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


: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.


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




Has Abstract


2009-01-09 00:00:00














  • LncRNA TP73-AS1 predicts the prognosis of bladder cancer patients and functions as a suppressor for bladder cancer by EMT pathway.

    abstract::Long noncoding RNAs (lncRNAs) have been identified to have more and more important roles in tumorigenesis and may be novel biomarker for cancer therapy. LncRNA TP73-AS1 is a novel identified lncRNA that has been demonstrated to be increased in several cancers, however, its function in bladder cancer remains unknown. T...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Tuo Z,Zhang J,Xue W

    更新日期:2018-05-23 00:00:00

  • Regulation of progastricsin mRNA levels in sea bass (Dicentrarchus labrax) in response to fluctuations in food availability.

    abstract::In this study the sea bass (Dicentrarchus labrax) pepsinogen C gene was isolated. The nucleotide sequences of all exons are presented. The organization of the gene is compatible with that of other aspartic proteinases. The predicted 388-residue amino acid (aa) sequence of sea bass pepsinogen C consists of a signal seq...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Terova G,Rimoldi S,Larghi S,Bernardini G,Gornati R,Saroglia M

    更新日期:2007-11-23 00:00:00

  • Functional characterization of mouse cation transporter mOCT2 compared with mOCT1.

    abstract::We characterized the function of mouse organic cation transporter OCT2 (TC 2.A.19.1.5) in comparison with that of OCT1 (TC 2.A.19.1.1). Uptake of [(3)H]1-methyl-4-phenylpyridinium ([(3)H]MPP(+)) by Xenopus laevis oocytes injected with mOCT1 (Slc22a1) or mOCT2 (Slc22a2) cRNA was attenuated by an increase of extracellul...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Kakehi M,Koyabu N,Nakamura T,Uchiumi T,Kuwano M,Ohtani H,Sawada Y

    更新日期:2002-08-23 00:00:00

  • A method for specific cloning and sequencing of human hprt cDNA for mutation analysis.

    abstract::A method has been developed for the specific amplification and cloning of human hprt cDNA which can be used for mutant sequence analysis. Messenger RNA is isolated from TK6 lymphoblasts and is used to produce a first strand cDNA with reverse transcriptase primed with oligo dT. Second strand synthesis and subsequent am...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Simpson D,Crosby RM,Skopek TR

    更新日期:1988-02-29 00:00:00

  • Pentamethylquercetin protects against cardiac remodeling via activation of Sestrin2.

    abstract::Oxidative stress is widely involved in pathophysiological processes of cardiac remodeling. Molecules associated with antioxidant functions may be ideal targets for reversing cardiac remodeling. Sestrin2 is the important component of endogenous antioxidant defense, while there is little information on the pathophysiolo...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Du JX,Wu JZ,Li Z,Zhang C,Shi MT,Zhao J,Jin MW,Liu H

    更新日期:2019-04-30 00:00:00

  • Influence of the degree of unsaturation of the acyl side chain upon the interaction of analogues of 1-arachidonoylglycerol with monoacylglycerol lipase and fatty acid amide hydrolase.

    abstract::Little is known as to the structural requirements of the acyl side chain for interaction of acylglycerols with monoacylglycerol lipase (MAGL), the enzyme chiefly responsible for the metabolism of the endocannabinoid 2-arachidonoylglycerol (2-AG) in the brain. In the present study, a series of twelve analogues of 1-AG ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Vandevoorde S,Saha B,Mahadevan A,Razdan RK,Pertwee RG,Martin BR,Fowler CJ

    更新日期:2005-11-11 00:00:00

  • Molecular hierarchy in neurons differentiated from mouse ES cells containing a single human chromosome 21.

    abstract::Defects in neurogenesis and neuronal differentiation in the fetal brain of Down syndrome (DS) patients lead to the apparent neuropathological abnormalities and contribute to the phenotypic characters of mental retardation, and premature development of Alzheimer's disease, those being the most common phenotype in DS. I...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Wang CC,Kadota M,Nishigaki R,Kazuki Y,Shirayoshi Y,Rogers MS,Gojobori T,Ikeo K,Oshimura M

    更新日期:2004-02-06 00:00:00

  • Alpha interferon accelerates lateral diffusion of Daudi cell surface differentiation antigens: measurement by fluorescence redistribution after photobleaching.

