| Name | mcl 1 |
|---|---|
| Synonyms | Bcl 2 related protein EAT/mcl1; EAT; Induced myeloid leukemia cell differentiation protein Mcl 1; MCL 1; MCL1; MCL1L; MCL1S; Myeloid cell leukemia 1… |
| Name | biphenyl |
|---|---|
| CAS | 1,1′-biphenyl |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 18413764 | Huang S, Sinicrope FA: BH3 mimetic ABT-737 potentiates TRAIL-mediated apoptotic signaling by unsequestering Bim and Bak in human pancreatic cancer cells. Cancer Res. 2008 Apr 15;68(8):2944-51. Finally, Mcl-1 shRNA potentiated caspase-3 cleavage by ABT-737 and enhanced its cytotoxic effects. |
1(0,0,0,1) | Details |
| 18806758 | Vogler M, Dinsdale D, Dyer MJ, Cohen GM: Bcl-2 inhibitors: small molecules with a big impact on cancer therapy. Cell Death Differ. 2009 Mar;16(3):360-7. Epub 2008 Sep 19. Antiapoptotic Bcl-2 family members may be divided into two subclasses, one comprising Bcl-2, Bcl-X (L) and Bcl-w and the other Mcl-1 and Bcl2A1. |
1(0,0,0,1) | Details |
| 20023629 | Schwickart M, Huang X, Lill JR, Liu J, Ferrando R, French DM, Maecker H, O'Rourke K, Bazan F, Eastham-Anderson J, Yue P, Dornan D, Huang DC, Dixit VM: Deubiquitinase USP9X stabilizes MCL1 and promotes tumour cell survival. Nature. 2010 Jan 7;463(7277):103-7. Epub 2009 Dec 20. |
7(0,0,0,7) | Details |
| 18398104 | Kang MH, Wan Z, Kang YH, Sposto R, Reynolds CP: Mechanism of synergy of N-(4-hydroxyphenyl) retinamide and ABT-737 in acute lymphoblastic leukemia cell lines: Mcl-1 inactivation. J Natl Cancer Inst. 2008 Apr 16;100(8):580-95. Epub 2008 Apr 8. |
6(0,0,0,6) | Details |
| 19372561 | Hauck P, Chao BH, Litz J, Krystal GW: Alterations in the Noxa/Mcl-1 axis determine sensitivity of small cell lung cancer to the BH3 mimetic ABT-737. Mol Cancer Ther. 2009 Apr;8(4):883-92. |
5(0,0,0,5) | Details |
| 19088028 | Okumura K, Huang S, Sinicrope FA: Induction of Noxa sensitizes human colorectal cancer cells expressing Mcl-1 to the small-molecule Bcl-2/Bcl-xL inhibitor, ABT-737. Clin Cancer Res. 2008 Dec 15;14(24):8132-42. |
4(0,0,0,4) | Details |
| 19684859 | Keuling AM, Felton KE, Parker AA, Akbari M, Andrew SE, Tron VA: RNA silencing of Mcl-1 enhances ABT-737-mediated apoptosis in melanoma: role for a caspase-8-dependent pathway. PLoS One. 2009 Aug 17;4(8):e6651. |
4(0,0,0,4) | Details |
| 19097992 | Yang TM, Barbone D, Fennell DA, Broaddus VC: Bcl-2 family proteins contribute to apoptotic resistance in lung cancer multicellular spheroids. Am J Respir Cell Mol Biol. 2009 Jul;41(1):14-23. Epub 2008 Dec 18. When cells formed spheroids, antiapoptotic Bcl-2 increased, whereas antiapoptotic Mcl-1 decreased. |
3(0,0,0,3) | Details |
| 19805519 | Chen S, Dai Y, Pei XY, Grant S: Bim upregulation by histone deacetylase inhibitors mediates interactions with the Bcl-2 antagonist ABT-737: evidence for distinct roles for Bcl-2, Bcl-xL, and Mcl-1. Mol Cell Biol. 2009 Dec;29(23):6149-69. Epub 2009 Oct 5. |
3(0,0,0,3) | Details |
| 18663354 | Tagscherer KE, Fassl A, Campos B, Farhadi M, Kraemer A, Bock BC, Macher-Goeppinger S, Radlwimmer B, Wiestler OD, Herold-Mende C, Roth W: Apoptosis-based treatment of glioblastomas with ABT-737, a novel small molecule inhibitor of Bcl-2 family proteins. Oncogene. 2008 Nov 6;27(52):6646-56. Epub 2008 Jul 28. Downregulation of Mcl-1 and overexpression of Bcl-2 sensitized the cells to ABT-737-mediated apoptosis. |
2(0,0,0,2) | Details |
| 19737977 | Bray K, Chen HY, Karp CM, May M, Ganesan S, Karantza-Wadsworth V, DiPaola RS, White E: Bcl-2 modulation to activate apoptosis in prostate cancer. . Mol Cancer Res. 2009 Sep;7(9):1487-96. Epub 2009 Sep 8. Combining ABT-737 with agents that target Mcl-1 sensitized prostate cancer cell lines with an apoptotic block to cell death in vitro. |
