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Items: 47

1.

Inhibitor of intramembrane protease RseP blocks the σE response causing lethal accumulation of unfolded outer membrane proteins.

Konovalova A, Grabowicz M, Balibar CJ, Malinverni JC, Painter RE, Riley D, Mann PA, Wang H, Garlisi CG, Sherborne B, Rigel NW, Ricci DP, Black TA, Roemer T, Silhavy TJ, Walker SS.

Proc Natl Acad Sci U S A. 2018 Jul 10;115(28):E6614-E6621. doi: 10.1073/pnas.1806107115. Epub 2018 Jun 25.

2.

The synthesis of 2,3,6-trisubstituted 1-oxo-1,2-dihydroisoquinolines as potent CRTh2 antagonists.

Huang X, Rao A, Zhou W, Aslanian R, Nargund R, Buevich A, Zhang LK, Qiu H, Yang X, Garlisi CG, Correll C, Palani A.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5344-5348. doi: 10.1016/j.bmcl.2017.07.064. Epub 2017 Jul 25.

PMID:
29110986
3.

Discovery of 3-morpholino-imidazole[1,5-a]pyrazine BTK inhibitors for rheumatoid arthritis.

Boga SB, Alhassan AB, Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Zhu H, Desai J, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Cooper A, Kim RM, Kozlowski JA.

Bioorg Med Chem Lett. 2017 Aug 15;27(16):3939-3943. doi: 10.1016/j.bmcl.2017.03.040. Epub 2017 Mar 18.

PMID:
28720503
4.

Antibacterial small molecules targeting the conserved TOPRIM domain of DNA gyrase.

Walker SS, Labroli M, Painter RE, Wiltsie J, Sherborne B, Murgolo N, Sher X, Mann P, Zuck P, Garlisi CG, Su J, Kargman S, Xiao L, Scapin G, Salowe S, Devito K, Sheth P, Buist N, Tan CM, Black TA, Roemer T.

PLoS One. 2017 Jul 10;12(7):e0180965. doi: 10.1371/journal.pone.0180965. eCollection 2017.

5.

Can We Make Small Molecules Lean? Optimization of a Highly Lipophilic TarO Inhibitor.

Mandal M, Tan Z, Madsen-Duggan C, Buevich AV, Caldwell JP, Dejesus R, Flattery A, Garlisi CG, Gill C, Ha SN, Ho G, Koseoglu S, Labroli M, Basu K, Lee SH, Liang L, Liu J, Mayhood T, McGuinness D, McLaren DG, Wen X, Parmee E, Rindgen D, Roemer T, Sheth P, Tawa P, Tata J, Yang C, Yang SW, Xiao L, Wang H, Tan C, Tang H, Walsh P, Walsh E, Wu J, Su J.

J Med Chem. 2017 May 11;60(9):3851-3865. doi: 10.1021/acs.jmedchem.7b00113. Epub 2017 Mar 29.

PMID:
28322556
6.

Discovery of novel BTK inhibitors with carboxylic acids.

Gao X, Wang J, Liu J, Guiadeen D, Krikorian A, Boga SB, Alhassan AB, Selyutin O, Yu W, Yu Y, Anand R, Liu S, Yang C, Wu H, Cai J, Cooper A, Zhu H, Maloney K, Gao YD, Fischmann TO, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA.

Bioorg Med Chem Lett. 2017 Mar 15;27(6):1471-1477. doi: 10.1016/j.bmcl.2016.11.079. Epub 2016 Nov 25.

PMID:
28254166
7.

Benzimidazole analogs as WTA biosynthesis inhibitors targeting methicillin resistant Staphylococcus aureus.

Yang SW, Pan J, Yang C, Labroli M, Pan W, Caldwell J, Ha S, Koseoglu S, Xiao JC, Mayhood T, Sheth PR, Garlisi CG, Wu J, Lee SH, Wang H, Tan CM, Roemer T, Su J.

Bioorg Med Chem Lett. 2016 Oct 1;26(19):4743-4747. doi: 10.1016/j.bmcl.2016.08.036. Epub 2016 Aug 16.

PMID:
27575474
8.

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
9.

Discovery of potent wall teichoic acid early stage inhibitors.

Labroli MA, Caldwell JP, Yang C, Lee SH, Wang H, Koseoglu S, Mann P, Yang SW, Xiao J, Garlisi CG, Tan C, Roemer T, Su J.

Bioorg Med Chem Lett. 2016 Aug 15;26(16):3999-4002. doi: 10.1016/j.bmcl.2016.06.090. Epub 2016 Jun 30.

PMID:
27436582
10.

