Structure-activity profiles of macrolactam immunosuppressant FK-506 analogues.

Abstract:

:The immunosuppressive agent FK-506 has received much attention due to its efficacy and potency in the areas of transplant rejection and autoimmune disease. Calcineurin, a Ca(2+)-calmodulin activated phosphatase, was recently implicated in the immunosuppressive mechanism of FK-506. In our ongoing search for superior immunosuppressive agents, we have synthesized several analogues of FK-506 and tested their mechanistic and immunosuppressive actions. It was found that C-18 hydroxyl analogues of ascomycin, an analogue of FK-506 also called FR900520, bound tightly to immunophilin FKBP-12, but do not show any immunosuppressive activity in vitro or in vivo despite good bioavailability. Further, they reverse the inhibition of calcineurin caused by FK-506/FKBP-12 complex.

journal_name

FEBS Lett

journal_title

FEBS letters

authors

Kawai M,Lane BC,Hsieh GC,Mollison KW,Carter GW,Luly JR

doi

10.1016/0014-5793(93)81196-7

subject

Has Abstract

pub_date

1993-01-25 00:00:00

pages

107-13

issue

2

eissn

0014-5793

issn

1873-3468

pii

0014-5793(93)81196-7

journal_volume

316

pub_type

杂志文章
  • The hepatitis B viral X protein activates NF-kappaB signaling pathway through the up-regulation of TBK1.

    abstract::The hepatitis B viral X protein (HBx) is a multifunctional protein that plays a role in the activation of the NF-kappaB signaling pathway. In this study, we demonstrate that HBx up-regulates expression of TANK-binding kinase-1 (TBK1) at the transcriptional level. Increased levels of TBK1 protein then induce the phosph...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2009.11.091

    authors: Kim HR,Lee SH,Jung G

    更新日期:2010-02-05 00:00:00

  • Phosphorylation of smooth muscle myosin light chain by five different kinases.

    abstract::Phosphorylation of the 20 kDa myosin light chain from smooth muscle by five different kinases was investigated. Three of the kinases (myosin light chain kinase, phosphorylase kinase, and cAMP-dependent protein kinase) phosphorylate serine residues, the fourth (casein-kinase-2) mainly threonine, and the fifth (glycogen...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(83)80449-9

    authors: Singh TJ,Akatsuka A,Huang KP

    更新日期:1983-08-08 00:00:00

  • Silencing of filamin A gene expression inhibits Ca2+ -sensing receptor signaling.

    abstract::Filamin plays an important role in actin cytoskeleton organization, membrane stabilization, and anchoring of transmembrane proteins. Using short interfering RNA (siRNA) to selectively target the filamin A gene and silence its expression, we studied the role of filamin A in G protein coupled receptor (GPCR) signaling. ...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2006.02.035

    authors: Huang C,Wu Z,Hujer KM,Miller RT

    更新日期:2006-03-20 00:00:00

  • Incorporation of synthetic 1,2-diacylglycerol into platelet phosphatidylinositol is increased by cyclic AMP.

    abstract::1,2-Didecanoylglycerol (diC10) is taken up by human platelets and sequentially converted to 1,2-didecanoylphosphatidic acid (PA10) and 1,2-didecanoylphosphatidylinositol (PI10). Agents that increase cyclic AMP in platelets, such as prostacyclin and forskolin, sequentially convert diC10 to PA10 and PI10. They decrease ...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(86)80141-7

    authors: Lapetina EG

    更新日期:1986-01-20 00:00:00

  • Endogenously generated 5-hydroperoxyeicosatetraenoic acid is the preferred substrate for human leukocyte leukotriene A4 synthase activity.

