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Items: 1 to 50 of 64

1.

Discovery of N-[Bis(4-methoxyphenyl)methyl]-4-hydroxy-2-(pyridazin-3-yl)pyrimidine-5-carboxamide (MK-8617), an Orally Active Pan-Inhibitor of Hypoxia-Inducible Factor Prolyl Hydroxylase 1-3 (HIF PHD1-3) for the Treatment of Anemia.

Debenham JS, Madsen-Duggan C, Clements MJ, Walsh TF, Kuethe JT, Reibarkh M, Salowe SP, Sonatore LM, Hajdu R, Milligan JA, Visco DM, Zhou D, Lingham RB, Stickens D, DeMartino JA, Tong X, Wolff M, Pang J, Miller RR, Sherer EC, Hale JJ.

J Med Chem. 2016 Dec 22;59(24):11039-11049. doi: 10.1021/acs.jmedchem.6b01242. Epub 2016 Nov 30.

PMID:
28002958
2.

Pharmacological Characterization of a Novel Beta 3 Adrenergic Agonist, Vibegron: Evaluation of Antimuscarinic Receptor Selectivity for Combination Therapy for Overactive Bladder.

Di Salvo J, Nagabukuro H, Wickham LA, Abbadie C, DeMartino JA, Fitzmaurice A, Gichuru L, Kulick A, Donnelly MJ, Jochnowitz N, Hurley AL, Pereira A, Sanfiz A, Veronin G, Villa K, Woods J, Zamlynny B, Zycband E, Salituro GM, Frenkl T, Weber AE, Edmondson SD, Struthers M.

J Pharmacol Exp Ther. 2017 Feb;360(2):346-355. doi: 10.1124/jpet.116.237313. Epub 2016 Dec 13.

PMID:
27965369
3.

Assessment of Brd4 inhibition in idiopathic pulmonary fibrosis lung fibroblasts and in vivo models of lung fibrosis.

Tang X, Peng R, Phillips JE, Deguzman J, Ren Y, Apparsundaram S, Luo Q, Bauer CM, Fuentes ME, DeMartino JA, Tyagi G, Garrido R, Hogaboam CM, Denton CP, Holmes AM, Kitson C, Stevenson CS, Budd DC.

Am J Pathol. 2013 Aug;183(2):470-9. doi: 10.1016/j.ajpath.2013.04.020. Epub 2013 Jun 10.

4.

Development of a pharmacodynamic assay based on PLCγ2 phosphorylation for quantifying spleen tyrosine kinase (SYK)-Bruton's tyrosine kinase (BTK) signaling.

Hsu J, Zhang J, Kitson C, Tan SL, Narula S, DeMartino JA, Liao C.

J Biomol Screen. 2013 Sep;18(8):890-8. doi: 10.1177/1087057113489881. Epub 2013 May 23.

PMID:
23704133
5.

Targeting the SYK-BTK axis for the treatment of immunological and hematological disorders: recent progress and therapeutic perspectives.

Tan SL, Liao C, Lucas MC, Stevenson C, DeMartino JA.

Pharmacol Ther. 2013 May;138(2):294-309. doi: 10.1016/j.pharmthera.2013.02.001. Epub 2013 Feb 7. Review.

PMID:
23396081
6.

Characterization of a novel CRAC inhibitor that potently blocks human T cell activation and effector functions.

Chen G, Panicker S, Lau KY, Apparsundaram S, Patel VA, Chen SL, Soto R, Jung JK, Ravindran P, Okuhara D, Bohnert G, Che Q, Rao PE, Allard JD, Badi L, Bitter HM, Nunn PA, Narula SK, DeMartino JA.

Mol Immunol. 2013 Jul;54(3-4):355-67. doi: 10.1016/j.molimm.2012.12.011. Epub 2013 Jan 26.

PMID:
23357789
7.

Bruton's Tyrosine Kinase mediates platelet receptor-induced generation of microparticles: a potential mechanism for amplification of inflammatory responses in rheumatoid arthritis synovial joints.

Hsu J, Gu Y, Tan SL, Narula S, DeMartino JA, Liao C.

Immunol Lett. 2013 Feb;150(1-2):97-104. doi: 10.1016/j.imlet.2012.12.007. Epub 2012 Dec 21.

PMID:
23266841
8.

Evidence for cyclic diguanylate as a vaccine adjuvant with novel immunostimulatory activities.

Gray PM, Forrest G, Wisniewski T, Porter G, Freed DC, DeMartino JA, Zaller DM, Guo Z, Leone J, Fu TM, Vora KA.