In Vitro and In Vivo Characterization of the Novel Oxabicyclooctane-Linked Bacterial Topoisomerase Inhibitor AM-8722, a Selective, Potent Inhibitor of Bacterial DNA Gyrase.

Tan CM, Gill CJ, Wu J, Toussaint N, Yin J, Tsuchiya T, Garlisi CG, Kaelin D, Meinke PT, Miesel L, Olsen DB, Lagrutta A, Fukuda H, Kishii R, Takei M, Oohata K, Takeuchi T, Shibue T, Takano H, Nishimura A, Fukuda Y, Singh SB.

Antimicrob Agents Chemother. 2016 Jul 22;60(8):4830-9. doi: 10.1128/AAC.00619-16. Print 2016 Aug.

11.

High-throughput screening of antibiotic-resistant bacteria in picodroplets.

Liu X, Painter RE, Enesa K, Holmes D, Whyte G, Garlisi CG, Monsma FJ, Rehak M, Craig FF, Smith CA.

Lab Chip. 2016 Apr 26;16(9):1636-43. doi: 10.1039/c6lc00180g.

PMID:
27033300
12.

Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.

Liu J, Guiadeen D, Krikorian A, Gao X, Wang J, Boga SB, Alhassan AB, Yu Y, Vaccaro H, Liu S, Yang C, Wu H, Cooper A, de Man J, Kaptein A, Maloney K, Hornak V, Gao YD, Fischmann TO, Raaijmakers H, Vu-Pham D, Presland J, Mansueto M, Xu Z, Leccese E, Zhang-Hoover J, Knemeyer I, Garlisi CG, Bays N, Stivers P, Brandish PE, Hicks A, Kim R, Kozlowski JA.

ACS Med Chem Lett. 2015 Dec 19;7(2):198-203. doi: 10.1021/acsmedchemlett.5b00463. eCollection 2016 Feb 11.

13.

TarO-specific inhibitors of wall teichoic acid biosynthesis restore β-lactam efficacy against methicillin-resistant staphylococci.

Lee SH, Wang H, Labroli M, Koseoglu S, Zuck P, Mayhood T, Gill C, Mann P, Sher X, Ha S, Yang SW, Mandal M, Yang C, Liang L, Tan Z, Tawa P, Hou Y, Kuvelkar R, DeVito K, Wen X, Xiao J, Batchlett M, Balibar CJ, Liu J, Xiao J, Murgolo N, Garlisi CG, Sheth PR, Flattery A, Su J, Tan C, Roemer T.

Sci Transl Med. 2016 Mar 9;8(329):329ra32. doi: 10.1126/scitranslmed.aad7364.

PMID:
26962156
14.

Chemical Genomics-Based Antifungal Drug Discovery: Targeting Glycosylphosphatidylinositol (GPI) Precursor Biosynthesis.

Mann PA, McLellan CA, Koseoglu S, Si Q, Kuzmin E, Flattery A, Harris G, Sher X, Murgolo N, Wang H, Devito K, de Pedro N, Genilloud O, Kahn JN, Jiang B, Costanzo M, Boone C, Garlisi CG, Lindquist S, Roemer T.

ACS Infect Dis. 2015 Jan 9;1(1):59-72. doi: 10.1021/id5000212. Epub 2014 Dec 12.

15.

Selective small-molecule inhibition of an RNA structural element.

Howe JA, Wang H, Fischmann TO, Balibar CJ, Xiao L, Galgoci AM, Malinverni JC, Mayhood T, Villafania A, Nahvi A, Murgolo N, Barbieri CM, Mann PA, Carr D, Xia E, Zuck P, Riley D, Painter RE, Walker SS, Sherborne B, de Jesus R, Pan W, Plotkin MA, Wu J, Rindgen D, Cummings J, Garlisi CG, Zhang R, Sheth PR, Gill CJ, Tang H, Roemer T.

Nature. 2015 Oct 29;526(7575):672-7. doi: 10.1038/nature15542. Epub 2015 Sep 30.

PMID:
26416753
16.

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.

17.

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
18.

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.

19.

Kibdelomycin is a bactericidal broad-spectrum aerobic antibacterial agent.

Singh SB, Dayananth P, Balibar CJ, Garlisi CG, Lu J, Kishii R, Takei M, Fukuda Y, Ha S, Young K.

Antimicrob Agents Chemother. 2015;59(6):3474-81. doi: 10.1128/AAC.00382-15. Epub 2015 Apr 6.

20.

Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.