    abstract::Lateral diffusion coefficients (D) of two surface differentiation antigens (sIgM and Bp35) were determined on interferon-sensitive (-IFs) or resistant (-IFr) Daudi cells by fluorescence photobleaching, using monospecific FITC-anti-IgM or PE-anti-Leu 16 probes. For untreated Daudi -IFs, mean (D) were 5.8 and 5.3 (x10(-...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Balint E,Aszalos A,Grimley PM

    更新日期:1988-12-15 00:00:00

  • EVI1 is expressed in megakaryocyte cell lineage and enforced expression of EVI1 in UT-7/GM cells induces megakaryocyte differentiation.

    abstract::3q21q26 syndrome, an acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) with chromosomal translocations or inversions between the bands 3q21 and 3q26, is frequently associated with dysmegakaryocytopoiesis and increased platelet counts at the initial diagnosis. Since the EVI1 gene at 3q26 is transcriptional...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Shimizu S,Nagasawa T,Katoh O,Komatsu N,Yokota J,Morishita K

    更新日期:2002-04-05 00:00:00

  • Caveolin-1 up-regulates ST6Gal-I to promote the adhesive capability of mouse hepatocarcinoma cells to fibronectin via FAK-mediated adhesion signaling.

    abstract::Caveolin-1 is a major structural protein of caveolae and plays important functions in tumorigenesis and development. Hca-F and Hepa1-6 are mouse hepatocarcinoma cell lines with high and low malignant potential, respectively. Our previous studies revealed that caveolin-1 promoted cell invasion by up-regulating the glyc...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Yu S,Zhang L,Li N,Fan J,Liu L,Zhang J,Wang S

    更新日期:2012-10-26 00:00:00

  • Circular dichroism spectra demonstrate formation of the thrombin-binding DNA aptamer G-quadruplex under stabilizing-cation-deficient conditions.

    abstract::It is noteworthy that the formation of the DNA G-quadruplex is induced by factors other than stabilizing cations because this event probably occurs in living cells. Previous studies have shown that thrombin-binding DNA aptamer (TBA) forms a chair-type intramolecular G-quadruplex structure that binds with thrombin prot...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Nagatoishi S,Tanaka Y,Tsumoto K

    更新日期:2007-01-19 00:00:00

  • Elicitation of metastasis associated protein 2 expression in the phagocytosis by murine testicular Sertoli cells.

    abstract::Efficient phagocytic clearance of apoptotic spermatogenic cells and residual bodies (RBs) by Sertoli cells (SCs) is crucial for functional mature spermatogenesis. However, little is known about the molecular mechanisms underlying this SCs function. Herein, we reported for the first time that SCs-expressing metastasis ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Zhu CJ,Zhang S,Liang Y,Li W

    更新日期:2014-03-14 00:00:00

  • Time-course curves of enzyme reactions with dilute substrates can be determined from the reverse reactions.

    abstract::We present a novel and useful principle that can be applied to enzyme reactions with dilute substrates and enables to obtain the desired time-course curve from the reverse reaction when the latter can be measured more easily. Let us imagine an enzyme mixture that can catalyze the interconversion between substances A, ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Kijima S,Kijima H

    更新日期:1994-09-15 00:00:00

  • Purification of normal cellular prion protein from human platelets and the formation of a high molecular weight prion protein complex following platelet activation.

    abstract::A method for the extraction and purification of PrP(C), in its native monomeric form, from outdated human platelet concentrates is described. Both calcium ionophore platelet activation and lysis in Triton X-100 were evaluated as methods for the extraction of soluble platelet PrP(C) in its monomeric form. Following pla...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Jones M,Head MW,Connolly JG,Farquhar CF,Hornsey VS,Pepper DS,MacGregor IR

    更新日期:2005-09-16 00:00:00

  • Genotoxicity of human milk extracts and detection of DNA damage in exfoliated cells recovered from breast milk.

    abstract::Genotoxic agents of environmental or dietary origin may play a role in breast cancer initiation. The ability of extracts of human milk to cause mutations in S. typhimurium TA1538 and YG1019 and to induce micronuclei and DNA strand breaks in MCL-5 cells was investigated. Twenty samples from different donors were analys...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Martin FL,Cole KJ,Weaver G,Grover PL,Phillips DH

