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Items: 13

1.

Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.

McDaniel KF, Wang L, Soltwedel T, Fidanze SD, Hasvold LA, Liu D, Mantei RA, Pratt JK, Sheppard GS, Bui MH, Faivre EJ, Huang X, Li L, Lin X, Wang R, Warder SE, Wilcox D, Albert DH, Magoc TJ, Rajaraman G, Park CH, Hutchins CW, Shen JJ, Edalji RP, Sun CC, Martin R, Gao W, Wong S, Fang G, Elmore SW, Shen Y, Kati WM.

J Med Chem. 2017 Oct 26;60(20):8369-8384. doi: 10.1021/acs.jmedchem.7b00746. Epub 2017 Oct 12.

PMID:
28949521
2.

Vulnerability of Small-Cell Lung Cancer to Apoptosis Induced by the Combination of BET Bromodomain Proteins and BCL2 Inhibitors.

Lam LT, Lin X, Faivre EJ, Yang Z, Huang X, Wilcox DM, Bellin RJ, Jin S, Tahir SK, Mitten M, Magoc T, Bhathena A, Kati WM, Albert DH, Shen Y, Uziel T.

Mol Cancer Ther. 2017 Aug;16(8):1511-1520. doi: 10.1158/1535-7163.MCT-16-0459. Epub 2017 May 3.

3.

Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies.

Bui MH, Lin X, Albert DH, Li L, Lam LT, Faivre EJ, Warder SE, Huang X, Wilcox D, Donawho CK, Sheppard GS, Wang L, Fidanze S, Pratt JK, Liu D, Hasvold L, Uziel T, Lu X, Kohlhapp F, Fang G, Elmore SW, Rosenberg SH, McDaniel KF, Kati WM, Shen Y.

Cancer Res. 2017 Jun 1;77(11):2976-2989. doi: 10.1158/0008-5472.CAN-16-1793. Epub 2017 Apr 17.

4.

Exploitation of Castration-Resistant Prostate Cancer Transcription Factor Dependencies by the Novel BET Inhibitor ABBV-075.

Faivre EJ, Wilcox D, Lin X, Hessler P, Torrent M, He W, Uziel T, Albert DH, McDaniel K, Kati W, Shen Y.

Mol Cancer Res. 2017 Jan;15(1):35-44. doi: 10.1158/1541-7786.MCR-16-0221. Epub 2016 Oct 5.

5.

A gene-expression screen identifies a non-toxic sumoylation inhibitor that mimics SUMO-less human LRH-1 in liver.

Suzawa M, Miranda DA, Ramos KA, Ang KK, Faivre EJ, Wilson CG, Caboni L, Arkin MR, Kim YS, Fletterick RJ, Diaz A, Schneekloth JS, Ingraham HA.

Elife. 2015 Dec 11;4. pii: e09003. doi: 10.7554/eLife.09003.

6.

Eliminating SF-1 (NR5A1) sumoylation in vivo results in ectopic hedgehog signaling and disruption of endocrine development.

Lee FY, Faivre EJ, Suzawa M, Lontok E, Ebert D, Cai F, Belsham DD, Ingraham HA.

Dev Cell. 2011 Aug 16;21(2):315-27. doi: 10.1016/j.devcel.2011.06.028. Epub 2011 Aug 4.

7.

Scaffolding actions of membrane-associated progesterone receptors.

Hagan CR, Faivre EJ, Lange CA.

Steroids. 2009 Jul;74(7):568-72. doi: 10.1016/j.steroids.2008.12.004. Epub 2008 Dec 24. Review.

8.

Decreased recognition of SUMO-sensitive target genes following modification of SF-1 (NR5A1).

Campbell LA, Faivre EJ, Show MD, Ingraham JG, Flinders J, Gross JD, Ingraham HA.

Mol Cell Biol. 2008 Dec;28(24):7476-86. doi: 10.1128/MCB.00103-08. Epub 2008 Oct 6.

9.

Progesterone receptor rapid signaling mediates serine 345 phosphorylation and tethering to specificity protein 1 transcription factors.

Faivre EJ, Daniel AR, Hillard CJ, Lange CA.

Mol Endocrinol. 2008 Apr;22(4):823-37. doi: 10.1210/me.2007-0437. Epub 2008 Jan 17.

10.

Phosphorylation-dependent antagonism of sumoylation derepresses progesterone receptor action in breast cancer cells.

Daniel AR, Faivre EJ, Lange CA.

Mol Endocrinol. 2007 Dec;21(12):2890-906. Epub 2007 Aug 23.

PMID:
17717077
13.

Regulated association of protein kinase B/Akt with breast tumor kinase.

Zhang P, Ostrander JH, Faivre EJ, Olsen A, Fitzsimmons D, Lange CA.

J Biol Chem. 2005 Jan 21;280(3):1982-91. Epub 2004 Nov 10.

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