Designing Smac-mimetics as antagonists of XIAP, cIAP1, and cIAP2.

Abstract:

:Inhibitor of apoptosis proteins (IAPs) such as XIAP, cIAP1, and cIAP2 are upregulated in many cancer cells. Several compounds targeting IAPs and inducing cell death in cancer cells have been developed. Some of these are synthesized mimicking the N-terminal tetrapeptide sequence of Smac/DIABLO, the natural endogenous IAPs inhibitor. Starting from such conceptual design, we generated a library of 4-substituted azabicyclo[5.3.0]alkane Smac-mimetics. Here we report the crystal structure of the BIR3 domain from XIAP in complex with Smac037, a compound designed according to structural principles emerging from our previously analyzed XIAP BIR3/Smac-mimetic complexes. In parallel, we present an in silico docking analysis of three Smac-mimetics to the BIR3 domain of cIAP1, providing general considerations for the development of high affinity lead compounds targeting three members of the IAP family.

authors

Cossu F,Mastrangelo E,Milani M,Sorrentino G,Lecis D,Delia D,Manzoni L,Seneci P,Scolastico C,Bolognesi M

doi

10.1016/j.bbrc.2008.10.139

subject

Has Abstract

pub_date

2009-01-09 00:00:00

pages

162-7

issue

2

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(08)02112-8

journal_volume

378

pub_type

杂志文章
  • Adrenomedullin stimulates cyclic AMP formation in rat vascular smooth muscle cells.

    abstract::A newly identified human peptide, adrenomedullin (AM) increased cAMP levels with dose and time dependencies in a manner similar to that of human calcitonin gene-related peptide (CGRP) in rat vascular smooth muscle cells (VSMC). The EC50 value of human AM is 2 x 10(-8) M which is slightly higher than that of CGRP (8.5 ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.1994.1496

    authors: Ishizaka Y,Ishizaka Y,Tanaka M,Kitamura K,Kangawa K,Minamino N,Matsuo H,Eto T

    更新日期:1994-04-15 00:00:00

  • TLE, the human homolog of groucho, interacts with AML1 and acts as a repressor of AML1-induced transactivation.

    abstract::The AML1 gene encodes DNA-binding proteins that contain the Runt domain and is found at the breakpoints of some translocations associated with leukemias. It has been reported that AML1 plays pivotal roles in myeloid differentiation, probably through the transcriptional regulation of various hematopoietic genes. Here w...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.1998.9705

    authors: Imai Y,Kurokawa M,Tanaka K,Friedman AD,Ogawa S,Mitani K,Yazaki Y,Hirai H

    更新日期:1998-11-27 00:00:00

  • Skeletal analysis and differential gene expression in Runx2/Osterix double heterozygous embryos.

    abstract::The transcription factors, Runx2 and Osterix (Osx), act downstream in the BMP2 pathway, and they are essential for osteoblast differentiation and bone formation. While Runx2 expression is normal in Osx-null mice, Osx is not expressed in Runx2-null mice, indicating that Osx acts downstream of Runx2 during bone formatio...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2014.08.010

    authors: Baek JE,Choi JY,Kim JE

    更新日期:2014-08-29 00:00:00

  • The myosin head can bind two actin monomers.

    abstract::Force impulse is thought to be generated in muscle when myosin head (S-1), while weakly bound to actin filament, undergoes orientational change to form a strong (rigor) bond with actin. There is ample evidence that this bond involves interaction of 1 myosin head with 1 actin monomer. However, X-ray diffraction data of...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/0006-291x(91)91990-t

    authors: Andreev OA,Borejdo J

    更新日期:1991-05-31 00:00:00

  • Altered gelatinolytic activity by keratoconus corneal cells.

    abstract::Keratoconus involves thinning and central protuberance of the cornea, scarring and significantly decreased vision. It is one of the major causes of corneal transplantation in this country, but the etiology of this disorder is unclear. In the present study stromal keratocytes were isolated and cultured from normal and ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/0006-291x(89)91604-5

    authors: Kenney MC,Chwa M,Escobar M,Brown D

    更新日期:1989-05-30 00:00:00

  • Evidence for production of hydroxyl radicals by pentachlorophenol metabolites and hydrogen peroxide: A metal-independent organic Fenton reaction.

    abstract::The production of hydroxyl radicals by tetrachlorohydroquinone (TCHQ, a major metabolite of the widely used biocide pentachlorophenol) in the presence of H(2)O(2) was studied by salicylate hydroxylation method. HPLC with electrochemical detection was used to measure the levels of 2,3- and 2,5-dihydroxybenzoic acid (DH...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.2000.2539

    authors: Zhu BZ,Kitrossky N,Chevion M

    更新日期:2000-04-21 00:00:00

  • Inhibition of protein import into mitochondria by amphiphilic cations: potential targets and mechanism of action.