    abstract::A single protein from human leukocytes possesses both 5-lipoxygenase and leukotriene A4 (LTA4) synthase activities. It has been reported that LTA4 production is more efficient when the enzyme utilizes arachidonic acid, than when 5-HPETE is exogenously supplied as substrate. In the present study, human leukocyte homoge...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(87)80675-0

    authors: Puustinen T,Scheffer MM,Samuelsson B

    更新日期:1987-06-15 00:00:00

  • Thrombin-induced inhibition of myoblast differentiation is mediated by Gbetagamma.

    abstract::Thrombin has been shown to inhibit skeletal muscle differentiation. However, the mechanisms by which thrombin represses myogenesis remain unknown. Since the thrombin receptor couples to G(i), G(q/11) and G(12), we examined which subunits of heterotrimeric guanine nucleotide-binding regulatory proteins (Galpha(i), Galp...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/s0014-5793(00)01458-7

    authors: Nagao M,Kaziro Y,Itoh H

    更新日期:2000-04-28 00:00:00

  • Biochemical engineering of the N-acyl side chain of sialic acids alters the kinetics of a glycosylated potassium channel Kv3.1.

    abstract::The sialic acid of complex N-glycans can be biochemically engineered by substituting the physiological precursor N-acetylmannosamine with non-natural N-acylmannosamines. The Kv3.1 glycoprotein, a neuronal voltage-gated potassium channel, contains sialic acid. Western blots of the Kv3.1 glycoprotein isolated from trans...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2011.09.021

    authors: Hall MK,Reutter W,Lindhorst T,Schwalbe RA

    更新日期:2011-10-20 00:00:00

  • Degradation of type IX collagen by matrix metalloproteinase 3 (stromelysin) from human rheumatoid synovial cells.

    abstract::The degradation of type IX collagen, a minor collagen in cartilage, was examined by treatment with three different types of matrix metalloproteinases (MMPs) purified from the culture medium of rheumatoid synovial cells. Neither MMP-1 (collagenase) nor MMP-2 (so-called 'gelatinase') could digest type IX collagen, but M...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(89)80586-1

    authors: Okada Y,Konomi H,Yada T,Kimata K,Nagase H

    更新日期:1989-02-27 00:00:00

  • Arsenate-mediated G2 cell cycle arrest in U-2OS cells involves phosphorylation of human polycomb protein 2 by p38 MAPK.

    abstract::G2/M checkpoints ensure the proper timing of cell mitosis. We previously reported that p38 mitogen-activated protein kinase (MAPK) activation is essential for stress-induced G2 arrest in the U-2OS osteosarcoma cell line, but the molecular mechanism was obscure. Here, using the T7 phage display system, we find p38 dire...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1002/1873-3468.13272

    authors: Wu W,Zhou H,He F,Xiao Z,Jiang Y,Zhao M

    更新日期:2018-12-01 00:00:00

  • Malignant transformation-linked imbalance: decreased xanthine oxidase activity in hepatomas.

    abstract::Xanthine oxidase was decreased 2- to 10-fold in all examined rat hepatomas irrespective of the malignancy; growth rate and degrees of histological differentiation of the neoplasms. The affinity to substrate (KM=6-8 muM) and the pH optimum (8.0) of the liver and hepatoma enzymes were the same. The reprogramming of gene...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(75)80385-1

    authors: Prajda N,Weber G

    更新日期:1975-11-15 00:00:00

  • Molecular cloning of the canine angiotensin II receptor. An AT1-like receptor with reduced affinity for DuP753.

    abstract::Canine aortic strip studies revealed insensitivity of angiotensin II (AII)-induced aortic contraction to inhibition by the non-peptide antagonist DuP753 (pKB = 6.7 +/- 0.1). In order to determine the origin of this phenomenon we cloned the canine homologue of the AT1 AII receptor. Expression of this cDNA in COS-7 cell...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(94)80307-2

    authors: Burns L,Clark KL,Bradley J,Robertson MJ,Clark AJ

    更新日期:1994-04-25 00:00:00

  • Inhibition of the replication of native and 3'-azido-2',3'-dideoxythymidine (AZT)-resistant simian immunodeficiency virus (SIV) by 3-nitrosobenzamide.

