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Items: 46

1.

Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841).

Fensome A, Ambler CM, Arnold E, Banker ME, Brown MF, Chrencik J, Clark JD, Dowty ME, Efremov IV, Flick A, Gerstenberger BS, Gopalsamy A, Hayward MM, Hegen M, Hollingshead BD, Jussif J, Knafels JD, Limburg DC, Lin D, Lin TH, Pierce BS, Saiah E, Sharma R, Symanowicz PT, Telliez JB, Trujillo JI, Vajdos FF, Vincent F, Wan ZK, Xing L, Yang X, Yang X, Zhang L.

J Med Chem. 2018 Oct 11;61(19):8597-8612. doi: 10.1021/acs.jmedchem.8b00917. Epub 2018 Aug 16.

PMID:
30113844
2.

The Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a TYK2/JAK1 Inhibitor (PF-06700841) in Healthy Subjects and Patients With Plaque Psoriasis.

Banfield C, Scaramozza M, Zhang W, Kieras E, Page KM, Fensome A, Vincent M, Dowty ME, Goteti K, Winkle PJ, Peeva E.

J Clin Pharmacol. 2018 Apr;58(4):434-447. doi: 10.1002/jcph.1046. Epub 2017 Dec 21.

PMID:
29266308
3.

Roads and bats: a meta-analysis and review of the evidence on vehicle collisions and barrier effects.

Fensome AG, Mathews F.

Mamm Rev. 2016 Oct;46(4):311-323. Epub 2016 May 29. Review.

4.

Sympatric woodland Myotis bats form tight-knit social groups with exclusive roost home ranges.

August TA, Nunn MA, Fensome AG, Linton DM, Mathews F.

PLoS One. 2014 Oct 30;9(10):e112225. doi: 10.1371/journal.pone.0112225. eCollection 2014.

5.

ATP-mediated kinome selectivity: the missing link in understanding the contribution of individual JAK Kinase isoforms to cellular signaling.

Thorarensen A, Banker ME, Fensome A, Telliez JB, Juba B, Vincent F, Czerwinski RM, Casimiro-Garcia A.

ACS Chem Biol. 2014 Jul 18;9(7):1552-8. doi: 10.1021/cb5002125. Epub 2014 May 28.

PMID:
24814050
6.

Novel progesterone receptor modulators: 4-aryl-phenylsulfonamides.

McComas C, Cohen J, Huselton C, Marella M, Melenski E, Mugford C, Slayden O, Winneker R, Wrobel J, Yudt MR, Fensome A.

Bioorg Med Chem Lett. 2012 Dec 1;22(23):7119-22. doi: 10.1016/j.bmcl.2012.09.077. Epub 2012 Sep 29.

PMID:
23079530
7.

Discovery of novel selective norepinephrine inhibitors: 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxides (WYE-114152).

O'Neill DJ, Adedoyin A, Bray JA, Deecher DC, Fensome A, Goldberg JA, Harrison J, Leventhal L, Mann C, Mark L, Nogle L, Sullivan NR, Spangler TB, Terefenko EA, Trybulski EJ, Uveges AJ, Vu A, Whiteside GT, Zhang P.

J Med Chem. 2011 Oct 13;54(19):6824-31. doi: 10.1021/jm200733r. Epub 2011 Sep 14.

PMID:
21916421
8.

Discovery of a novel mechanism of steroid receptor antagonism: WAY-255348 modulates progesterone receptor cellular localization and promoter interactions.

Yudt MR, Russo LA, Berrodin TJ, Jelinsky SA, Ellis D, Cohen JC, Cooch N, Haglund E, Unwalla RJ, Fensome A, Wrobel J, Zhang Z, Nagpal S, Winneker RC.

Biochem Pharmacol. 2011 Dec 1;82(11):1709-19. doi: 10.1016/j.bcp.2011.08.006. Epub 2011 Aug 11.

PMID:
21854761
9.

Discovery of novel selective norepinephrine reuptake inhibitors: 4-[3-aryl-2,2-dioxido-2,1,3-benzothiadiazol-1(3H)-yl]-1-(methylamino)butan-2-ols (WYE-103231).