    更新日期:1999-04-13 00:00:00

  • Mutation of the carboxy terminal zinc finger of E. coli isoleucyl-tRNA synthetase alters zinc binding and aminoacylation activity.

    abstract::Escherichia coli isoleucyl-tRNA synthetase has been shown to contain two enzyme-bound zinc atoms per polypeptide chain. To investigate the structural and functional significance of the C-terminal enzyme-bound zinc, mutagenesis was used to alter Cys 922 to Ser [IleRS(C922S)] and to replace Cys 922 through Ala 939 with ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Zhou L,Rosevear PR

    更新日期:1995-11-13 00:00:00

  • tsBN75 and tsBN423, temperature-sensitive x-linked mutants of the BHK21 cell line, can be complemented by the ubiquitin-activating enzyme E1 cDNA.

    abstract::tsBN75 and tsBN423 are independently isolated temperature-sensitive (ts) mutants of the BHK21 cell line for cell growth. Both tsBN75 and tsBN423 belong to the same complementation group and show G2 block at the nonpermissive temperature. Both were efficiently transformed to ts+ cells with the mouse and human cDNA enco...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Nishitani H,Goto H,Kaneda S,Yamao F,Seno T,Handley P,Schwartz AL,Nishimoto T

    更新日期:1992-04-30 00:00:00

  • Activated macrophages kill pancreatic syngeneic islet cells via arginine-dependent nitric oxide generation.

    abstract::IL-1 and TNF alpha are assumed to be major mediators of islet cell destruction during the pathogenesis of type 1 diabetes. Here we show by neutralization of the two cytokines with excess antibody that IL-1 and TNF alpha do not contribute to the cytotoxic activity of activated macrophages towards isolated islet cells. ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Kröncke KD,Kolb-Bachofen V,Berschick B,Burkart V,Kolb H

    更新日期:1991-03-29 00:00:00

  • Enhancer binding proteins predicted by informational spectrum method.

    abstract::Enhancer sequences analysed using the informational spectrum method (ISM) show a characteristic frequency at .0488. It has been shown that the characteristic frequency for some DNA binding proteins overlaps the characteristic frequency of their target DNA sequences. We suggest here that two types of proteins, homeopro...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Cosić I,Nesić D,Pavlović M,Williams R

    更新日期:1986-12-15 00:00:00

  • Tissue- and stressor-specific differential expression of two hsc70 genes in carp.

    abstract::Two genes expressing 70 kDa heat shock proteins were identified in Cyprinus carpio. The sequence similarities and the intron-interrupted structure of the coding regions indicate that carp Hsc70-1 and Hsc70-2 belong to the Hsp70 cognate subfamily. The expressions of the two hsc70 genes were followed by semi-quantitativ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Ali KS,Dorgai L,Abrahám M,Hermesz E

    更新日期:2003-08-01 00:00:00

  • Adrenodoxin supports reactions catalyzed by microsomal steroidogenic cytochrome P450s.

    abstract::The interaction of adrenodoxin (Adx) and NADPH cytochrome P450 reductase (CPR) with human microsomal steroidogenic cytochrome P450s was studied. It is found that Adx, mitochondrial electron transfer protein, is able to support reactions catalyzed by human microsomal P450s: full length CYP17, truncated CYP17, and trunc...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Pechurskaya TA,Harnastai IN,Grabovec IP,Gilep AA,Usanov SA

    更新日期:2007-02-16 00:00:00

  • Microinjection of an nm23 specific antibody inhibits cell division in rat embryo fibroblasts.

    abstract::Expression of the nm23/NDP-K gene correlates with reduced metastasis in some tumors and with increased proliferation in both nontransformed and transformed cells in culture. Decreased nm23/NDP-K expression results in mitotic arrest in neuroblasts of developing Drosophila. In order to better understand the biological r...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Sorscher SM,Steeg P,Feramisco JR,Buckmaster C,Boss GR,Meinkoth J

    更新日期:1993-08-31 00:00:00

  • Transforming growth factor-beta inhibits endothelial cell proliferation.

    abstract::Transforming growth factor-beta (TGF-beta) is an inhibitor of the proliferation of bovine aortic endothelial cells in culture. Basal cell growth in serum-containing medium and cell proliferation stimulated by fibroblast growth factor (FGF) are inhibited by TGF-beta in a dose-dependent manner. Half-maximal inhibition o...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Fràter-Schröder M,Müller G,Birchmeier W,Böhlen P

