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Items: 1 to 20 of 138

1.

Benzazepinones and benzoxazepinones as antagonists of inhibitor of apoptosis proteins (IAPs) selective for the second baculovirus IAP repeat (BIR2) domain.

Donnell AF, Michoud C, Rupert KC, Han X, Aguilar D, Frank KB, Fretland AJ, Gao L, Goggin B, Hogg JH, Hong K, Janson CA, Kester RF, Kong N, Le K, Li S, Liang W, Lombardo LJ, Lou Y, Lukacs CM, Mischke S, Moliterni JA, Polonskaia A, Schutt AD, Solis DS, Specian A, Taylor RT, Weisel M, Remiszewski SW.

J Med Chem. 2013 Oct 24;56(20):7772-87. doi: 10.1021/jm400731m. Epub 2013 Oct 1.

PMID:
24083782
2.

Optimization of benzodiazepinones as selective inhibitors of the X-linked inhibitor of apoptosis protein (XIAP) second baculovirus IAP repeat (BIR2) domain.

Kester RF, Donnell AF, Lou Y, Remiszewski SW, Lombardo LJ, Chen S, Le NT, Lo J, Moliterni JA, Han X, Hogg JH, Liang W, Michoud C, Rupert KC, Mischke S, Le K, Weisel M, Janson CA, Lukacs CM, Fretland AJ, Hong K, Polonskaia A, Gao L, Li S, Solis DS, Aguilar D, Tardell C, Dvorozniak M, Tannu S, Lee EC, Schutt AD, Goggin B.

J Med Chem. 2013 Oct 24;56(20):7788-803. doi: 10.1021/jm400732v. Epub 2013 Oct 7.

PMID:
24093940
3.

Structural insight into inhibitor of apoptosis proteins recognition by a potent divalent smac-mimetic.

Cossu F, Milani M, Vachette P, Malvezzi F, Grassi S, Lecis D, Delia D, Drago C, Seneci P, Bolognesi M, Mastrangelo E.

PLoS One. 2012;7(11):e49527. doi: 10.1371/journal.pone.0049527. Epub 2012 Nov 15.

4.

Engineering ML-IAP to produce an extraordinarily potent caspase 9 inhibitor: implications for Smac-dependent anti-apoptotic activity of ML-IAP.

Vucic D, Franklin MC, Wallweber HJ, Das K, Eckelman BP, Shin H, Elliott LO, Kadkhodayan S, Deshayes K, Salvesen GS, Fairbrother WJ.

Biochem J. 2005 Jan 1;385(Pt 1):11-20.

5.

Structural basis for bivalent Smac-mimetics recognition in the IAP protein family.

Cossu F, Milani M, Mastrangelo E, Vachette P, Servida F, Lecis D, Canevari G, Delia D, Drago C, Rizzo V, Manzoni L, Seneci P, Scolastico C, Bolognesi M.

J Mol Biol. 2009 Sep 25;392(3):630-44. doi: 10.1016/j.jmb.2009.04.033. Epub 2009 Apr 22.

PMID:
19393243
6.

The structure of XIAP BIR2: understanding the selectivity of the BIR domains.

Lukacs C, Belunis C, Crowther R, Danho W, Gao L, Goggin B, Janson CA, Li S, Remiszewski S, Schutt A, Thakur MK, Singh SK, Swaminathan S, Pandey R, Tyagi R, Gosu R, Kamath AV, Kuglstatter A.

Acta Crystallogr D Biol Crystallogr. 2013 Sep;69(Pt 9):1717-25. doi: 10.1107/S0907444913016284. Epub 2013 Aug 15.

7.
8.

Design, synthesis, and biological activity of a potent Smac mimetic that sensitizes cancer cells to apoptosis by antagonizing IAPs.

Zobel K, Wang L, Varfolomeev E, Franklin MC, Elliott LO, Wallweber HJ, Okawa DC, Flygare JA, Vucic D, Fairbrother WJ, Deshayes K.