    abstract::The 3-nitrosobenzamide (NOBA) drug abolishes SIV replication sharply at 20 microM concentration when CEM x 174 cells are preincubated for 1 h with the drug prior to viral infection. Treatment of CEM x 174 cells with 20 microM NOBA resulted in the inhibition of the synthesis of the DNA sequence coding for the gag gene,...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(93)81778-x

    authors: Chuang AJ,Killam KF Jr,Chuang RY,Rice WG,Schaeffer CA,Mendeleyev J,Kun E

    更新日期:1993-07-12 00:00:00

  • Mutations in the glucose-6-phosphate transporter (G6PT) gene in patients with glycogen storage diseases type 1b and 1c.

    abstract::Glycogen storage diseases type 1 (GSD 1) are a group of autosomal recessive disorders characterized by impairment of terminal steps of glycogenolysis and gluconeogenesis. Mutations of the glucose-6-phosphatase gene are responsible for the most frequent form of GSD 1, the subtype 1a, while mutations of the glucose-6-ph...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/s0014-5793(99)01248-x

    authors: Galli L,Orrico A,Marcolongo P,Fulceri R,Burchell A,Melis D,Parini R,Gatti R,Lam C,Benedetti A,Sorrentino V

    更新日期:1999-10-08 00:00:00

  • Regulation of LacZ mRNA translatability in a cell-free system at heat shock by the last four sense codons.

    abstract::Under heat shock conditions translation of Xenopus laevis normal mRNAs in a rabbit reticulocyte cell-free system is blocked whereas hsp70 mRNA is translated. mRNA for E. coli beta-galactosidase containing the last four sense codons of Drosophila hsp70 at its 3'-end was constructed. This mRNA is efficiently translated ...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(89)81346-8

    authors: Denisenko ON,Yarchuk OB

    更新日期:1989-04-24 00:00:00

  • Phosphorylation of the glycogen-binding subunit of protein phosphatase-1G in response to adrenalin.

    abstract::The glycogen-binding (G) subunit of protein phosphatase-1 is phosphorylated in vivo. In rabbits injected with propranolol the serine residue termed site-1 was phosphorylated in 56% of the molecules isolated, and phosphorylation increased to 82% after administration of adrenalin. It is concluded that the G-subunit is a...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(88)81331-0

    authors: MacKintosh C,Campbell DG,Hiraga A,Cohen P

    更新日期:1988-07-04 00:00:00

  • Replicable and recombinogenic RNAs.

    abstract::This paper summarizes results of the 40-year studies on replication and recombination of RNA molecules in the cell-free amplification system of bacteriophage Q. Special attention is paid to the molecular colony technique that has provided for the discovery of the nature of "spontaneous" RNA synthesis by Q replicase an...

    journal_title:FEBS letters

    pub_type: 杂志文章,评审

    doi:10.1016/j.febslet.2004.03.066

    authors: Chetverin AB

    更新日期:2004-06-01 00:00:00

  • Visualisation by electron microscopy of the unique part of the cytoplasmic domain of a desmoglein, a cadherin-like protein of the desmosome type of cell junction.

    abstract::Part of the cytoplasmic domain of a human desmoglein, Dsg1, a cadherin-like protein found in desmosomes of epithelial cells, has been visualised by electron microscopy. The cloned fragment contains five repeats of a 29 +/- 4 residue sequence unique to desmogleins, followed by a glycine-rich region. In rotary shadowed ...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(94)01049-8

    authors: Rutman AJ,Buxton RS,Burdett ID

    更新日期:1994-10-17 00:00:00

  • RNA/DNA hybrid duplexes with identical nearest-neighbor base-pairs have identical stability.