    更新日期:1986-05-29 00:00:00

  • An aprotinin binding site localized in the hormone binding domain of the estrogen receptor from calf uterus.

    abstract::It has been proposed that the estrogen receptor bears proteolytic activity responsible for its own transformation. This activity was inhibited by aprotinin. Incubation of transformed ER with aprotinin modified the proteolytic digestion of the hormone binding subunit by proteinase K. The smallest hormone-binding fragme...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Nigro V,Medici N,Abbondanza C,Minucci S,Moncharmont B,Molinari AM,Puca GA

    更新日期:1990-07-31 00:00:00

  • Induction of ornithine decarboxylase activity in mouse tissues by phorbol ester is effectively blocked by methylglyoxal bis(butylamidinohydrazone).

    abstract::Ornithine decarboxylase (ODC) was induced in the liver, lung and brain of the mouse injected intraperitoneally with 12-O-tetradecanoylphorbol 13-acetate (TPA), showing maximal enzyme activity four hours after the injection. The increase of ODC activity was due to the enhanced syntheses of mRNA and protein. The inducti...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Hibasami H,Tsukada T,Maekawa S,Sakurai M,Nakashima K

    更新日期:1987-04-29 00:00:00

  • Purification of the yellow fluorescent protein from Vibrio fischeri and identity of the flavin chromophore.

    abstract::A low molecular weight protein (approximately 25,000 D) exhibiting a yellow fluorescence emission peaking at approximately 540 nm was isolated from Vibrio fischeri (strain Y-1) and purified to apparent homogeneity. FMN is the chromophore, but it exhibits marked red shifts in both the absorption (lambda max = 380, 460 ...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Macheroux P,Schmidt KU,Steinerstauch P,Ghisla S,Colepicolo P,Buntic R,Hastings JW

    更新日期:1987-07-15 00:00:00

  • Rat insulinoma-derived pancreatic beta-cells express a functional leptin receptor that mediates a proliferative response.

    abstract::In addition to its interaction at hypothalamic sites to affect feeding and energy expenditure, leptin has been shown to exhibit a proliferative response in erythropoietic cells. The functional leptin receptor is also present in pancreatic islets and we now demonstrate that a commonly used clonal insulin secreting beta...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Islam MS,Morton NM,Hansson A,Emilsson V

    更新日期:1997-09-29 00:00:00

  • TNFalpha induces HIF-1alpha expression through activation of IKKbeta.

    abstract::The transcription factor hypoxia-inducible factor 1alpha (HIF-1alpha) is regulated by oxygen availability as well as various inflammatory mediators, including tumor necrosis factor alpha (TNFalpha). Early work suggested that the phosphatidylinositol-3-kinase (PI3K) and mitogen-activated protein kinase (MAPK) signaling...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Kuo HP,Lee DF,Xia W,Wei Y,Hung MC

    更新日期:2009-11-27 00:00:00

  • Mitochondrial DNA mutation m.3635G>A may be associated with Leber hereditary optic neuropathy in Chinese.

    abstract::Leber hereditary optic neuropathy (LHON) was the first disease to be linked to the presence of a mitochondrial DNA (mtDNA) mutation. Nowadays over 95% of LHON cases are known to be caused by one of three primary mutations (m.11778G>A, m.14484T>C, and m.3460G>A). Reports for other (rare) primary mutations in LHON patie...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Zhang AM,Zou Y,Guo X,Jia X,Zhang Q,Yao YG

    更新日期:2009-08-21 00:00:00

  • Resveratrol restores the circadian rhythmic disorder of lipid metabolism induced by high-fat diet in mice.

    abstract::Circadian rhythmic disorders induced by high-fat diet are associated with metabolic diseases. Resveratrol could improve metabolic disorder, but few reports focused on its effects on circadian rhythm disorders in a variety of studies. The aim of the present study was to analyze the potential effects of resveratrol on h...

    journal_title:Biochemical and biophysical research communications

    pub_type: 杂志文章


    authors: Sun L,Wang Y,Song Y,Cheng XR,Xia S,Rahman MR,Shi Y,Le G

    更新日期:2015-02-27 00:00:00