    abstract::In this paper we describe for the first time the inhibitory effect of three amphiphilic cations, trifluoperazine, propranolol and dibucaine on mitochondrial protein import. The amphiphilic cations did not affect binding of mitochondrial precursor proteins to mitochondria. Import into mitoplasts was affected in a simil...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.1998.9590

    authors: Pavlov PF,Glaser E

    更新日期:1998-11-09 00:00:00

  • Ornithine decarboxylase is directly involved in mouse mammary carcinoma cell invasion in vitro.

    abstract::To elucidate the role of ornithine decarboxylase (ODC) in cancer cell invasion, we have compared the invasiveness of mouse mammary carcinoma, FM3A and its variant cell line, EXOD, which overproduces ODC. We have found that EXOD cells showed about 5.6-fold more invasiveness through a reconstituted basement membrane (Ma...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.1995.1448

    authors: Kubota S,Yamada T,Kamei S,Seyama Y

    更新日期:1995-03-28 00:00:00

  • UDP-glucuronosyltransferase 1A7 polymorphisms are associated with liver cirrhosis.

    abstract::Variations in the UDP-glucuronosyltransferase (UGT) 1A7 gene have been found to be related to the development of hepatocellular carcinoma (HCC). Since the pathogenesis of liver cirrhosis is not dissimilar to that of HCC, we hypothesized that UGT1A7 genetic polymorphisms may be associated with liver cirrhosis. PCR-rest...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2007.11.125

    authors: Tang KS,Lee CM,Teng HC,Huang MJ,Huang CS

    更新日期:2008-02-15 00:00:00

  • Knockdown of TIGAR by RNA interference induces apoptosis and autophagy in HepG2 hepatocellular carcinoma cells.

    abstract::Apoptosis and autophagy are crucial mechanisms regulating cell death, and the relationship between apoptosis and autophagy in the liver has yet to be thoroughly explored. TIGAR (TP53-induced glycolysis and apoptosis regulator), which is a p53-inducible gene, functions in the suppression of ROS (reactive oxygen species...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2013.06.072

    authors: Ye L,Zhao X,Lu J,Qian G,Zheng JC,Ge S

    更新日期:2013-07-26 00:00:00

  • Trypanosoma cruzi: TcRAB7 protein is localized at the Golgi apparatus in epimastigotes.

    abstract::In mammalian cells, the Rab7 protein is a key element of late endocytic membrane traffic. Several results suggest that it is involved in the transport from early to late endosome or from late endosome to lysosome. We have previously characterized a Rab7 gene homologue (TcRAB7) in Trypanosoma cruzi. Now, using an affin...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2004.06.159

    authors: Araripe JR,Cunha e Silva NL,Leal ST,de Souza W,Rondinelli E

    更新日期:2004-08-20 00:00:00

  • Plicatamide: A lead to the biosynthetic origins of the tunichromes?

    abstract::Plicatamide is a modified octapeptide from the ascidian Styela plicata having the structure Phe-Phe-His-Leu-His-Phe-His-decarboxyDeltaDOPA (where decarboxyDeltaDOPA = decarboxy-(E)-alpha,beta-dehydro-3, 4-dihydroxyphenylalanine). Edman sequencing, tandem mass spectrometry, and proton NMR have been used to characterize...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.2000.2449

    authors: Tincu JA,Craig AG,Taylor SW

    更新日期:2000-04-13 00:00:00

  • BmICE-2 is a novel pro-apoptotic caspase involved in apoptosis in the silkworm, Bombyx mori.

    abstract::In this study we identified a potential pro-apoptotic caspase gene, Bombyx mori(B. mori)ICE-2 (BmICE-2) which encoded a polypeptide of 284 amino acid residues, including a (169)QACRG(173) sequence which surrounded the catalytic site and contained a p20 and a p10 domain. BmICE-2 expressed in Escherichia coli (E. coli) ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2014.01.139

    authors: Yi HS,Pan CX,Pan C,Song J,Hu YF,Wang L,Pan MH,Lu C

    更新日期:2014-02-28 00:00:00

  • Cloning and characterization of a novel RNA polymerase II C-terminal domain phosphatase.

    abstract::Reversible phosphorylation of RNA polymerase (RNAP) II's largest subunit C-terminal domain (CTD) is a key event during mRNA metabolism. The CTD phosphatase, FCP1, catalyzes the dephosphorylation of RNAP II and is thought to play a major role in polymerase recycling. In this study, we isolated a novel phosphatase gene ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2005.04.065

    authors: Zheng H,Ji C,Gu S,Shi B,Wang J,Xie Y,Mao Y

    更新日期:2005-06-17 00:00:00

  • GPI-alkaline phosphatase insertion into phosphatidylcholine monolayers: phase behavior and morphology changes.