    abstract::Energetic behaviors of eight pairs of RNA/DNA hybrid duplexes with identical nearest neighbors have been investigated by UV melting analysis. In the pairs with identical nearest-neighbor pairs, the melting curve traces at the same strand concentration were very similar. The average difference in stabilization energy o...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(94)01098-6

    authors: Sugimoto N,Katoh M,Nakano S,Ohmichi T,Sasaki M

    更新日期:1994-10-31 00:00:00

  • Sphingomyelinases: enzymology and membrane activity.

    abstract::This paper reviews our present knowledge of sphingomyelinases as enzymes, and as enzymes acting on a membrane constituent lipid, sphingomyelin. Six types of sphingomyelinases are considered, namely acidic, secretory, Mg(2+)-dependent neutral, Mg(2+)-independent neutral, alkaline, and bacterial enzymes with both phosph...

    journal_title:FEBS letters

    pub_type: 杂志文章,评审

    doi:10.1016/s0014-5793(02)03482-8

    authors: Goñi FM,Alonso A

    更新日期:2002-10-30 00:00:00

  • Nucleolar disruption impairs Kaposi's sarcoma-associated herpesvirus ORF57-mediated nuclear export of intronless viral mRNAs.

    abstract::Kaposi's sarcoma-associated herpesvirus (KSHV) ORF57 plays a pivotal role in mediating the nuclear export of KSHV intronless transcripts. We demonstrate that ORF57 localises and dynamically trafficks through the nucleolus. To assess if nucleolar shuttling of ORF57 is important for the export of intronless viral mRNA, ...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2009.10.040

    authors: Boyne JR,Whitehouse A

    更新日期:2009-11-19 00:00:00

  • Substrate activation behaviour of pyruvate decarboxylase from Pisum sativum cv. Miko.

    abstract::The substrate activation behaviour of pyruvate decarboxylase from germinating seeds of Pisum sativum is characterised kinetically via stopped-flow measurements and discussed with respect to other species. The involvement of SH-groups in this process is demonstrated by reference experiments with chemically modified enz...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/s0014-5793(96)01326-9

    authors: Dietrich A,König S

    更新日期:1997-01-02 00:00:00

  • Characterization of cDNA encoding the mouse hepatic triglyceride lipase and expression by in vitro translation.

    abstract::A cDNA coding for the mouse hepatic triglyceride lipase has been isolated from a mouse liver cDNA library. The nucleotide sequence of the cDNA shows an open reading frame encoding a polypeptide of 510 amino acids that is 91.5% and 86% homologous to rat and human hepatic lipase, respectively. The most drastic protein s...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(91)80910-u

    authors: Chang SF,Netter HJ,Will H

    更新日期:1991-09-02 00:00:00

  • Physico-chemical properties of the hydroxysterol binding protein of human lymphocyte cytosol. Effects of high salt concentrations and molybdate.

    abstract::Side chain-hydroxylated derivatives of cholesterol (OH sterol) inhibiting lymphoblastic transformation bind with high affinity and specificity to a hydroxysterol binding protein (OHSBP) in the cytosol of human lymphocytes. These binding properties of OHSBP suggested some analogies with that of steroid hormone receptor...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(84)80798-x

    authors: Defay R,Astruc M,Beseme F,Descomps B,Crastes de Paulet A

    更新日期:1984-08-06 00:00:00

  • Lifespan decrease in a Caenorhabditis elegans mutant lacking TRX-1, a thioredoxin expressed in ASJ sensory neurons.

    abstract::Thioredoxins are a class of small proteins that play a key role in regulating many cellular redox processes. We report here the characterization of the first member of the thioredoxin family in metazoans that is mainly associated with neurons. The Caenorhabditis elegans gene B0228.5 encodes a thioredoxin (TRX-1) that ...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2005.12.046

    authors: Miranda-Vizuete A,Fierro González JC,Gahmon G,Burghoorn J,Navas P,Swoboda P

    更新日期:2006-01-23 00:00:00

  • High hydrostatic pressure activates gene expression through Msn2/4 stress transcription factors which are involved in the acquired tolerance by mild pressure precondition in Saccharomyces cerevisiae.