2(0,0,0,2) | Details |
| 18987671 | Miller LA, Goldstein NB, Johannes WU, Walton CH, Fujita M, Norris DA, Shellman YG: BH3 mimetic ABT-737 and a proteasome inhibitor synergistically kill melanomas through Noxa-dependent apoptosis. J Invest Dermatol. 2009 Apr;129(4):964-71. Epub 2008 Nov 6. Furthermore, mechanistic analysis revealed that this combination treatment induced expression of the pro-apoptotic protein Noxa- and caspase-dependent degradation of the anti-apoptotic protein, Mcl-1. |
2(0,0,0,2) | Details |
| 19060243 | Whitecross KF, Alsop AE, Cluse LA, Wiegmans A, Banks KM, Coomans C, Peart MJ, Newbold A, Lindemann RK, Johnstone RW: Defining the target specificity of ABT-737 and synergistic antitumor activities in combination with histone deacetylase inhibitors. Blood. 2009 Feb 26;113(9):1982-91. Epub 2008 Dec 5. ABT-737 was ineffective against Emu-myc/Mcl-1 and Emu-myc/A1 cells either as a single agent or in combination with HDACi. |
2(0,0,0,2) | Details |
| 19228717 | Kang MH, Reynolds CP: Bcl-2 inhibitors: targeting mitochondrial apoptotic pathways in cancer therapy. Clin Cancer Res. 2009 Feb 15;15(4):1126-32. One pathway being targeted for antineoplastic therapy is the anti-apoptotic B-cell lymphoma-2 (Bcl-2) family of proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1, Bfl1/A-1, and Bcl-B) that bind to and inactivate BH3-domain pro-apoptotic proteins. |
2(0,0,0,2) | Details |
| 18949058 | Cragg MS, Jansen ES, Cook M, Harris C, Strasser A, Scott CL: Treatment of B-RAF mutant human tumor cells with a MEK inhibitor requires Bim and is enhanced by a BH3 mimetic. J Clin Invest. 2008 Nov;118(11):3651-9. Epub 2008 Oct 23. This treatment was successful because of both efficient antagonism of the prosurvival Bcl-2 family member Mcl-1 by Bim and inhibition of Bcl-2 and Bcl-x (L) by ABT-737. |
1(0,0,0,1) | Details |
| 19726685 | Lee EF, Czabotar PE, Yang H, Sleebs BE, Lessene G, Colman PM, Smith BJ, Fairlie WD: Conformational changes in Bcl-2 pro-survival proteins determine their capacity to bind ligands. J Biol Chem. 2009 Oct 30;284(44):30508-17. Epub 2009 Sep 2. Here we describe new structures of mutant BH3 peptides bound to Bcl-x (L) and Mcl-1. |
1(0,0,0,1) | Details |
| 19004807 | Mason KD, Vandenberg CJ, Scott CL, Wei AH, Cory S, Huang DC, Roberts AW: In vivo efficacy of the Bcl-2 antagonist ABT-737 against aggressive Myc-driven lymphomas. Proc Natl Acad Sci U S A. 2008 Nov 18;105(46):17961-6. Epub 2008 Nov 11. As a single agent, ABT-737 significantly prolonged the survival of mice transplanted with the myc/bcl-2 lymphomas but was ineffective for the myc lymphomas, probably because of the relatively higher Mcl-1 levels found in the latter. |
1(0,0,0,1) | Details |
| 18689543 | Stolz C, Hess G, Hahnel PS, Grabellus F, Hoffarth S, Schmid KW, Schuler M: Targeting Bcl-2 family proteins modulates the sensitivity of B-cell lymphoma to rituximab-induced apoptosis. Blood. 2008 Oct 15;112(8):3312-21. Epub 2008 Aug 8. B-NHL cells insensitive to rituximab-induced apoptosis exhibit increased endogenous expression of multiple antiapoptotic Bcl-2 family proteins, or activation of phosphatidylinositol-3-kinase signaling resulting in up-regulation of Mcl-1. |
1(0,0,0,1) | Details |
| 19839062 | Hikita H, Takehara T, Kodama T, Shimizu S, Hosui A, Miyagi T, Tatsumi T, Ishida H, Ohkawa K, Li W, Kanto T, Hiramatsu N, Hennighausen L, Yin XM, Hayashi N: BH3-only protein bid participates in the Bcl-2 network in healthy liver cells. Hepatology. 2009 Dec;50(6):1972-80. Hepatocyte-specific knockout (KO) of Bcl-xL leads to naturally-occurring apoptosis despite co-expression of Mcl-1, which shares a similar anti-apoptotic function. |