O'Neill DJ, Adedoyin A, Alfinito PD, Bray JA, Cosmi S, Deecher DC, Fensome A, Harrison J, Leventhal L, Mann C, McComas CC, Sullivan NR, Spangler TB, Uveges AJ, Trybulski EJ, Whiteside GT, Zhang P.

J Med Chem. 2010 Jun 10;53(11):4511-21. doi: 10.1021/jm100053t.

PMID:
20462211
10.

Structure-activity relationships of norepinephrine reuptake inhibitors with benzothiadiazine dioxide or dihydrosulfostyril cores.

Fensome A, Goldberg J, McComas CC, Trybulski EJ, Woodworth RP, Deecher DC, Whiteside GT, Zhang P.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1555-8. doi: 10.1016/j.bmcl.2010.01.056. Epub 2010 Jan 20.

PMID:
20153188
11.

Selective Kv1.5 blockers: development of (R)-1-(methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a potential treatment for atrial arrhythmia.

Blass BE, Fensome A, Trybulski E, Magolda R, Gardell SJ, Liu K, Samuel M, Feingold I, Huselton C, Jackson CM, Djandjighian L, Ho D, Hennan J, Janusz JM.

J Med Chem. 2009 Nov 12;52(21):6531-4. doi: 10.1021/jm901042m.

PMID:
19888755
12.

1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: potent, selective, and orally efficacious norepinephrine reuptake inhibitors.

Zhang P, Terefenko EA, Bray J, Deecher D, Fensome A, Harrison J, Kim C, Koury E, Mark L, McComas CC, Mugford CA, Trybulski EJ, Vu AT, Whiteside GT, Mahaney PE.

J Med Chem. 2009 Sep 24;52(18):5703-11. doi: 10.1021/jm900888c.

PMID:
19722525
13.

Synthesis and activity of 1-(3-amino-1-phenylpropyl)indolin-2-ones: a new class of selective norepinephrine reuptake inhibitors.

McComas CC, Vu AT, Mahaney PE, Cohn ST, Fensome A, Marella MA, Nogle L, Trybulski EJ, Ye F, Zhang P, Alfinito P, Bray J, Johnston G, Koury E, Deecher DC.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):4929-31. doi: 10.1016/j.bmcl.2008.08.060. Epub 2008 Aug 22.

PMID:
18771916
14.

1,5-Dihydro-benzo[e][1,4]oxazepin-2(1H)-ones containing a 7-(5'-cyanopyrrol-2-yl) group as nonsteroidal progesterone receptor modulators.

Kern JC, Terefenko EA, Fensome A, Unwalla R, Wrobel J, Cohen J, Zhu Y, Berrodin TJ, Yudt MR, Winneker RC, Zhang Z, Zhang P.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5015-7. doi: 10.1016/j.bmcl.2008.08.015. Epub 2008 Aug 9.

PMID:
18722119
15.

In vitro and in vivo characterization of a novel nonsteroidal, species-specific progesterone receptor modulator, PRA-910.

Zhang Z, Lundeen SG, Slayden O, Zhu Y, Cohen J, Berrodin TJ, Bretz J, Chippari S, Wrobel J, Zhang P, Fensome A, Winneker RC, Yudt MR.

Ernst Schering Found Symp Proc. 2007;(1):171-97.

PMID:
18540573
16.

7-aryl 1,5-dihydro-benzo[e][1,4]oxazepin-2-ones and analogs as non-steroidal progesterone receptor antagonists.

Zhang P, Kern JC, Terefenko EA, Fensome A, Unwalla R, Zhang Z, Cohen J, Berrodin TJ, Yudt MR, Winneker RC, Wrobel J.

Bioorg Med Chem. 2008 Jul 1;16(13):6589-600. doi: 10.1016/j.bmc.2008.05.018. Epub 2008 May 10.

PMID:
18504132
17.

A new generation of progesterone receptor modulators.

Winneker RC, Fensome A, Zhang P, Yudt MR, McComas CC, Unwalla RJ.

Steroids. 2008 Aug;73(7):689-701. doi: 10.1016/j.steroids.2008.03.005. Epub 2008 Mar 28. Review.

PMID:
18472121
18.

Design, synthesis, and SAR of new pyrrole-oxindole progesterone receptor modulators leading to 5-(7-fluoro-3,3-dimethyl-2-oxo-2,3-dihydro-1H-indol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile (WAY-255348).

