Protein Information

Name caspase (protein family or complex)
Synonyms caspase; caspases

Compound Information

Name biphenyl
CAS 1,1′-biphenyl

Reference List

PubMed Abstract RScore(About this table)
19010845 Micha D, Cummings J, Shoemaker A, Elmore S, Foster K, Greaves M, Ward T, Rosenberg S, Dive C, Simpson K: Circulating biomarkers of cell death after treatment with the BH-3 mimetic ABT-737 in a preclinical model of small-cell lung cancer. Clin Cancer Res. 2008 Nov 15;14(22):7304-10.


Plasma collected before and 2 to 360 hours after treatment was analyzed by M30 (caspase-cleaved cytokeratin 18) and M65 (intact and cleaved cytokeratin 18) ELISA.
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19390557 Vogler M, Weber K, Dinsdale D, Schmitz I, Schulze-Osthoff K, Dyer MJ, Cohen GM: Different forms of cell death induced by putative BCL2 inhibitors. . Cell Death Differ. 2009 Jul;16(7):1030-9. Epub 2009 Apr 24.


Furthermore, investigations of the effects of these compounds in primary chronic lymphocytic leukemic cells showed that all compounds induced certain biochemical hallmarks of apoptosis, such as release of cytochrome c and caspase cleavage.
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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.


The expression of Bcl-2 family messenger RNAs was measured by real-time reverse transcription-polymerase chain reaction, and caspase activity was measured enzymatically.
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18309326 Vogler M, Dinsdale D, Sun XM, Young KW, Butterworth M, Nicotera P, Dyer MJ, Cohen GM: A novel paradigm for rapid ABT-737-induced apoptosis involving outer mitochondrial membrane rupture in primary leukemia and lymphoma cells. Cell Death Differ. 2008 May;15(5):820-30. Epub 2008 Feb 29.


Primary chronic lymphocytic leukemia (CLL) cells are exquisitely sensitive to ABT-737, a small molecule BCL2-antagonist, which induces many of the classical biochemical and ultrastructural features of apoptosis, including BAX/BAK oligomerization, cytochrome c release, caspase activation and chromatin condensation.
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19966836 Dai L, Ji H, Kong XW, Zhang YH: Antifibrotic effects of ZK14, a novel nitric oxide-donating biphenyldicarboxylate derivative, on rat HSC-T6 cells and CCl4-induced hepatic fibrosis. Acta Pharmacol Sin. 2010 Jan;31(1):27-34. Epub 2009 Dec 7.


Mitochondrial membrane potential (MMP) and caspase activities were tested.
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18588872 Liu H, Zang C, Emde A, Planas-Silva MD, Rosche M, Kuhnl A, Schulz CO, Elstner E, Possinger K, Eucker J: Anti-tumor effect of honokiol alone and in combination with other anti-cancer agents in breast cancer. Eur J Pharmacol. 2008 Sep 4;591(1-3):43-51. Epub 2008 Jun 12.


The inhibition of growth was associated with a G1-phase cell cycle arrest and induction of caspase-dependent apoptosis.
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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.
1(0,0,0,1) Details
19561125 Hermanson D, Addo SN, Bajer AA, Marchant JS, Das SG, Srinivasan B, Al-Mousa F, Michelangeli F, Thomas DD, Lebien TW, Xing C: Dual mechanisms of sHA 14-1 in inducing cell death through endoplasmic reticulum and mitochondria. Mol Pharmacol. 2009 Sep;76(3):667-78. Epub 2009 Jun 26.

Evaluation of the mitochondrial pathway showed that sHA 14-1 triggered a loss of mitochondrial transmembrane potential (Delta psi m) and weak caspase-9 activation, whereas thapsigargin had no effect. (R)-4-(3-Dimethylamino-1-phenylsulfanylmethyl-propylamino)-N-{4-[4-(4'-chl oro-biphenyl-2-ylmethyl)-piperazin-1-yl]-benzoyl}-3-nitrobenzenesulfonamid e (ABT-737), a well established small-molecule Bcl-2 antagonist, rapidly induced loss of Delta psi m and caspase-9 activation but had no effect on the ER.
The pan-caspase inhibitor N-benzyloxycarbonyl-Val-Ala-Asp-fluoromethyl ketone had some protective effect on sHA 14-1-induced cell death.
1(0,0,0,1) Details
19366808 Kurosu T, Ohki M, Wu N, Kagechika H, Miura O: Sorafenib induces apoptosis specifically in cells expressing BCR/ABL by inhibiting its kinase activity to activate the intrinsic mitochondrial pathway. Cancer Res. 2009 May 1;69(9):3927-36. Epub 2009 Apr 14.


Sorafenib-induced apoptosis in these cells and Ph+ leukemic cells was synergistically enhanced by rottlerin, bortezomib, or ABT-737 and inhibited by the pan-caspase inhibitor BOC-d-fmk or the overexpression of Bcl-XL.
1(0,0,0,1) Details
17762392 Kim BS, Bae E, Kim YJ, Ahn KS, Park J, Rhee JY, Lee YY, Kim Y, Lee D, Kim BK, Yoon SS: Combination of SK-7041, one of novel histone deacetylase inhibitors, and STI571-induced synergistic apoptosis in chronic myeloid leukemia. Anticancer Drugs. 2007 Jul;18(6):641-7.


SK-7041 exhibited growth inhibition of leukemia cells by downregulation of CDK4, cyclin E and cyclin B1 expression, and by upregulation of p21 expression with subsequent activation of the mitochondria-mediated caspase pathway.
1(0,0,0,1) Details
19135778 Park EJ, Min HY, Chung HJ, Hong JY, Kang YJ, Hung TM, Youn UJ, Kim YS, Bae K, Kang SS, Lee SK: Down-regulation of c-Src/EGFR-mediated signaling activation is involved in the honokiol-induced cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells. Cancer Lett. 2009 May 18;277(2):133-40. Epub 2009 Jan 9.


Apoptosis caused by honokiol was also concomitant with the cleavage of caspases (caspase-3, -8, and -9) and Bid along with the suppressive expression of Bcl-2, but it was independent on the expression of Bax and p53.
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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.


We find that rituximab directly triggers apoptosis via the mitochondrial pathway of caspase activation.
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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.


EXPERIMENTAL DESIGN: Human colorectal carcinoma cell lines (HCT116 wild-type and Bax (-/-), HT-29, and RKO) were incubated with ABT-737 alone and combined with CPT-11 or bortezomib, and cell viability, caspase cleavage, and Annexin V labeling were measured.
1(0,0,0,1) Details
19404643 Howard AN, Bridges KA, Meyn RE, Chandra J: ABT-737, a BH3 mimetic, induces glutathione depletion and oxidative stress. Cancer Chemother Pharmacol. 2009 Dec;65(1):41-54. Epub 2009 Apr 29.


GSH concentrations, intracellular reactive oxygen species (ROS), caspase activation and apoptotic DNA fragmentation were measured.
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