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Items: 1 to 20 of 102


Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.

González-López M, Welsh K, Finlay D, Ardecky RJ, Ganji SR, Su Y, Yuan H, Teriete P, Mace PD, Riedl SJ, Vuori K, Reed JC, Cosford ND.

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4332-6. doi: 10.1016/j.bmcl.2011.05.049. Epub 2011 May 24.


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.


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.


Rational design, synthesis and characterization of potent, non-peptidic Smac mimics/XIAP inhibitors as proapoptotic agents for cancer therapy.

Seneci P, Bianchi A, Battaglia C, Belvisi L, Bolognesi M, Caprini A, Cossu F, Franco Ed, Matteo Md, Delia D, Drago C, Khaled A, Lecis D, Manzoni L, Marizzoni M, Mastrangelo E, Milani M, Motto I, Moroni E, Potenza D, Rizzo V, Servida F, Turlizzi E, Varrone M, Vasile F, Scolastico C.

Bioorg Med Chem. 2009 Aug 15;17(16):5834-56. doi: 10.1016/j.bmc.2009.07.009. Epub 2009 Jul 10.


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.


Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).

Sun H, Stuckey JA, Nikolovska-Coleska Z, Qin D, Meagher JL, Qiu S, Lu J, Yang CY, Saito NG, Wang S.

J Med Chem. 2008 Nov 27;51(22):7169-80. doi: 10.1021/jm8006849.


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.


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.


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.


Smac mimetic Birinapant induces apoptosis and enhances TRAIL potency in inflammatory breast cancer cells in an IAP-dependent and TNF-α-independent mechanism.

Allensworth JL, Sauer SJ, Lyerly HK, Morse MA, Devi GR.

Breast Cancer Res Treat. 2013 Jan;137(2):359-71. doi: 10.1007/s10549-012-2352-6. Epub 2012 Dec 7.


Novel SMAC-mimetics synergistically stimulate melanoma cell death in combination with TRAIL and Bortezomib.

Lecis D, Drago C, Manzoni L, Seneci P, Scolastico C, Mastrangelo E, Bolognesi M, Anichini A, Kashkar H, Walczak H, Delia D.

Br J Cancer. 2010 Jun 8;102(12):1707-16. doi: 10.1038/sj.bjc.6605687. Epub 2010 May 11.


Design of small-molecule peptidic and nonpeptidic Smac mimetics.

Sun H, Nikolovska-Coleska Z, Yang CY, Qian D, Lu J, Qiu S, Bai L, Peng Y, Cai Q, Wang S.

Acc Chem Res. 2008 Oct;41(10):1264-77. doi: 10.1021/ar8000553.


Smac mimetics in combination with TRAIL selectively target cancer stem cells in nasopharyngeal carcinoma.

Wu MS, Wang GF, Zhao ZQ, Liang Y, Wang HB, Wu MY, Min P, Chen LZ, Feng QS, Bei JX, Zeng YX, Yang D.

Mol Cancer Ther. 2013 Sep;12(9):1728-37. doi: 10.1158/1535-7163.MCT-13-0017. Epub 2013 May 22.


Solid phase synthesis of Smac/DIABLO-derived peptides using a 'Safety-Catch' resin: identification of potent XIAP BIR3 antagonists.

Elsawy MA, Martin L, Tikhonova IG, Walker B.

Bioorg Med Chem. 2013 Sep 1;21(17):5004-11. doi: 10.1016/j.bmc.2013.06.055. Epub 2013 Jul 2.


A dimeric Smac/diablo peptide directly relieves caspase-3 inhibition by XIAP. Dynamic and cooperative regulation of XIAP by Smac/Diablo.

Gao Z, Tian Y, Wang J, Yin Q, Wu H, Li YM, Jiang X.

J Biol Chem. 2007 Oct 19;282(42):30718-27. Epub 2007 Aug 27.


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.


Effect of the XIAP inhibitor Embelin on TRAIL-induced apoptosis of pancreatic cancer cells.

Mori T, Doi R, Kida A, Nagai K, Kami K, Ito D, Toyoda E, Kawaguchi Y, Uemoto S.

J Surg Res. 2007 Oct;142(2):281-6. Epub 2007 Jul 19.


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.


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.

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