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Going further than Lipinski's rule in drug design.

Walters WP.

Expert Opin Drug Discov. 2012 Feb;7(2):99-107. doi: 10.1517/17460441.2012.648612. Epub 2012 Jan 13. Review.


Separation of Betti Reaction Product Enantiomers: Absolute Configuration and Inhibition of Botulinum Neurotoxin A.

Cardellina JH 2nd, Vieira RC, Eccard V, Skerry J, Montgomery V, Campbell Y, Roxas-Duncan V, Leister W, Leclair CA, Maloney DJ, Padula D, Pescitelli G, Khavrutskii I, Hu X, Wallqvist A, Smith LA.

ACS Med Chem Lett. 2011 Mar 10;2(5):396-401.


Structural alert/reactive metabolite concept as applied in medicinal chemistry to mitigate the risk of idiosyncratic drug toxicity: a perspective based on the critical examination of trends in the top 200 drugs marketed in the United States.

Stepan AF, Walker DP, Bauman J, Price DA, Baillie TA, Kalgutkar AS, Aleo MD.

Chem Res Toxicol. 2011 Sep 19;24(9):1345-410. doi: 10.1021/tx200168d. Epub 2011 Jul 11. Review.


A survey of the anti-apoptotic Bcl-2 subfamily expression in cancer types provides a platform to predict the efficacy of Bcl-2 antagonists in cancer therapy.

Placzek WJ, Wei J, Kitada S, Zhai D, Reed JC, Pellecchia M.

Cell Death Dis. 2010 May 6;1:e40. doi: 10.1038/cddis.2010.18.


Mechanisms of chemical carcinogenicity and mutagenicity: a review with implications for predictive toxicology.

Benigni R, Bossa C.

Chem Rev. 2011 Apr 13;111(4):2507-36. doi: 10.1021/cr100222q. Epub 2011 Jan 25. Review. No abstract available.


3-Thiomorpholin-8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile (S1) based molecules as potent, dual inhibitors of B-cell lymphoma 2 (Bcl-2) and myeloid cell leukemia sequence 1 (Mcl-1): structure-based design and structure-activity relationship studies.

Zhang Z, Wu G, Xie F, Song T, Chang X.

J Med Chem. 2011 Feb 24;54(4):1101-5. doi: 10.1021/jm101181u. Epub 2011 Jan 14. Erratum in: J Med Chem. 2013 Nov 27;56(22):9366-7.


Mcl-1 stability determines mitotic cell fate of human multiple myeloma tumor cells treated with the kinesin spindle protein inhibitor ARRY-520.

Tunquist BJ, Woessner RD, Walker DH.

Mol Cancer Ther. 2010 Jul;9(7):2046-56. doi: 10.1158/1535-7163.MCT-10-0033. Epub 2010 Jun 22.


The MCL-1 BH3 helix is an exclusive MCL-1 inhibitor and apoptosis sensitizer.

Stewart ML, Fire E, Keating AE, Walensky LD.

Nat Chem Biol. 2010 Aug;6(8):595-601. doi: 10.1038/nchembio.391. Epub 2010 Jun 20.


MCL-1-dependent leukemia cells are more sensitive to chemotherapy than BCL-2-dependent counterparts.

Brunelle JK, Ryan J, Yecies D, Opferman JT, Letai A.

J Cell Biol. 2009 Nov 2;187(3):429-42. doi: 10.1083/jcb.200904049. Epub 2009 Oct 26.


Selective and brain penetrant neuropeptide y y2 receptor antagonists discovered by whole-cell high-throughput screening.

Brothers SP, Saldanha SA, Spicer TP, Cameron M, Mercer BA, Chase P, McDonald P, Wahlestedt C, Hodder PS.

Mol Pharmacol. 2010 Jan;77(1):46-57. doi: 10.1124/mol.109.058677. Epub 2009 Oct 16.


Different forms of cell death induced by putative BCL2 inhibitors.

Vogler M, Weber K, Dinsdale D, Schmitz I, Schulze-Osthoff K, Dyer MJ, Cohen GM.

Cell Death Differ. 2009 Jul;16(7):1030-9. doi: 10.1038/cdd.2009.48. Epub 2009 Apr 24.


Phase I study of obatoclax mesylate (GX15-070), a small molecule pan-Bcl-2 family antagonist, in patients with advanced chronic lymphocytic leukemia.

O'Brien SM, Claxton DF, Crump M, Faderl S, Kipps T, Keating MJ, Viallet J, Cheson BD.

Blood. 2009 Jan 8;113(2):299-305. doi: 10.1182/blood-2008-02-137943. Epub 2008 Oct 17.


Mechanisms of proteasome inhibitor action and resistance in cancer.

McConkey DJ, Zhu K.

Drug Resist Updat. 2008 Aug-Oct;11(4-5):164-79. doi: 10.1016/j.drup.2008.08.002. Epub 2008 Sep 24. Review.


Current trends in multiple myeloma management.

Redzepovic J, Weinmann G, Ott I, Gust R.

J Int Med Res. 2008 May-Jun;36(3):371-86. Review.


Mechanisms of antileukemic activity of the novel Bcl-2 homology domain-3 mimetic GX15-070 (obatoclax).

Konopleva M, Watt J, Contractor R, Tsao T, Harris D, Estrov Z, Bornmann W, Kantarjian H, Viallet J, Samudio I, Andreeff M.

Cancer Res. 2008 May 1;68(9):3413-20. doi: 10.1158/0008-5472.CAN-07-1919.


Downregulation of Mcl-1 potentiates HDACi-mediated apoptosis in leukemic cells.

Inoue S, Walewska R, Dyer MJ, Cohen GM.

Leukemia. 2008 Apr;22(4):819-25. doi: 10.1038/leu.2008.1. Epub 2008 Jan 31.


The challenge of drugging undruggable targets in cancer: lessons learned from targeting BCL-2 family members.

Verdine GL, Walensky LD.

Clin Cancer Res. 2007 Dec 15;13(24):7264-70. Review.


Cytochrome p450 and chemical toxicology.

Guengerich FP.

Chem Res Toxicol. 2008 Jan;21(1):70-83. Epub 2007 Dec 6. Review.


Mcl-1 is a relevant therapeutic target in acute and chronic lymphoid malignancies: down-regulation enhances rituximab-mediated apoptosis and complement-dependent cytotoxicity.

Hussain SR, Cheney CM, Johnson AJ, Lin TS, Grever MR, Caligiuri MA, Lucas DM, Byrd JC.

Clin Cancer Res. 2007 Apr 1;13(7):2144-50.


Programmed anuclear cell death delimits platelet life span.

Mason KD, Carpinelli MR, Fletcher JI, Collinge JE, Hilton AA, Ellis S, Kelly PN, Ekert PG, Metcalf D, Roberts AW, Huang DC, Kile BT.

Cell. 2007 Mar 23;128(6):1173-86.

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