effects or other structural changes. Progress in our understanding of the mechanism of action of these inhibitors has been made by the determination of high-resolution enzyme inhibitor structures (both muscle and liver). The knowledge of the three-dimensional structures of protein-ligand complexes allows analysis of how the ligands interact with the target and has the potential to facilitate structure-based drug design. In this review, the synthesis, structure determination and computational studies of the most recent inhibitors of glycogen phosphorylase at the different binding sites are presented and analyzed.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban glycogen phosphorylase inhibitor type 2 diabetes structure-based drug design antidiabetic agent
Megjelenés:	Current Medicinal Chemistry. - 15 : 28 (2008), p. 2933-2983. -
További szerzők:	Czifrák Katalin (1978-) (vegyész) Tóth Marietta (1974-) (vegyész) Bokor Éva (1982-) (vegyész) Chrysina, Evangelia D. Alexacou, Kyra-Melinda Hayes, Joseph M. Tiraidis, Costantinos Lazoura, E. Leonidas, Demetres D. Zographos, Spyros E. Oikonomakos, George N.
Internet cím:	elektronikus változat
Borító:
Saját polcon: