Results 181 to 190 of about 23,499 (227)

Synthesis and pharmacokinetics of a novel macromolecular prodrug of Tacrolimus (FK506), FK506–dextran conjugate

Journal of Controlled Release, 1999
A novel macromolecular prodrug of Tacrolimus (FK506), FK506-dextran conjugate, was developed and its physico-chemical, biological and pharmacokinetic characteristics were studied. The conjugate was estimated to contain 0.45% of FK506 and the coupling molar ratio was approximately 1:1 (dextran-FK-506).
Rikio Yoshimura, Takashi Hamashima, Makiya Nishikawa   +2 more
exaly   +3 more sources

Preformulation of FK506 Prodrugs for Improving Solubility

Bulletin of the Korean Chemical Society, 2016
In order to improve water solubility of a lipophilic drug, tacrolimus (FK506), two prodrugs (FK506-G or FK506-S) such as FK506-M32-LS-G (FK506-G) and FK506-M32-LS-SL (FK506-S) were synthesized.
Young-Guk Na, Sung-Joo Hwang, Jeong-Sook Park   +2 more
exaly   +2 more sources

The mechanism of action of cyclosporin A and FK506

Immunology Today, 1992
CsA and FK506 are powerful suppressors of the immune system, most notably of T cells. They act at a point in activation that lies between receptor ligation and the transcription of early genes. Here, Stuart Schreiber and Gerald Crabtree review recent findings that indicate CsA and FK506 operate as prodrugs: they bind endogenous intracellular receptors,
S L, Schreiber, G R, Crabtree
openaire   +2 more sources

Oral Absorption of FK506 in Rats

Pharmaceutical Research, 1993
The oral absorption of FK506 in solid dispersion formulation was studied in rats. The obtained area under the concentration versus time curve (AUC) increased in a nonlinear fashion with a small dose-dependent increase in the peak blood concentrations (Cmax).
A, Kagayama, S, Tanimoto, J, Fujisaki, A, Kaibara, K, Ohara, K, Iwasaki, Y, Hirano, T, Hata   +7 more
openaire   +2 more sources

The FK506-binding protein of the malaria parasite, Plasmodium falciparum, is a FK506-sensitive chaperone with FK506-independent calcineurin-inhibitory activity

Molecular and Biochemical Parasitology, 2005
We have identified an immunophilin of the FKBP family in Plasmodium falciparum that contains a conserved peptidyl prolyl isomerase (PPIase) and tetratricopeptide repeat (TPR) domains. The 35 kDa protein was named FKBP35 and expressed in bacteria. Recombinant FKBP35 exhibited potent PPIase and protein folding activities against defined substrates in ...
Rajinder, Kumar, Brian, Adams, Alla, Musiyenko, Olena, Shulyayeva, Sailen, Barik   +4 more
openaire   +2 more sources

FK506 Treatment of Noninfectious Uveitis

American Journal of Ophthalmology, 1994
We studied the clinical effects of the immunosuppressive agent FK506 in patients with noninfectious uveitis.This study was designed as a multicenter open clinical trial in Japan. Sixteen patients with noninfectious uveitis who had visited the Uveitis Survey Clinic of the Yokohama City University Hospital were given FK506.
M, Ishioka, S, Ohno, S, Nakamura, K, Isobe, N, Watanabe, Y, Ishigatsubo, S, Tanaka   +6 more
openaire   +2 more sources

Evaluation of Synthetic FK506 Analogues as Ligands for the FK506-Binding Proteins 51 and 52

Journal of Medicinal Chemistry, 2012
The FK506-binding proteins (FKBP) 51 and 52 are cochaperones that modulate the signal transduction of steroid hormone receptors. Both proteins have been implicated in prostate cancer. Furthermore, single nucleotide polymorphisms in the gene encoding FKBP51 have been associated with a variety of psychiatric disorders.
Ranganath, Gopalakrishnan, Christian, Kozany, Steffen, Gaali, Christoph, Kress, Bastiaan, Hoogeland, Andreas, Bracher, Felix, Hausch   +6 more
openaire   +2 more sources

FK506 vs. cyclosporin

Cardiovascular Pathology, 2003
Abstract Introduction: Whether FK506 or cyclosporin is better for chronic immunosuppression in heart transplant patients has been debated. We examined endomyocardial biopsies from patients treated with these two drugs to determine if there was a difference in frequency of histologic cellular rejection episodes and Quilty lesions. The Quilty lesion (
Nupoor A. Gajjar, Jon A. Kobashigawa, Hillel Laks, Maria Espejo-Vassilakis, Michael C. Fishbein   +4 more
openaire   +1 more source

The nephrotoxicity of FK506 as compared with cyclosporine

Current Opinion in Nephrology and Hypertension, 1993
FK506, a new macrolide immunosuppressant agent, is approximately 100 times more potent than cyclosporine. Early clinical trials demonstrated FK506 to be effective in reversing refractory rejection in liver, kidney, and heart transplantation. Like cyclosporine, FK506 has significant nephrotoxicity.
openaire   +2 more sources

A Clinical Trial of FK506 in Refractory Uveitis

American Journal of Ophthalmology, 1993
We performed a clinical open trial to evaluate the efficacy and the adverse side effects of a single therapy with FK506 in refractory uveitis as a multicenter study in Japan. Fifty-three patients (41 patients with Bechçet's disease, five with Vogt-Koyanagi-Harada disease, four with idiopathic retinal vasculitis, and three with other forms of uveitis ...
Manabu Mochizuki, Kanjiro Masuda, Tsuyoshi Sakane, Koji Ito, Mitsuko Kogure, Nobuhiro Sugino, Masahiko Usui, Yutaka Mizushima, Shigeaki Ohno, Goro Inaba, Yoshitaka Miyanaga, Seiji Hayasaka, Kotaro Oizumi   +12 more
openaire   +2 more sources