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Items: 1 to 20 of 185


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.


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.


Small-molecule SMAC mimetics as new cancer therapeutics.

Bai L, Smith DC, Wang S.

Pharmacol Ther. 2014 Oct;144(1):82-95. doi: 10.1016/j.pharmthera.2014.05.007. Epub 2014 May 16. Review.


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.


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.


Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.

Peng Y, Sun H, Lu J, Liu L, Cai Q, Shen R, Yang CY, Yi H, Wang S.

J Med Chem. 2012 Jan 12;55(1):106-14. doi: 10.1021/jm201072x. Epub 2011 Dec 7.


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.


Potent bivalent Smac mimetics: effect of the linker on binding to inhibitor of apoptosis proteins (IAPs) and anticancer activity.

Sun H, Liu L, Lu J, Bai L, Li X, Nikolovska-Coleska Z, McEachern D, Yang CY, Qiu S, Yi H, Sun D, Wang S.

J Med Chem. 2011 May 12;54(9):3306-18. doi: 10.1021/jm101651b. Epub 2011 Apr 13.


Cyclopeptide Smac mimetics as antagonists of IAP proteins.

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

Bioorg Med Chem Lett. 2010 May 15;20(10):3043-6.


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.


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.


Characterization of Potent SMAC Mimetics that Sensitize Cancer Cells to TNF Family-Induced Apoptosis.

Welsh K, Milutinovic S, Ardecky RJ, Gonzalez-Lopez M, Ganji SR, Teriete P, Finlay D, Riedl S, Matsuzawa S, Pinilla C, Houghten R, Vuori K, Reed JC, Cosford ND.

PLoS One. 2016 Sep 12;11(9):e0161952. doi: 10.1371/journal.pone.0161952. eCollection 2016.


SM-164: a novel, bivalent Smac mimetic that induces apoptosis and tumor regression by concurrent removal of the blockade of cIAP-1/2 and XIAP.

Lu J, Bai L, Sun H, Nikolovska-Coleska Z, McEachern D, Qiu S, Miller RS, Yi H, Shangary S, Sun Y, Meagher JL, Stuckey JA, Wang S.

Cancer Res. 2008 Nov 15;68(22):9384-93. doi: 10.1158/0008-5472.CAN-08-2655.


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.


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.


Novel second mitochondria-derived activator of caspases (Smac) mimetic compounds sensitize human leukemic cell lines to conventional chemotherapeutic drug-induced and death receptor-mediated apoptosis.

Servida F, Lecis D, Scavullo C, Drago C, Seneci P, Carlo-Stella C, Manzoni L, Polli E, Lambertenghi Deliliers G, Delia D, Onida F.

Invest New Drugs. 2011 Dec;29(6):1264-75. doi: 10.1007/s10637-010-9475-6. Epub 2010 Jul 8.


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.


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.


A Smac-mimetic sensitizes prostate cancer cells to TRAIL-induced apoptosis via modulating both IAPs and NF-kappaB.

Dai Y, Liu M, Tang W, Li Y, Lian J, Lawrence TS, Xu L.

BMC Cancer. 2009 Nov 6;9:392. doi: 10.1186/1471-2407-9-392.

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