Fensome A, Adams WR, Adams AL, Berrodin TJ, Cohen J, Huselton C, Illenberger A, Kern JC, Hudak VA, Marella MA, Melenski EG, McComas CC, Mugford CA, Slayden OD, Yudt M, Zhang Z, Zhang P, Zhu Y, Winneker RC, Wrobel JE.

J Med Chem. 2008 Mar 27;51(6):1861-73. doi: 10.1021/jm701080t. Epub 2008 Mar 5.

PMID:
18318463
19.

5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.

Zhang P, Terefenko E, Kern J, Fensome A, Trybulski E, Unwalla R, Wrobel J, Lockhead S, Zhu Y, Cohen J, Lacava M, Winneker RC, Zhang Z.

Bioorg Med Chem. 2007 Oct 15;15(20):6556-64. Epub 2007 Jul 26.

PMID:
17681796
20.

SAR studies of 6-(arylamino)-4,4-disubstituted-1-methyl-1,4-dihydro-benzo[d][1,3]oxazin-2-ones as progesterone receptor antagonists.

Kern JC, Terefenko EA, Fensome A, Unwallla R, Wrobel J, Zhu Y, Cohen J, Winneker R, Zhang Z, Zhang P.

Bioorg Med Chem Lett. 2007 Jan 1;17(1):189-92. Epub 2006 Oct 5.

PMID:
17027272
21.

Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget.

Fensome A, Bender R, Chopra R, Cohen J, Collins MA, Hudak V, Malakian K, Lockhead S, Olland A, Svenson K, Terefenko EA, Unwalla RJ, Wilhelm JM, Wolfrom S, Zhu Y, Zhang Z, Zhang P, Winneker RC, Wrobel J.

J Med Chem. 2005 Aug 11;48(16):5092-5.

PMID:
16078826
22.

SAR studies of 6-aryl-1,3-dihydrobenzimidazol-2-ones as progesterone receptor antagonists.

Terefenko EA, Kern J, Fensome A, Wrobel J, Zhu Y, Cohen J, Winneker R, Zhang Z, Zhang P.

Bioorg Med Chem Lett. 2005 Aug 1;15(15):3600-3.

PMID:
15978807
23.

Molecular and pharmacological properties of a potent and selective novel nonsteroidal progesterone receptor agonist tanaproget.

Zhang Z, Olland AM, Zhu Y, Cohen J, Berrodin T, Chippari S, Appavu C, Li S, Wilhem J, Chopra R, Fensome A, Zhang P, Wrobel J, Unwalla RJ, Lyttle CR, Winneker RC.

J Biol Chem. 2005 Aug 5;280(31):28468-75. Epub 2005 Jun 3.

24.

Nonsteroidal progesterone receptor modulators: structure activity relationships.

Winneker RC, Fensome A, Wrobel JE, Zhang Z, Zhang P.

Semin Reprod Med. 2005 Feb;23(1):46-57. Review.

PMID:
15714389
25.

Novel pyrrole-containing progesterone receptor modulators.

Collins MA, Hudak V, Bender R, Fensome A, Zhang P, Miller L, Winneker RC, Zhang Z, Zhu Y, Cohen J, Unwalla RJ, Wrobel J.

Bioorg Med Chem Lett. 2004 May 3;14(9):2185-9.

PMID:
15081005
26.

Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.

Fensome A, Koko M, Wrobel J, Zhang P, Zhang Z, Cohen J, Lundeen S, Rudnick K, Zhu Y, Winneker R.

Bioorg Med Chem Lett. 2003 Apr 7;13(7):1317-20.

PMID:
12657272
27.

Novel 6-aryl-1,4-dihydrobenzo[d]oxazine-2-thiones as potent, selective, and orally active nonsteroidal progesterone receptor agonists.

Zhang P, Terefenko EA, Fensome A, Wrobel J, Winneker R, Zhang Z.

Bioorg Med Chem Lett. 2003 Apr 7;13(7):1313-6.

PMID:
12657271
28.

New progesterone receptor antagonists: 3,3-disubstituted-5-aryloxindoles.

Fensome A, Bender R, Cohen J, Collins MA, Mackner VA, Miller LL, Ullrich JW, Winneker R, Wrobel J, Zhang P, Zhang Z, Zhu Y.