    abstract::GPI-anchored proteins are localized on the outer layer of plasma membranes and clustered in microdomains generally called lipid rafts. To study the interactions between the lipidic GPI-anchor of the protein and phospholipids, we used phosphatidylcholine monolayers at the air-water interface as a biomimetic membrane sy...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2005.06.049

    authors: Kouzayha A,Besson F

    更新日期:2005-08-12 00:00:00

  • Effect of ELOVL3 expression on bovine skeletal muscle-derived satellite cell differentiation.

    abstract::ELOVL3 is involved in elongating saturated and monounsaturated fatty acids, and is a critical enzyme for lipid accumulation in brown adipocytes during the early phase of tissue recruitment. In addition, ELOVL3 is related to increased fatty acid oxidation in brown adipocytes. However, the potential functions of ELOVL3 ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2017.07.118

    authors: Liu D,Xu JH,Tong HL,Li SF,Yan YQ

    更新日期:2017-12-02 00:00:00

  • Bufalin inhibits cell proliferation and migration of hepatocellular carcinoma cells via APOBEC3F induced intestinal immune network for IgA production signaling pathway.

    abstract:OBJECTIVE:This study aimed to evaluate functions of APOBEC3F gene in biological process of hepatocellular carcinoma (HCC) and anti-tumor mechanisms of bufalin. METHODS:Effect of APOBEC3F and bufalin on cell proliferation and migration abilities were evaluated by CCK-8, wounding healing tests and transwell assays in SK...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2018.07.169

    authors: Yang Z,Tao Y,Xu X,Cai F,Yu Y,Ma L

    更新日期:2018-09-10 00:00:00

  • Glutathione increases the binding affinity of a bovine B₁₂ trafficking chaperone bCblC for vitamin B₁₂.

    abstract::Intracellular B(12) metabolism involves a B(12) trafficking chaperone CblC that is well conserved in mammals including human. The protein CblC is known to bind cyanocobalamin (CNCbl, vitamin B(12)) inducing the base-off transition and convert it into an intermediate that can be used in enzyme cofactor synthesis. The b...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2011.07.103

    authors: Jeong J,Kim J

    更新日期:2011-08-26 00:00:00

  • Granulins, a novel class of peptide from leukocytes.

    abstract::We report the isolation and characterization of a novel class of leukocyte peptides with possible cytokine-like activities which we call granulins. They are cystine-rich with molecular weights of approximately 6 Kda, except for granulin D, which appears to be a dimer. We present the sequence of one member of this fami...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/s0006-291x(05)80908-8

    authors: Bateman A,Belcourt D,Bennett H,Lazure C,Solomon S

    更新日期:1990-12-31 00:00:00

  • TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin) reduces lipoprotein lipase activity in the adipose tissue of the guinea pig.

    abstract::TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin) administered to young male guinea pigs at a dose of 1 microgram/kg (single intraperitoneal injection) caused a large reduction in adipose tissue lipoprotein lipase (LPL) activity. This effect occurred rapidly; a 70% decrease was noticed after 24 hour and 80% of LPL activity w...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/s0006-291x(84)80106-0

    authors: Brewster DW,Matsumura F

    更新日期:1984-07-31 00:00:00

  • Establishment of a novel method for the identification of fertilization defective mutants in Arabidopsis thaliana.

    abstract::Plant reproduction is an extremely important phenomenon, as it is strongly associated with plant genetics and early development. Additionally, foundations of the reproductive system have direct implications on plant breeding and agriculture. Investigation of the functions of male and female gametophytes is critical si...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2019.11.028

    authors: Liu X,Wu X,Adhikari PB,Zhu S,Kinoshita Y,Berger F,Higashiyama T,Kasahara RD

    更新日期:2020-01-22 00:00:00

  • Efficient production and purification of functional bacteriorhodopsin with a wheat-germ cell-free system and a combination of Fos-choline and CHAPS detergents.

    abstract::Cell-free translation is one potential approach to the production of functional transmembrane proteins. We have now examined various detergents as supplements to a wheat-germ cell-free system in order to optimize the production and subsequent purification of a functional model transmembrane protein, bacteriorhodopsin....