    abstract::Msn2 and Msn4 transcription factors activate expression of stress-responsive element (STRE) controlled genes in response to various stresses triggering the environmental stress response in Saccharomyces cerevisiae. Although high hydrostatic pressure is known to induce gene expression modification in yeast, the transcr...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2006.10.007

    authors: Domitrovic T,Fernandes CM,Boy-Marcotte E,Kurtenbach E

    更新日期:2006-11-13 00:00:00

  • Transforming growth factor alpha protects against Fas-mediated liver apoptosis in mice.

    abstract::The Fas/Fas ligand interaction plays a crucial role in various liver diseases, and administration of agonistic anti-Fas antibody to mice causes massive hepatic apoptosis and fulminant hepatic failure. Several growth factors have recently been found to function in preventing apoptosis. In this study, we demonstrated th...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/s0014-5793(02)02677-7

    authors: Kanda D,Takagi H,Toyoda M,Horiguchi N,Nakajima H,Otsuka T,Mori M

    更新日期:2002-05-22 00:00:00

  • Intracellular distribution of hepatic glucokinase and glucokinase regulatory protein during the fasted to refed transition in rats.

    abstract::We have studied the intracellular distribution in vivo of glucokinase (GK) and glucokinase regulatory protein (GKRP) in livers of fasted and refed rats, using specific antibodies against both proteins and laser confocal fluorescence microscopy. GK was found predominantly in the nucleus of hepatocytes from starved rats...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/s0014-5793(99)01249-1

    authors: Fernández-Novell JM,Castel S,Bellido D,Ferrer JC,Vilaró S,Guinovart JJ

    更新日期:1999-10-08 00:00:00

  • Evidence for Rap1 in vascular smooth muscle cells. Regulation of their expression by platelet-derived growth factor BB.

    abstract::The effect of platelet-derived growth factor (PDGF) on Rap1 expression was investigated in rat vascular smooth muscle cells (SMC). First, evidence for Rap1 proteins was shown by their: (i) detection in membranes using a specific anti-Rap1 antibody, (ii) typical shift in electrophoretic mobility as a consequence of red...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/0014-5793(94)80492-3

    authors: Quarck R,Bryckaert M,Magnier C,Corvazier E,Bredoux R,de Gunzburg J,Fontenay M,Tobelem G,Enouf J

    更新日期:1994-04-04 00:00:00

  • Identification of nucleolar effects in JNK-deficient cells.

    abstract::The c-Jun N-terminal kinase (JNK) signalling pathway has an established role in cellular stress signalling, cell survival and tumorigenesis. Here, we demonstrate that inhibition of JNK signalling results in partial delocalization of the RNA helicase DDX21 from the nucleolus to the nucleoplasm, increased nucleolar mobi...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2008.08.004

    authors: Mialon A,Thastrup J,Kallunki T,Mannermaa L,Westermarck J,Holmström TH

    更新日期:2008-09-03 00:00:00

  • Synthetic peptides derived from SARS coronavirus S protein with diagnostic and therapeutic potential.

    abstract::The spike (S) protein of severe acute respiratory syndrome coronavirus (SARS-CoV) is an important viral structural protein. Based on bioinformatics analysis, 10 antigenic peptides derived from the S protein sequence were selected and synthesized. The antigenicity and immunoreactivity of all the peptides were tested in...

    journal_title:FEBS letters

    pub_type: 杂志文章

    doi:10.1016/j.febslet.2005.02.070

    authors: Lu W,Wu XD,Shi MD,Yang RF,He YY,Bian C,Shi TL,Yang S,Zhu XL,Jiang WH,Li YX,Yan LC,Ji YY,Lin Y,Lin GM,Tian L,Wang J,Wang HX,Xie YH,Pei G,Wu JR,Sun B

    更新日期:2005-04-11 00:00:00