Xiao D, Zhu X, Yu Y, Shao N, Wu J, McCormick KD, Dhondi P, Qin J, Mazzola R, Tang H, Rao A, Siliphaivanh P, Qiu H, Yang X, Rivelli M, Garlisi CG, Eckel S, Mukhopadhyay G, Correll C, Rindgen D, Aslanian R, Palani A.

Bioorg Med Chem Lett. 2014 Mar 15;24(6):1615-20. doi: 10.1016/j.bmcl.2014.01.043. Epub 2014 Feb 2.

PMID:
24556380
21.

Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 1.

Matasi JJ, Brumfield S, Tulshian D, Czarnecki M, Greenlee W, Garlisi CG, Qiu H, Devito K, Chen SC, Sun Y, Bertorelli R, Geiss W, Le VD, Martin GS, Vellekoop SA, Haber J, Allard ML.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3805-8. doi: 10.1016/j.bmcl.2011.04.034. Epub 2011 Apr 24.

PMID:
21570840
22.

The synthesis of substituted bipiperidine amide compounds as CCR3 ligands: antagonists versus agonists.

Ting PC, Umland SP, Aslanian R, Cao J, Garlisi CG, Huang Y, Jakway J, Liu Z, Shah H, Tian F, Wan Y, Shih NY.

Bioorg Med Chem Lett. 2005 Jun 15;15(12):3020-3.

PMID:
15908209
23.

The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists.

Ting PC, Lee JF, Wu J, Umland SP, Aslanian R, Cao J, Dong Y, Garlisi CG, Gilbert EJ, Huang Y, Jakway J, Kelly J, Liu Z, McCombie S, Shah H, Tian F, Wan Y, Shih NY.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1375-8.

PMID:
15713390
24.

Catalytic activity of human ADAM33.

Zou J, Zhu F, Liu J, Wang W, Zhang R, Garlisi CG, Liu YH, Wang S, Shah H, Wan Y, Umland SP.

J Biol Chem. 2004 Mar 12;279(11):9818-30. Epub 2003 Dec 15.

25.

Mouse ADAM33: two splice variants differ in protein maturation and localization.

Umland SP, Wan Y, Shah H, Garlisi CG, Devito KE, Braunschweiger K, Gheyas F, Del Mastro R.

Am J Respir Cell Mol Biol. 2004 Apr;30(4):530-9. Epub 2003 Sep 11.

PMID:
12972401
26.

Human ADAM33 messenger RNA expression profile and post-transcriptional regulation.

Umland SP, Garlisi CG, Shah H, Wan Y, Zou J, Devito KE, Huang WM, Gustafson EL, Ralston R.

Am J Respir Cell Mol Biol. 2003 Nov;29(5):571-82. Epub 2003 May 30.

PMID:
12777249
27.

Human ADAM33: protein maturation and localization.

Garlisi CG, Zou J, Devito KE, Tian F, Zhu FX, Liu J, Shah H, Wan Y, Motasim Billah M, Egan RW, Umland SP.

Biochem Biophys Res Commun. 2003 Jan 31;301(1):35-43.

PMID:
12535637
28.

Identification of full, partial and inverse CC chemokine receptor 3 agonists using [35S]GTPgammaS binding.

Wan Y, Jakway JP, Qiu H, Shah H, Garlisi CG, Tian F, Ting P, Hesk D, Egan RW, Billah MM, Umland SP.

Eur J Pharmacol. 2002 Dec 5;456(1-3):1-10.

PMID:
12450563
29.

Effect of anti-mIL-9 antibody on the development of pulmonary inflammation and airway hyperresponsiveness in allergic mice.

Kung TT, Luo B, Crawley Y, Garlisi CG, Devito K, Minnicozzi M, Egan RW, Kreutner W, Chapman RW.

Am J Respir Cell Mol Biol. 2001 Nov;25(5):600-5.

PMID:
11713102
30.

A unique mRNA initiated within a middle intron of WHSC1/MMSET encodes a DNA binding protein that suppresses human IL-5 transcription.

Garlisi CG, Uss AS, Xiao H, Tian F, Sheridan KE, Wang L, Motasim Billah M, Egan RW, Stranick KS, Umland SP.

Am J Respir Cell Mol Biol. 2001 Jan;24(1):90-98.

PMID:
11152655
31.

Receptor reserve analysis of the human CCR3 receptor in eosinophils and CCR3-transfected cells.

Umland SP, Wan Y, Shortall J, Shah H, Jakway J, Garlisi CG, Tian F, Egan RW, Billah MM.

J Leukoc Biol. 2000 Mar;67(3):441-7.

PMID:
10733106
32.

