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Items: 1 to 20 of 79

1.

Dimeric Smac mimetics/IAP inhibitors as in vivo-active pro-apoptotic agents. Part II: Structural and biological characterization.

Lecis D, Mastrangelo E, Belvisi L, Bolognesi M, Civera M, Cossu F, De Cesare M, Delia D, Drago C, Manenti G, Manzoni L, Milani M, Moroni E, Perego P, Potenza D, Rizzo V, Scavullo C, Scolastico C, Servida F, Vasile F, Seneci P.

Bioorg Med Chem. 2012 Nov 15;20(22):6709-23. doi: 10.1016/j.bmc.2012.09.041. Epub 2012 Sep 24.

PMID:
23062821
2.

Homo- and heterodimeric Smac mimetics/IAP inhibitors as in vivo-active pro-apoptotic agents. Part I: Synthesis.

Manzoni L, Belvisi L, Bianchi A, Conti A, Drago C, de Matteo M, Ferrante L, Mastrangelo E, Perego P, Potenza D, Scolastico C, Servida F, Timpano G, Vasile F, Rizzo V, Seneci P.

Bioorg Med Chem. 2012 Nov 15;20(22):6687-708. doi: 10.1016/j.bmc.2012.09.020. Epub 2012 Sep 21.

PMID:
23036335
3.

A NMR and computational study of Smac mimics targeting both the BIR2 and BIR3 domains in XIAP protein.

Potenza D, Belvisi L, Vasile F, Moroni E, Cossu F, Seneci P.

Org Biomol Chem. 2012 Apr 28;10(16):3278-87. doi: 10.1039/c2ob06979b. Epub 2012 Mar 12.

PMID:
22407164
4.

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
5.

Discovery of a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer (AZD5582).

Hennessy EJ, Adam A, Aquila BM, Castriotta LM, Cook D, Hattersley M, Hird AW, Huntington C, Kamhi VM, Laing NM, Li D, MacIntyre T, Omer CA, Oza V, Patterson T, Repik G, Rooney MT, Saeh JC, Sha L, Vasbinder MM, Wang H, Whitston D.

J Med Chem. 2013 Dec 27;56(24):9897-919. doi: 10.1021/jm401075x. Epub 2013 Dec 13.

PMID:
24320998
6.

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
7.
8.

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
9.

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.

10.

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
11.

Design, synthesis and evaluation of inhibitor of apoptosis protein (IAP) antagonists that are highly selective for the BIR2 domain of XIAP.

Ardecky RJ, Welsh K, Finlay D, Lee PS, González-López M, Ganji SR, Ravanan P, Mace PD, Riedl SJ, Vuori K, Reed JC, Cosford ND.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4253-7. doi: 10.1016/j.bmcl.2013.04.096. Epub 2013 May 14.

12.

Targeting the X-linked inhibitor of apoptosis protein through 4-substituted azabicyclo[5.3.0]alkane smac mimetics. Structure, activity, and recognition principles.

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

J Mol Biol. 2008 Dec 19;384(3):673-89. doi: 10.1016/j.jmb.2008.09.064. Epub 2008 Oct 7.

PMID:
18851976
13.

Design of small-molecule Smac mimetics as IAP antagonists.

Wang S.

Curr Top Microbiol Immunol. 2011;348:89-113. doi: 10.1007/82_2010_111.

PMID:
21072626
14.

Recognition of Smac-mimetic compounds by the BIR domain of cIAP1.

Cossu F, Malvezzi F, Canevari G, Mastrangelo E, Lecis D, Delia D, Seneci P, Scolastico C, Bolognesi M, Milani M.

Protein Sci. 2010 Dec;19(12):2418-29. doi: 10.1002/pro.523.

15.

Design, synthesis, and characterization of a potent, nonpeptide, cell-permeable, bivalent Smac mimetic that concurrently targets both the BIR2 and BIR3 domains in XIAP.

Sun H, Nikolovska-Coleska Z, Lu J, Meagher JL, Yang CY, Qiu S, Tomita Y, Ueda Y, Jiang S, Krajewski K, Roller PP, Stuckey JA, Wang S.

J Am Chem Soc. 2007 Dec 12;129(49):15279-94. Epub 2007 Nov 14.

16.

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
17.

Theoretical studies on the interactions of XIAP-BIR3 domain with bicyclic and tricyclic core monovalent Smac mimetics.

Ling B, Dong L, Zhang R, Wang Z, Liu Y, Liu C.

J Mol Graph Model. 2010 Nov;29(3):354-62. doi: 10.1016/j.jmgm.2010.09.011. Epub 2010 Oct 25.

PMID:
20980180
18.
19.

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
20.

Smac mimetics as IAP antagonists.

Fulda S.

Semin Cell Dev Biol. 2015 Mar;39:132-8. doi: 10.1016/j.semcdb.2014.12.005. Epub 2014 Dec 27. Review.

PMID:
25550219

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