1(0,0,0,1) | Details |
| 18281560 | Hahm ER, Arlotti JA, Marynowski SW, Singh SV: Honokiol, a constituent of oriental medicinal herb magnolia officinalis, inhibits growth of PC-3 xenografts in vivo in association with apoptosis induction. Clin Cancer Res. 2008 Feb 15;14(4):1248-57. Honokiol-induced apoptosis correlated with induction of Bax, Bak, and Bad and a decrease in Bcl-xL and Mcl-1 protein levels. |
1(0,0,0,1) | Details |
| 18767026 | Azmi AS, Mohammad RM: Non-peptidic small molecule inhibitors against Bcl-2 for cancer therapy. J Cell Physiol. 2009 Jan;218(1):13-21. Cancer cells that are resistant to various anti-cancer drugs and treatment regimen are found to over express these Bcl-2 proteins such as Bcl-2, Bcl-X (L), Mcl-1, Bcl-w, and A1/Bfl1. |
1(0,0,0,1) | Details |
| 18028486 | Kuroda J, Kimura S, Andreeff M, Ashihara E, Kamitsuji Y, Yokota A, Kawata E, Takeuchi M, Tanaka R, Murotani Y, Matsumoto Y, Tanaka H, Strasser A, Taniwaki M, Maekawa T: ABT-737 is a useful component of combinatory chemotherapies for chronic myeloid leukaemias with diverse drug-resistance mechanisms. Br J Haematol. 2008 Jan;140(2):181-90. Epub 2007 Nov 20. The combination of homoharringtonine that reduces Mcl-1 enhanced the killing by ABT-737 strongly in Bcr-Abl (+) cells even with T315I mutation. |
1(0,0,0,1) | Details |
| 20038611 | High LM, Szymanska B, Wilczynska-Kalak U, Barber N, O'Brien R, Khaw SL, Vikstrom IB, Roberts AW, Lock RB: The Bcl-2 homology domain 3 mimetic ABT-737 targets the apoptotic machinery in acute lymphoblastic leukemia resulting in synergistic in vitro and in vivo interactions with established drugs. Mol Pharmacol. 2010 Mar;77(3):483-94. Epub 2009 Dec 28. Finally, we show that the combination of L-asparaginase (by specifically down-regulating Mcl-1 protein levels), topotecan (by activating p53 via DNA damage), and ABT-737 (by inhibiting antiapoptotic Bcl-2 family members) caused profound synergistic antileukemic efficacy both in vitro and in vivo. |
1(0,0,0,1) | Details |
| 19380879 | Gallenne T, Gautier F, Oliver L, Hervouet E, Noel B, Hickman JA, Geneste O, Cartron PF, Vallette FM, Manon S, Juin P: Bax activation by the BH3-only protein Puma promotes cell dependence on antiapoptotic Bcl-2 family members. J Cell Biol. 2009 Apr 20;185(2):279-90. Finally, endogenous Puma is involved in the apoptotic response of human colorectal cancer cells to the Bcl-2/Bcl-xL inhibitor ABT-737, even in conditions where the expression of Mcl-1 is down-regulated. |
1(0,0,0,1) | Details |
| 19008458 | Vogler M, Butterworth M, Majid A, Walewska RJ, Sun XM, Dyer MJ, Cohen GM: Concurrent up-regulation of BCL-XL and BCL2A1 induces approximately 1000-fold resistance to ABT-737 in chronic lymphocytic leukemia. Blood. 2009 Apr 30;113(18):4403-13. Epub 2008 Nov 13. In contrast to data from cell lines, ABT-737-induced apoptosis in CLL cells was largely MCL1-independent. |
1(0,0,0,1) | Details |
| 18451169 | Konopleva M, Watt J, Contractor R, Tsao T, Harris D, Estrov Z, Bornmann W, Kantarjian H, Viallet J, Samudio I, Andreeff M: Mechanisms of antileukemic activity of the novel Bcl-2 homology domain-3 mimetic GX15-070 (obatoclax). Cancer Res. 2008 May 1;68(9):3413-20. We show that obatoclax can promote the release of cytochrome c from isolated leukemia cell mitochondria and that apoptosis induced by this agent is preceded by the release of Bak from Mcl-1, liberation of Bim from both Bcl-2 and Mcl-1, and the formation of an active Bak/Bax complex. |
1(0,0,0,1) | Details |