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Items: 26

1.

A High-Throughput Time-Resolved Fluorescence Energy Transfer Assay to Screen for Modulators of RGS7/Gβ5/R7BP Complex.

Muntean BS, Patil DN, Madoux F, Fossetta J, Scampavia L, Spicer TP, Martemyanov KA.

Assay Drug Dev Technol. 2018 Apr;16(3):150-161. doi: 10.1089/adt.2017.839.

2.

Efforts towards the optimization of a bi-aryl class of potent IRAK4 inhibitors.

Hanisak J, Seganish WM, McElroy WT, Tang H, Zhang R, Tsui HC, Fischmann T, Tulshian D, Tata J, Sondey C, Devito K, Fossetta J, Garlisi CG, Lundell D, Niu X.

Bioorg Med Chem Lett. 2016 Sep 1;26(17):4250-5. doi: 10.1016/j.bmcl.2016.07.048. Epub 2016 Jul 22.

PMID:
27476420
3.

Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.

Seganish WM, Fischmann TO, Sherborne B, Matasi J, Lavey B, McElroy WT, Tulshian D, Tata J, Sondey C, Garlisi CG, Devito K, Fossetta J, Lundell D, Niu X.

ACS Med Chem Lett. 2015 Jul 12;6(8):942-7. doi: 10.1021/acsmedchemlett.5b00279. eCollection 2015 Aug 13.

4.

Initial optimization and series evolution of diaminopyrimidine inhibitors of interleukin-1 receptor associated kinase 4.

Seganish WM, McElroy WT, Herr RJ, Brumfield S, Greenlee WJ, Harding J, Komanduri V, Matasi J, Prakash KC, Tulshian D, Yang J, Yet L, Devito K, Fossetta J, Garlisi CG, Lundell D, Niu X, Sondey C.

Bioorg Med Chem Lett. 2015 Aug 15;25(16):3203-7. doi: 10.1016/j.bmcl.2015.05.097. Epub 2015 Jun 6.

PMID:
26115573
5.

Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation.

McElroy WT, Tan Z, Ho G, Paliwal S, Li G, Seganish WM, Tulshian D, Tata J, Fischmann TO, Sondey C, Bian H, Bober L, Jackson J, Garlisi CG, Devito K, Fossetta J, Lundell D, Niu X.

ACS Med Chem Lett. 2015 May 12;6(6):677-82. doi: 10.1021/acsmedchemlett.5b00106. eCollection 2015 Jun 11.

6.

Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.

Xiao D, Zhu X, Sofolarides M, Degrado S, Shao N, Rao A, Chen X, Aslanian R, Fossetta J, Tian F, Trivedi P, Lundell D, Palani A.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3609-13. doi: 10.1016/j.bmcl.2014.05.024. Epub 2014 May 16.

PMID:
24913714
7.

Conformation constraint of anilides enabling the discovery of tricyclic lactams as potent MK2 non-ATP competitive inhibitors.

Xiao D, Palani A, Huang X, Sofolarides M, Zhou W, Chen X, Aslanian R, Guo Z, Fossetta J, Tian F, Trivedi P, Spacciapoli P, Whitehurst CE, Lundell D.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3262-6. doi: 10.1016/j.bmcl.2013.03.109. Epub 2013 Apr 4.

PMID:
23602398
8.

Discovery of a Potent Dihydrooxadiazole Series of Non-ATP-Competitive MK2 (MAPKAPK2) Inhibitors.

Qin J, Dhondi P, Huang X, Aslanian R, Fossetta J, Tian F, Lundell D, Palani A.

ACS Med Chem Lett. 2011 Dec 23;3(2):100-5. doi: 10.1021/ml200238g. eCollection 2012 Feb 9.

9.

Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors.

Rao AU, Xiao D, Huang X, Zhou W, Fossetta J, Lundell D, Tian F, Trivedi P, Aslanian R, Palani A.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1068-72. doi: 10.1016/j.bmcl.2011.11.113. Epub 2011 Dec 6.

PMID:
22182499
10.

A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors.

Huang X, Zhu X, Chen X, Zhou W, Xiao D, Degrado S, Aslanian R, Fossetta J, Lundell D, Tian F, Trivedi P, Palani A.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):65-70. doi: 10.1016/j.bmcl.2011.11.074. Epub 2011 Nov 23.

PMID:
22169260
11.

3,4-Diamino-1,2,5-thiadiazole as potent and selective CXCR2 antagonists.

Biju P, Taveras AG, Yu Y, Zheng J, Hipkin RW, Fossetta J, Fan X, Fine J, Lundell D.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1434-7. doi: 10.1016/j.bmcl.2009.01.027. Epub 2009 Jan 15.

PMID:
19200721
12.

Synthesis and structure-activity relationships of heteroaryl substituted-3,4-diamino-3-cyclobut-3-ene-1,2-dione CXCR2/CXCR1 receptor antagonists.

Yu Y, Dwyer MP, Chao J, Aki C, Chao J, Purakkattle B, Rindgen D, Bond R, Mayer-Ezel R, Jakway J, Qiu H, Hipkin RW, Fossetta J, Gonsiorek W, Bian H, Fan X, Terminelli C, Fine J, Lundell D, Merritt JR, He Z, Lai G, Wu M, Taveras A.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1318-22. doi: 10.1016/j.bmcl.2008.01.024. Epub 2008 Jan 11.

PMID:
18242983
13.

3,4-Diamino-2,5-thiadiazole-1-oxides as potent CXCR2/CXCR1 antagonists.