ACS Chem Biol. 2006 Sep 19;1(8):525-33. Erratum in: ACS Chem Biol. 2006 Oct 20;1(9):601.

PMID:
17168540
9.

Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.

Sun H, Lu J, Liu L, Yi H, Qiu S, Yang CY, Deschamps JR, Wang S.

J Med Chem. 2010 Sep 9;53(17):6361-7. doi: 10.1021/jm100487z.

10.

Identification of mammalian mitochondrial proteins that interact with IAPs via N-terminal IAP binding motifs.

Verhagen AM, Kratina TK, Hawkins CJ, Silke J, Ekert PG, Vaux DL.

Cell Death Differ. 2007 Feb;14(2):348-57. Epub 2006 Jun 23.

11.

A single BIR domain of XIAP sufficient for inhibiting caspases.

Takahashi R, Deveraux Q, Tamm I, Welsh K, Assa-Munt N, Salvesen GS, Reed JC.

J Biol Chem. 1998 Apr 3;273(14):7787-90.

12.

Characterization of dequalinium as a XIAP antagonist that targets the BIR2 domain.

Orzáez M, Gortat A, Sancho M, Carbajo RJ, Pineda-Lucena A, Palacios-Rodríguez Y, Pérez-Payá E.

Apoptosis. 2011 May;16(5):460-7. doi: 10.1007/s10495-011-0582-4.

PMID:
21340509
13.

The human anti-apoptotic proteins cIAP1 and cIAP2 bind but do not inhibit caspases.

Eckelman BP, Salvesen GS.

J Biol Chem. 2006 Feb 10;281(6):3254-60. Epub 2005 Dec 8.

14.

Interaction of a cyclic, bivalent smac mimetic with the x-linked inhibitor of apoptosis protein.

Nikolovska-Coleska Z, Meagher JL, Jiang S, Yang CY, Qiu S, Roller PP, Stuckey JA, Wang S.

Biochemistry. 2008 Sep 16;47(37):9811-24. doi: 10.1021/bi800785y. Epub 2008 Aug 22.

15.
16.

XIAP inhibits caspase-3 and -7 using two binding sites: evolutionarily conserved mechanism of IAPs.

Scott FL, Denault JB, Riedl SJ, Shin H, Renatus M, Salvesen GS.

EMBO J. 2005 Feb 9;24(3):645-55. Epub 2005 Jan 13.

17.

Inhibitors of apoptotic proteins: new targets for anticancer therapy.

Saleem M, Qadir MI, Perveen N, Ahmad B, Saleem U, Irshad T, Ahmad B.

Chem Biol Drug Des. 2013 Sep;82(3):243-51. doi: 10.1111/cbdd.12176. Review.

PMID:
23790005
18.

The discovery of macrocyclic XIAP antagonists from a DNA-programmed chemistry library, and their optimization to give lead compounds with in vivo antitumor activity.

Seigal BA, Connors WH, Fraley A, Borzilleri RM, Carter PH, Emanuel SL, Fargnoli J, Kim K, Lei M, Naglich JG, Pokross ME, Posy SL, Shen H, Surti N, Talbott R, Zhang Y, Terrett NK.

J Med Chem. 2015 Mar 26;58(6):2855-61. doi: 10.1021/jm501892g. Epub 2015 Mar 12.

19.

Design and characterization of bivalent Smac-based peptides as antagonists of XIAP and development and validation of a fluorescence polarization assay for XIAP containing both BIR2 and BIR3 domains.

Nikolovska-Coleska Z, Meagher JL, Jiang S, Kawamoto SA, Gao W, Yi H, Qin D, Roller PP, Stuckey JA, Wang S.

Anal Biochem. 2008 Mar 1;374(1):87-98. Epub 2007 Nov 20.

PMID:
18023397
20.

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

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

Biochem Biophys Res Commun. 2009 Jan 9;378(2):162-7. doi: 10.1016/j.bbrc.2008.10.139. Epub 2008 Nov 4.

PMID:
18992220
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