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2010.08.119

    authors: Genji T,Nozawa A,Tozawa Y

    更新日期:2010-10-01 00:00:00

  • Salinity- and ABA-induced up-regulation and light-mediated modulation of mRNA encoding glycine-rich RNA-binding protein from Sorghum bicolor.

    abstract::Glycine-rich RNA-binding proteins play an important role in post-transcriptional regulation of gene expression, including RNA processing, and are known to be up-regulated in response to a number of external stimuli. However, their regulation in response to salinity stress has not been reported. We have isolated a ligh...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/s0006-291x(02)02050-8

    authors: Aneeta,Sanan-Mishra N,Tuteja N,Kumar Sopory S

    更新日期:2002-09-06 00:00:00

  • Regulation of tankyrase activity by a catalytic domain dimer interface.

    abstract::Tankyrases (TNKS and TNKS2) are enzymes that catalyze poly-ADP-ribosylation (PARsylation) of their target proteins. Tankyrase-mediated PARsylation plays critical regulatory roles in cell signaling, particularly in the Wnt/β-catenin pathway. The sterile alpha motif (SAM) domain in tankyrases mediates their oligomerizat...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2018.07.113

    authors: Fan C,Yarravarapu N,Chen H,Kulak O,Dasari P,Herbert J,Yamaguchi K,Lum L,Zhang X

    更新日期:2018-09-10 00:00:00

  • Peptides from pinto bean and red bean with sequence homology to cowpea 10-kDa protein precursor exhibit antifungal, mitogenic, and HIV-1 reverse transcriptase-inhibitory activities.

    abstract::Peptides with a molecular weight of 5 kDa have been isolated from seeds of the pinto bean and red bean, respectively. The peptides manifest an N-terminal sequence with remarkable resemblance to those of cowpea 10-kDa protein precursor and garden pea disease resistance response protein. The bean peptides possess potent...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.2001.5194

    authors: Ye XY,Ng TB

    更新日期:2001-07-13 00:00:00

  • Interaction of rat lin-10 with brain-enriched F-actin-binding protein, neurabin-II/spinophilin.

    abstract::We have recently isolated a rat homologue of the Caenorrhabditis elegans lin-10 product. Although rat lin-10 is expressed in the cytosol and membrane fractions of various tissues, it is distributed only in the membrane fraction in brain where it is enriched in the synaptic plasma membrane and postsynaptic density frac...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.1998.8243

    authors: Ide N,Hata Y,Hirao K,Irie M,Deguchi M,Yao I,Satoh A,Wada M,Takahashi K,Nakanishi H,Takai Y

    更新日期:1998-03-06 00:00:00

  • Association of the putative B-lymphocyte surface molecule B7.3 with a protein kinase activity.

    abstract::Monoclonal antibody BB1 was previously shown to recognize the CD80 protein as well as a putative B7.3 molecule, both ligands of the important T-cell receptors CD28 and CTLA-4. We report that BB1 coprecipitated from detergent lysates of human B- and pre-B-cell lines a protein kinase activity, as detected by solid phase...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1006/bbrc.1996.1687

    authors: Angelisová P,Cerný J,Horejsí V

    更新日期:1996-11-12 00:00:00

  • PLAP-1/asporin inhibits activation of BMP receptor via its leucine-rich repeat motif.

    abstract::We previously identified the novel gene, periodontal ligament-associated protein-1 (PLAP-1)/asporin and reported that PLAP-1/asporin inhibited bone morphogenetic protein-2 (BMP-2)-induced cytodifferentiation of periodontal ligament (PDL) cells probably by direct interaction with BMP-2. Here, we elucidated the detailed...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2008.03.158

    authors: Tomoeda M,Yamada S,Shirai H,Ozawa Y,Yanagita M,Murakami S

    更新日期:2008-06-27 00:00:00

  • DNA-mediated transformation of N-acetylglucosaminyltransferase I activity into an enzyme deficient cell line.

    abstract::N-acetylglucosaminyltransferase I (GlcNAc-TI) catalyzes the first reaction in the conversion of ASN-linked cell surface oligosaccharides from a mannose-terminating structure to more complex carbohydrate structures. The mutant Chinese hamster ovary (CHO) cell line, Lec1, is deficient in this enzyme and, therefore, show...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/0006-291x(89)90029-6

    authors: Ripka J,Pierce M,Fregien N

    更新日期:1989-03-15 00:00:00

  • High resolution structure of Vibrio cholerae acylphosphatase (VcAcP) cage: Identification of drugs, location of its binding site and engineering to facilitate cage formation.

    abstract::Protein cages have recently emerged as an extraordinary drug-delivery system due to its biocompatibility, biodegradability, low toxicity, ease to manipulate and engineer. We have reported earlier the formation and architecture of a do-decameric cage-like architecture of Vibrio cholerae acylphosphatase (VcAcP) at 3.1 Å...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章

    doi:10.1016/j.bbrc.2019.12.060

    authors: Chatterjee S,Nath S,Sen U

    更新日期:2020-03-05 00:00:00