Biju P, Taveras A, Yu Y, Zheng J, Chao J, Rindgen D, Jakway J, Hipkin RW, Fossetta J, Fan X, Fine J, Qiu H, Merritt JR, Baldwin JJ.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):228-31. Epub 2007 Oct 30.

PMID:
18006311
14.

Pharmacological characterization of Sch527123, a potent allosteric CXCR1/CXCR2 antagonist.

Gonsiorek W, Fan X, Hesk D, Fossetta J, Qiu H, Jakway J, Billah M, Dwyer M, Chao J, Deno G, Taveras A, Lundell DJ, Hipkin RW.

J Pharmacol Exp Ther. 2007 Aug;322(2):477-85. Epub 2007 May 11.

PMID:
17496166
15.

Discovery of 2-hydroxy-N,N-dimethyl-3-{2-[[(R)-1-(5- methylfuran-2-yl)propyl]amino]-3,4-dioxocyclobut-1-enylamino}benzamide (SCH 527123): a potent, orally bioavailable CXCR2/CXCR1 receptor antagonist.

Dwyer MP, Yu Y, Chao J, Aki C, Chao J, Biju P, Girijavallabhan V, Rindgen D, Bond R, Mayer-Ezel R, Jakway J, Hipkin RW, Fossetta J, Gonsiorek W, Bian H, Fan X, Terminelli C, Fine J, Lundell D, Merritt JR, Rokosz LL, Kaiser B, Li G, Wang W, Stauffer T, Ozgur L, Baldwin J, Taveras AG.

J Med Chem. 2006 Dec 28;49(26):7603-6.

PMID:
17181143
16.

Characterization of peripheral human cannabinoid receptor (hCB2) expression and pharmacology using a novel radioligand, [35S]Sch225336.

Gonsiorek W, Hesk D, Chen SC, Kinsley D, Fine JS, Jackson JV, Bober LA, Deno G, Bian H, Fossetta J, Lunn CA, Kozlowski JA, Lavey B, Piwinski J, Narula SK, Lundell DJ, Hipkin RW.

J Biol Chem. 2006 Sep 22;281(38):28143-51. Epub 2006 Jun 5.

17.

Pharmacological characterization of human S1P4 using a novel radioligand, [4,5-3H]-dihydrosphingosine-1-phosphate.

Fossetta J, Deno G, Gonsiorek W, Fan X, Lavey B, Das P, Lunn C, Zavodny PJ, Lundell D, Hipkin RW.

Br J Pharmacol. 2004 Jul;142(5):851-60. Epub 2004 Jun 14.

18.

Pharmacological analysis of calcium responses mediated by the human A3 adenosine receptor in monocyte-derived dendritic cells and recombinant cells.

Fossetta J, Jackson J, Deno G, Fan X, Du XK, Bober L, Soudé-Bermejo A, de Bouteiller O, Caux C, Lunn C, Lundell D, Palmer RK.

Mol Pharmacol. 2003 Feb;63(2):342-50.

PMID:
12527805
19.

Structural characterization of nitric oxide synthase isoforms reveals striking active-site conservation.

Fischmann TO, Hruza A, Niu XD, Fossetta JD, Lunn CA, Dolphin E, Prongay AJ, Reichert P, Lundell DJ, Narula SK, Weber PC.

Nat Struct Biol. 1999 Mar;6(3):233-42.

PMID:
10074942
20.

Purification and crystallization of a complex between human interferon gamma receptor (extracellular domain) and human interferon gamma.

Windsor WT, Walter LJ, Syto R, Fossetta J, Cook WJ, Nagabhushan TL, Walter MR.

Proteins. 1996 Sep;26(1):108-14.

PMID:
8880934
21.

Expression of human inducible nitric oxide synthase in Escherichia coli.

Fossetta JD, Niu XD, Lunn CA, Zavodny PJ, Narula SK, Lundell D.

FEBS Lett. 1996 Jan 29;379(2):135-8.

22.

A point mutation of human interferon gamma abolishes receptor recognition.

Lunn CA, Fossetta J, Dalgarno D, Murgolo N, Windsor W, Zavodny PJ, Narula SK, Lundell D.

Protein Eng. 1992 Apr;5(3):253-7.

PMID:
1409546
23.

A point mutation that decreases the thermal stability of human interferon gamma.

Lunn CA, Fossetta J, Murgolo N, Zavodny PJ, Lundell D, Narula SK.

Protein Eng. 1992 Apr;5(3):249-52.

PMID:
1409545
24.

The carboxyl-terminal region of human interferon gamma is important for biological activity: mutagenic and NMR analysis.

Lundell D, Lunn C, Dalgarno D, Fossetta J, Greenberg R, Reim R, Grace M, Narula S.

Protein Eng. 1991 Feb;4(3):335-41.

PMID:
1830392
25.

Exploiting the cell membrane for the production of heterologous proteins in Escherichia coli.

Lundell D, Lunn C, Greenberg R, Fossetta J, Narula S, Kastelein R, Van Kimmenade A.

Biotechnol Appl Biochem. 1990 Oct;12(5):567-78.

PMID:
2288714
26.

Cytoplasmic and periplasmic expression of a highly basic protein, human interleukin 4, in Escherichia coli.

Lundell D, Greenberg R, Alroy Y, Condon R, Fossetta JD, Gewain K, Kastelein R, Lunn CA, Reim R, Shah C, et al.

J Ind Microbiol. 1990 Jun;5(4):215-27.

PMID:
1366607

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