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001-es BibID:	BIBFORM077837
035-os BibID:	(PMID)29792814 (WoS)000438114100006 (Scopus)85049826983
Első szerző:	Nánási Péter Pál ifj. (sejtbiológus)
Cím:	Perspectives of a myosin motor activator agent with increased selectivity / Péter Nánási Jr., István Komáromi, János Almássy
Dátum:	2018
ISSN:	0008-4212
Megjegyzések:	Clinical treatment of heart failure is still not fully solved. A novel class of agents, the myosin motor activators, acts directly on cardiac myosin resulting in an increased force generation and prolongation of contraction. Omecamtiv mecarbil, the lead molecule of this group, is now in human 3 phase displaying promising clinical performance. However, omecamtiv mecarbil is not selective to myosin, since it readily binds to and activates cardiac ryanodine receptors (RyR-2), an effect that may cause complications is case of overdose. In this study, in silico analysis was performed to investigate the docking of omecamtiv mecarbil and other structural analogues to cardiac myosin heavy chain and RyR-2 in order to select the structure which has a higher selectivity to myosin over RyR-2. In silico docking studies revealed that omecamtiv mecarbil has comparable affinity to myosin and RyR-2: the respective K values are 0.60 and 0.87 ?M. Another compound CK-1032100 has much lower affinity to RyR-2 than omecamtiv mecarbil, while it still has a moderate affinity to myosin. It was concluded that further research starting from the chemical structure of CK-1032100 may result a better myosin activator burdened probably less by the RyR-2 binding side effect. It also is possible, however, that the selectivity of omecamtiv mecarbil to myosin over RyR-2 cannot be substantially improved, because similar moieties seem to be responsible for the high affinity to both myosin and RyR-2.
Tárgyszavak:	Orvostudományok Elméleti orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk Inotropic agents Myosin activators Omecamtiv mecarbil Ryanodine receptor Cytosolic Ca 2+
Megjelenés:	Canadian Journal of Physiology and Pharmacology. - 96 : 7 (2018), p. 676-680. -
További szerzők:	Komáromi István (1957-) (vegyész, molekuláris biológus, biokémikus) Almássy János (1981-) (élettanász, biológus, angol-magyar szakfordító)
Pályázati támogatás:	NKFIH PD112199 Egyéb
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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001-es BibID:	BIBFORM091603
Első szerző:	Ząbczyk, Michał
Cím:	Plasma fibrin clots of pulmonary embolism patients present increased amounts of factor XIII and alpha2-antiplasmin at 3 months' anticoagulation since the acute phase / M. Zabczyk, J. Natorska, Z. Bagoly, F. Sarkady, B. Barath, E. Katona, A. H. Bryk, K. Zettl, J. R. Wisniewski, A. Undas
Dátum:	2020
ISSN:	0867-5910
Megjegyzések:	Fibrin cross-linking by coagulation factor (F)XIII leads to clot stabilization. Reduced plasma FXIII levels have been reported in acute pulmonary embolism (PE) patients. We investigated the impact of anticoagulant therapy on clot-bound amounts of FXIII and ?2-antiplasmin and their associations with fibrin clot properties in patients with PE. Clots generated from plasma of 18 acute symptomatic patients on admission and after a 3-month treatment with rivaroxaban were assessed off anticoagulation using mass spectrometry. Plasma FXIII and ?2-antiplasmin activity were determined at the 2 time points along with thrombin generation markers, plasma fibrin clot permeability (Ks), and clot lysis time (CLT). Following anticoagulant therapy, clot-bound FXIII increased from 2.97 (interquartile range, 1.98 ? 4.08) to 4.66 (3.5 ? 6.9) mg/g protein and ?2-antiplasmin from 9.4 (7.2 ? 10.6) to 11 (9.5 ? 14) mg/g protein (both p < 0.0001). The two parameters showed positive correlation at baseline only (r = 0.63, p = 0.0056). Similarly to clot-bound amounts, plasma FXIII (+25.8%) and ?2-antiplasmin activity (+12%) increased at 3 months. Plasma FXIII activity on admission, but not after 3 months since the index PE, was associated with amounts of clot-bound FXIII (r = 0.35, p = 0.043) and ?2-antiplasmin (r = 0.47, p = 0.048). At baseline, clot-bound FXIII correlated with plasma F1+2 prothrombin fragments levels (r = 0.51, p = 0.03), while clot-bound ?2-antiplasmin correlated with CLT (r = 0.43, p = 0.036). At 3 months associations of clot-bound FXIII and ?2-antiplasmin were abolished. This study assessed for the first time changes in the fibrin clot composition following acute PE, suggesting an increase of clot-bound and plasma FXIII and ?2-antiplasmin levels after 3 months.
Tárgyszavak:	Orvostudományok Klinikai orvostudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk
Megjelenés:	Journal of Physiology and Pharmacology. - 71 : 4 (2020), p. 519-524. -
További szerzők:	Natorska, Joanna Bagoly Zsuzsa (1978-) (orvos) Sarkady Ferenc (1982-) (laboratóriumi analitikus) Baráth Barbara (1991-) (orvosírnok) Katona Éva (1961-) (klinikai biokémikus) Bryk, Agata Hanna Zettl, K. Wisniewski, J. R. Undas Anetta
Pályázati támogatás:	GINOP-2.3.2-15-2016-00043 GINOP
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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