The assignment of chemokine-chemokine receptor pairs: TARC and MIP-1 beta are not ligands for human CC-chemokine receptor 8.

Garlisi CG, Xiao H, Tian F, Hedrick JA, Billah MM, Egan RW, Umland SP.

Eur J Immunol. 1999 Oct;29(10):3210-5.

33.
34.

IL-5 inhibition as a therapy for allergic disease.

Garlisi CG.

Pulm Pharmacol Ther. 1999;12(2):81-5. Review. No abstract available.

PMID:
10373386
35.

Effects of cyclosporin A and dinactin on T-cell proliferation, interleukin-5 production, and murine pulmonary inflammation.

Umland SP, Shah H, Jakway JP, Shortall J, Razac S, Garlisi CG, Falcone A, Kung TT, Stelts D, Hegde V, Patel M, Motasim Billah M, Egan RW.

Am J Respir Cell Mol Biol. 1999 Mar;20(3):481-92.

PMID:
10030847
36.

Effects of chronic anti-interleukin-5 monoclonal antibody treatment in a murine model of pulmonary inflammation.

Garlisi CG, Kung TT, Wang P, Minnicozzi M, Umland SP, Chapman RW, Stelts D, Crawley Y, Falcone A, Myers JG, Jones H, Billah MM, Kreutner W, Egan RW.

Am J Respir Cell Mol Biol. 1999 Feb;20(2):248-55.

PMID:
9922215
37.

Anti-inflammatory activity of inhaled mometasone furoate in allergic mice.

Chapman RW, Sehring SJ, Garlisi CG, Falcone A, Kung TT, Stelts D, Minnicozzi M, Jones H, Umland S, Egan RW, Kreutner W.

Arzneimittelforschung. 1998 Apr;48(4):384-91.

PMID:
9608881
38.

Eosinophils retain their granule major basic protein in a murine model of allergic pulmonary inflammation.

Stelts D, Egan RW, Falcone A, Garlisi CG, Gleich GJ, Kreutner W, Kung TT, Nahrebne DK, Chapman RW, Minnicozzi M.

Am J Respir Cell Mol Biol. 1998 Apr;18(4):463-70.

PMID:
9533933
39.

Airway eosinophils, T cells, Th2-type cytokine mRNA, and hyperreactivity in response to aerosol challenge of allergic mice with previously established pulmonary inflammation.

Garlisi CG, Falcone A, Hey JA, Paster TM, Fernandez X, Rizzo CA, Minnicozzi M, Jones H, Billah MM, Egan RW, Umland SP.

Am J Respir Cell Mol Biol. 1997 Nov;17(5):642-51.

PMID:
9374116
40.

T cells are the predominant source of interleukin-5 but not interleukin-4 mRNA expression in the lungs of antigen-challenged allergic mice.

Garlisi CG, Falcone A, Billah MM, Egan RW, Umland SP.

Am J Respir Cell Mol Biol. 1996 Sep;15(3):420-8.

PMID:
8810648
41.

sVCAM-1 levels after segmental antigen challenge correlate with eosinophil influx, IL-4 and IL-5 production, and the late phase response.

Zangrilli JG, Shaver JR, Cirelli RA, Cho SK, Garlisi CG, Falcone A, Cuss FM, Fish JE, Peters SP.

Am J Respir Crit Care Med. 1995 May;151(5):1346-53.

PMID:
7537586
42.

T cells are necessary for Th2 cytokine production and eosinophil accumulation in airways of antigen-challenged allergic mice.

Garlisi CG, Falcone A, Kung TT, Stelts D, Pennline KJ, Beavis AJ, Smith SR, Egan RW, Umland SP.

Clin Immunol Immunopathol. 1995 Apr;75(1):75-83.

PMID:
7533686
43.

IL-2 mRNA levels and degradation rates change with mode of stimulation and phorbol ester treatment of lymphocytes.

Bill O, Garlisi CG, Grove DS, Holt GE, Mastro AM.

Cytokine. 1994 Jan;6(1):102-10.

PMID:
8003628
44.

Cytokine gene expression in mice undergoing chronic graft-versus-host disease.

Garlisi CG, Pennline KJ, Smith SR, Siegel MI, Umland SP.

Mol Immunol. 1993 May;30(7):669-77.

PMID:
8487782
45.
46.
47.

Negative regulation of interleukin-2 production in primary lymphocytes by 12-O-tetradecanoylphorbol-13-acetate.

Mastro AM, Garlisi CG, Grove DS, Grier CE 3rd, Pishak SA.

Lymphokine Cytokine Res. 1991 Jun;10(3):153-64.

PMID:
1715761

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