Results 141 to 150 of about 11,965 (161)

Sirolimus and tacrolimus binding proteins: double-edged swords for GVHD prophylaxis

Blood, 2003
Postgrafting immunosuppression is the main approach for the prevention of graft-versus-host disease (GVHD) after allogeneic blood or marrow transplantation. Controlled trials have found that the combination of cyclosporine, a calcineurin inhibitor that reduces T-cell cytokine gene activation ...
Hans-Peter Kiem, Kiem Hans-Peter, Anasetti Claudio   +2 more
exaly   +2 more sources

Plasma Protein Binding of Tacrolimus in Humans

Journal of Pharmaceutical Sciences, 1993
An ultracentrifugation method was used for the determination of the tacrolimus (FK 506) free fraction in plasma. Samples of 400 microL were centrifuged for 6 h at 160,000 x g, and concentrations of [3H]tacrolimus were measured in the original plasma and in the second layer of the supernatant.
William J Jusko, Wojciech Piekoszewski
exaly   +3 more sources

Probing hydration contributions to the thermodynamics of ligand binding by proteins. Enthalpy and heat capacity changes of tacrolimus and rapamycin binding to FK506 binding protein in deuterium oxide and water

Biochemistry, 1993
Patrick R Connelly
exaly   +2 more sources

Tacrolimus-binding protein FKBP8 directs myosin light chain kinase-dependent barrier regulation and is a potential therapeutic target in Crohn’s disease

Gut, 2022
Objective Intestinal barrier loss is a Crohn’s disease (CD) risk factor. This may be related to increased expression and enzymatic activation of myosin light chain kinase 1 (MLCK1), which increases intestinal paracellular permeability and correlates with CD severity. Moreover, preclinical studies have shown that
Li Zuo, Wei-Ting Kuo, Feng Cao, Sandra D Chanez-Paredes, Daniel Zeve, Prabhath Mannam, Léa Jean-François, Anne Day, W Vallen Graham, Yan Y Sweat, Nitesh Shashikanth, David T Breault, Jerrold R Turner   +12 more
openaire   +2 more sources

Changes in Tacrolimus Distribution in Blood and Plasma Protein Binding Following Liver Transplantation

Therapeutic Drug Monitoring, 2004
Therapeutic drug monitoring of tacrolimus is complicated by the conflicting evidence of a relationship between trough blood tacrolimus concentration and clinical outcome. This prospective study investigated the blood distribution and protein binding of tacrolimus in liver transplant recipients over the first 60 days after transplantation with a view to
Hamim, Zahir, Geoffrey, McCaughan, Margaret, Gleeson, Romina A, Nand, Andrew J, McLachlan   +4 more
openaire   +2 more sources

Comparative X-ray structures of the major binding protein for the immunosuppressant FK506 (tacrolimus) in unliganded form and in complex with FK506 and rapamycin

Acta Crystallographica Section D Biological Crystallography, 1995
FK506 (tacrolimus) is a natural product now approved in the US and Japan for organ transplantation. FK506, in complex with its 12 kDa cytosolic receptor (FKBP12), is a potent agonist of immunosuppression through the inhibition of the phosphatase activity of calcineurin.
K P, Wilson, M M, Yamashita, M D, Sintchak, S H, Rotstein, M A, Murcko, J, Boger, J A, Thomson, M J, Fitzgibbon, J R, Black, M A, Navia   +9 more
openaire   +2 more sources

Hippocampal CA1 neuron survival and cytosolic FKBP12, the 12 kDa FK506-binding protein, after ischemia and tacrolimus treatment in gerbils

Neuroscience Letters, 2003
To assess the neuroprotective effect of tacrolimus (FK506) in transient forebrain ischemia models in gerbils, 10.0 mg/kg of FK506 was injected intraperitoneally immediately following reperfusion and at intervals of 1, 3, 6, 9, and 12 h after reperfusion.
Noriyuki, Fumoto, Hiroki, Nakatsuka, Shinsuke, Ohta, Yoshiaki, Kumon, Takanori, Ohnishi   +4 more
openaire   +2 more sources

Probing hydration contributions to the thermodynamics of ligand binding by proteins. Enthalpy and heat capacity changes of tacrolimus and rapamycin binding to FK506 binding protein in D2O and H2O.

Biochemistry, 1993
The stabilities of native proteins and protein-ligand complexes result from differential interactions among numerous polar and nonpolar atoms within the proteins and ligands and of these atoms with water. Delineation of the various energetic contributions of the stabilities of proteins or protein-ligand complexes in aqueous solution, and an evaluation ...
P R, Connelly, J A, Thomson, M J, Fitzgibbon, F J, Bruzzese   +3 more
openaire   +1 more source

Binding of tacrolimus (FK506) with human plasma proteins re-evaluation and effect of mycophenolic acid.

Research communications in molecular pathology and pharmacology, 1997
Protein binding of tacrolimus (FK506) in human plasma was re-evaluated by equilibration dialysis and compared with that of FK506 previously reported by two different methods (about 99 and 77% by an ultrafiltration and ultracentrifugation method, respectively). The binding determined in this study was about 99% irrespective of FK506 concentrations added
K, Iwasaki, Y, Miyazaki, Y, Teramura, A, Kawamura, Z, Tozuka, T, Hata, N, Undre   +6 more
openaire   +1 more source

CHANGES OF THE PROTEIN BINDING OF TACROLIMUS AND THE PLASMA ALPHA-1-ACID GLYCOPROTEIN CONCENTRATION IN LIVER TRANSPLANT RECIPIENTS

Transplantation Journal, 2010
S. Kishino, N. Mochizuki, K. Ohno, T. Shimamura, H. Furukawa, S. Todo   +5 more
openaire   +1 more source