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3487-90.

PMID:
12419390
29.

Continual production of phosphatidic acid by phospholipase D is essential for antigen-stimulated membrane ruffling in cultured mast cells.

O'Luanaigh N, Pardo R, Fensome A, Allen-Baume V, Jones D, Holt MR, Cockcroft S.

Mol Biol Cell. 2002 Oct;13(10):3730-46.

30.

6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.

Zhang P, Terefenko EA, Fensome A, Wrobel J, Winneker R, Lundeen S, Marschke KB, Zhang Z.

J Med Chem. 2002 Sep 26;45(20):4379-82.

PMID:
12238914
31.

Signalling role for ARF and phospholipase D in mast cell exocytosis stimulated by crosslinking of the high affinity FcepsilonR1 receptor.

Cockcroft S, Way G, O'Luanaigh N, Pardo R, Sarri E, Fensome A.

Mol Immunol. 2002 Sep;38(16-18):1277-82. Review.

PMID:
12217395
33.

Potent nonsteroidal progesterone receptor agonists: synthesis and SAR study of 6-aryl benzoxazines.

Zhang P, Terefenko EA, Fensome A, Zhang Z, Zhu Y, Cohen J, Winneker R, Wrobel J, Yardley J.

Bioorg Med Chem Lett. 2002 Mar 11;12(5):787-90.

PMID:
11859003
34.

Real time fluorescence imaging of PLC gamma translocation and its interaction with the epidermal growth factor receptor.

Matsuda M, Paterson HF, Rodriguez R, Fensome AC, Ellis MV, Swann K, Katan M.

J Cell Biol. 2001 Apr 30;153(3):599-612.

36.

A neutral magnesium-dependent sphingomyelinase isoform associated with intracellular membranes and reversibly inhibited by reactive oxygen species.

Fensome AC, Rodrigues-Lima F, Josephs M, Paterson HF, Katan M.

J Biol Chem. 2000 Jan 14;275(2):1128-36.

38.

ADP-ribosylation factor and Rho proteins mediate fMLP-dependent activation of phospholipase D in human neutrophils.

Fensome A, Whatmore J, Morgan C, Jones D, Cockcroft S.

J Biol Chem. 1998 May 22;273(21):13157-64.

39.

Phosphatidylinositol transfer proteins: an essential requirement in inositol lipid signalling.

Cockcroft S, Ball A, Fensome A, Hara S, Jones D, Prosser S, Swigart P.

Biochem Soc Trans. 1997 Nov;25(4):1125-31. Review. No abstract available.

PMID:
9449961
40.

ARF and PITP restore GTP gamma S-stimulated protein secretion from cytosol-depleted HL60 cells by promoting PIP2 synthesis.

Fensome A, Cunningham E, Prosser S, Tan SK, Swigart P, Thomas G, Hsuan J, Cockcroft S.

Curr Biol. 1996 Jun 1;6(6):730-8.

41.

The structure of rat ADP-ribosylation factor-1 (ARF-1) complexed to GDP determined from two different crystal forms.

Greasley SE, Jhoti H, Teahan C, Solari R, Fensome A, Thomas GM, Cockcroft S, Bax B.

Nat Struct Biol. 1995 Sep;2(9):797-806.

PMID:
7552752
42.

Crystallization and preliminary X-ray diffraction studies on ADP-ribosylation factor 1.

Greasley S, Jhoti H, Fensome AC, Cockcroft S, Thomas GM, Bax B.

J Mol Biol. 1994 Dec 16;244(5):651-3.

PMID:
7990146
44.

Phospholipase D: a downstream effector of ARF in granulocytes.

Cockcroft S, Thomas GM, Fensome A, Geny B, Cunningham E, Gout I, Hiles I, Totty NF, Truong O, Hsuan JJ.

Science. 1994 Jan 28;263(5146):523-6.

PMID:
8290961
45.

An essential role for phosphatidylinositol transfer protein in phospholipase C-mediated inositol lipid signaling.

Thomas GM, Cunningham E, Fensome A, Ball A, Totty NF, Truong O, Hsuan JJ, Cockcroft S.

Cell. 1993 Sep 10;74(5):919-28.

PMID:
8374957

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