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Designed BH3 peptides with high affinity and specificity for targeting Mcl-1 in cells.

Foight GW, Ryan JA, Gullá SV, Letai A, Keating AE.

ACS Chem Biol. 2014 Sep 19;9(9):1962-8. doi: 10.1021/cb500340w.


Myeloid cell leukemia-1 is an important apoptotic survival factor in triple-negative breast cancer.

Goodwin CM, Rossanese OW, Olejniczak ET, Fesik SW.

Cell Death Differ. 2015 Dec;22(12):2098-106. doi: 10.1038/cdd.2015.73.


In silico and in vitro elucidation of BH3 binding specificity toward Bcl-2.

London N, Gullá S, Keating AE, Schueler-Furman O.

Biochemistry. 2012 Jul 24;51(29):5841-50. doi: 10.1021/bi3003567.


Molecular dynamics study of segment peptides of Bax, Bim, and Mcl-1 BH3 domain of the apoptosis-regulating proteins bound to the anti-apoptotic Mcl-1 protein.

Zhao RN, Fan S, Han JG, Liu G.

J Biomol Struct Dyn. 2015;33(5):1067-81. doi: 10.1080/07391102.2014.929028.


Determinants of BH3 binding specificity for Mcl-1 versus Bcl-xL.

Dutta S, Gullá S, Chen TS, Fire E, Grant RA, Keating AE.

J Mol Biol. 2010 May 21;398(5):747-62. doi: 10.1016/j.jmb.2010.03.058.


Dual inhibition of Bcl-2 and Bcl-xL strikingly enhances PI3K inhibition-induced apoptosis in human myeloid leukemia cells through a GSK3- and Bim-dependent mechanism.

Rahmani M, Aust MM, Attkisson E, Williams DC Jr, Ferreira-Gonzalez A, Grant S.

Cancer Res. 2013 Feb 15;73(4):1340-51. doi: 10.1158/0008-5472.CAN-12-1365.


Molecular analysis of functional redundancy among anti-apoptotic Bcl-2 proteins and its role in cancer cell survival.

Eichhorn JM, Alford SE, Sakurikar N, Chambers TC.

Exp Cell Res. 2014 Apr 1;322(2):415-24. doi: 10.1016/j.yexcr.2014.02.010.


Differential targeting of prosurvival Bcl-2 proteins by their BH3-only ligands allows complementary apoptotic function.

Chen L, Willis SN, Wei A, Smith BJ, Fletcher JI, Hinds MG, Colman PM, Day CL, Adams JM, Huang DC.

Mol Cell. 2005 Feb 4;17(3):393-403.


A novel BH3 ligand that selectively targets Mcl-1 reveals that apoptosis can proceed without Mcl-1 degradation.

Lee EF, Czabotar PE, van Delft MF, Michalak EM, Boyle MJ, Willis SN, Puthalakath H, Bouillet P, Colman PM, Huang DC, Fairlie WD.

J Cell Biol. 2008 Jan 28;180(2):341-55. doi: 10.1083/jcb.200708096.


Identification of a novel Mcl-1 protein binding motif.

Placzek WJ, Sturlese M, Wu B, Cellitti JF, Wei J, Pellecchia M.

J Biol Chem. 2011 Nov 18;286(46):39829-35. doi: 10.1074/jbc.M111.305326.


Evaluation of diverse α/β-backbone patterns for functional α-helix mimicry: analogues of the Bim BH3 domain.

Boersma MD, Haase HS, Peterson-Kaufman KJ, Lee EF, Clarke OB, Colman PM, Smith BJ, Horne WS, Fairlie WD, Gellman SH.

J Am Chem Soc. 2012 Jan 11;134(1):315-23. doi: 10.1021/ja207148m.


Mcl-1-Bim complexes accommodate surprising point mutations via minor structural changes.

Fire E, Gullá SV, Grant RA, Keating AE.

Protein Sci. 2010 Mar;19(3):507-19. doi: 10.1002/pro.329.


A comparison of two strategies for affinity maturation of a BH3 peptide toward pro-survival Bcl-2 proteins.

Zhang S, Long A, Link AJ.

ACS Synth Biol. 2012 Mar 16;1(3):89-98. doi: 10.1021/sb200002m.


EGFR signaling defines Mcl⁻1 survival dependency in neuroblastoma.

Nalluri S, Peirce SK, Tanos R, Abdella HA, Karmali D, Hogarty MD, Goldsmith KC.

Cancer Biol Ther. 2015;16(2):276-86. doi: 10.1080/15384047.2014.1002333.


A novel BH3 mimetic efficiently induces apoptosis in melanoma cells through direct binding to anti-apoptotic Bcl-2 family proteins, including phosphorylated Mcl-1.

Liu Y, Xie M, Song T, Sheng H, Yu X, Zhang Z.

Pigment Cell Melanoma Res. 2015 Mar;28(2):161-70. doi: 10.1111/pcmr.12325.


Marinopyrrole derivatives with sulfide spacers as selective disruptors of Mcl-1 binding to pro-apoptotic protein Bim.

Cheng C, Liu Y, Balasis ME, Garner TP, Li J, Simmons NL, Berndt N, Song H, Pan L, Qin Y, Nicolaou KC, Gavathiotis E, Sebti SM, Li R.

Mar Drugs. 2014 Jul 29;12(8):4311-25. doi: 10.3390/md12084311.


Conformational changes in Bcl-2 pro-survival proteins determine their capacity to bind ligands.

Lee EF, Czabotar PE, Yang H, Sleebs BE, Lessene G, Colman PM, Smith BJ, Fairlie WD.

J Biol Chem. 2009 Oct 30;284(44):30508-17. doi: 10.1074/jbc.M109.040725.


Locating Herpesvirus Bcl-2 Homologs in the Specificity Landscape of Anti-Apoptotic Bcl-2 Proteins.

Foight GW, Keating AE.

J Mol Biol. 2015 Jul 31;427(15):2468-90. doi: 10.1016/j.jmb.2015.05.015.


BH3 domains other than Bim and Bid can directly activate Bax/Bak.

Du H, Wolf J, Schafer B, Moldoveanu T, Chipuk JE, Kuwana T.

J Biol Chem. 2011 Jan 7;286(1):491-501. doi: 10.1074/jbc.M110.167148.


PI3K/mTOR dual inhibitor NVP-BEZ235 decreases Mcl-1 expression and sensitizes ovarian carcinoma cells to Bcl-xL-targeting strategies, provided that Bim expression is induced.

Jebahi A, Villedieu M, Pétigny-Lechartier C, Brotin E, Louis MH, Abeilard E, Giffard F, Guercio M, Briand M, Gauduchon P, Lheureux S, Poulain L.

Cancer Lett. 2014 Jun 28;348(1-2):38-49. doi: 10.1016/j.canlet.2014.03.001.

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