Cell Immunol. 2012 Jul-Aug;278(1-2):113-9. doi: 10.1016/j.cellimm.2012.07.006. Epub 2012 Aug 4.

PMID:
23121983
9.

BET bromodomain proteins mediate downstream signaling events following growth factor stimulation in human lung fibroblasts and are involved in bleomycin-induced pulmonary fibrosis.

Tang X, Peng R, Ren Y, Apparsundaram S, Deguzman J, Bauer CM, Hoffman AF, Hamilton S, Liang Z, Zeng H, Fuentes ME, Demartino JA, Kitson C, Stevenson CS, Budd DC.

Mol Pharmacol. 2013 Jan;83(1):283-93. doi: 10.1124/mol.112.081661. Epub 2012 Oct 31.

PMID:
23115324
10.

1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia.

Vachal P, Miao S, Pierce JM, Guiadeen D, Colandrea VJ, Wyvratt MJ, Salowe SP, Sonatore LM, Milligan JA, Hajdu R, Gollapudi A, Keohane CA, Lingham RB, Mandala SM, DeMartino JA, Tong X, Wolff M, Steinhuebel D, Kieczykowski GR, Fleitz FJ, Chapman K, Athanasopoulos J, Adam G, Akyuz CD, Jena DK, Lusen JW, Meng J, Stein BD, Xia L, Sherer EC, Hale JJ.

J Med Chem. 2012 Apr 12;55(7):2945-59. doi: 10.1021/jm201542d. Epub 2012 Feb 27.

PMID:
22364528
11.

Dual targeting of CCR2 and CX3CR1 in an arterial injury model of vascular inflammation.

Jerath MR, Liu P, Struthers M, Demartino JA, Peng R, Peterson LB, Cumiskey AM, Yang L, Rojas M, Patel DD, Fong AM.

Thromb J. 2010 Sep 13;8:14. doi: 10.1186/1477-9560-8-14.

12.

Assessment of chemokine receptor function on monocytes in whole blood: In vitro and ex vivo evaluations of a CCR2 antagonist.

Wisniewski T, Bayne E, Flanagan J, Shao Q, Wnek R, Matheravidathu S, Fischer P, Forrest MJ, Peterson L, Song X, Yang L, Demartino JA, Struthers M.

J Immunol Methods. 2010 Jan 31;352(1-2):101-10. doi: 10.1016/j.jim.2009.10.010. Epub 2009 Nov 10.

PMID:
19913021
13.

Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.

Kothandaraman S, Donnely KL, Butora G, Jiao R, Pasternak A, Morriello GJ, Goble SD, Zhou C, Mills SG, Maccoss M, Vicario PP, Ayala JM, Demartino JA, Struthers M, Cascieri MA, Yang L.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1830-4. doi: 10.1016/j.bmcl.2008.12.050. Epub 2008 Dec 24.

PMID:
19237282
14.

Conformational studies of 3-amino-1-alkyl-cyclopentane carboxamide CCR2 antagonists leading to new spirocyclic antagonists.

Pasternak A, Goble SD, Doss GA, Tsou NN, Butora G, Vicario PP, Ayala JM, Struthers M, Demartino JA, Mills SG, Yang L.

Bioorg Med Chem Lett. 2008 Feb 15;18(4):1374-7. doi: 10.1016/j.bmcl.2008.01.016. Epub 2008 Jan 9.

PMID:
18215519
15.

Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists.

Pasternak A, Goble SD, Vicario PP, Di Salvo J, Ayala JM, Struthers M, DeMartino JA, Mills SG, Yang L.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):994-8. doi: 10.1016/j.bmcl.2007.12.029. Epub 2007 Dec 27.

PMID:
18164199
16.

Mice overexpressing chemokine ligand 2 (CCL2) in astrocytes display enhanced nociceptive responses.

Menetski J, Mistry S, Lu M, Mudgett JS, Ransohoff RM, Demartino JA, Macintyre DE, Abbadie C.

Neuroscience. 2007 Nov 9;149(3):706-14. Epub 2007 Aug 14.

PMID:
17870246
17.

CCR5 blockade modulates inflammation and alloimmunity in primates.

Schröder C, Pierson RN 3rd, Nguyen BN, Kawka DW, Peterson LB, Wu G, Zhang T, Springer MS, Siciliano SJ, Iliff S, Ayala JM, Lu M, Mudgett JS, Lyons K, Mills SG, Miller GG, Singer II, Azimzadeh AM, DeMartino JA.

J Immunol. 2007 Aug 15;179(4):2289-99.

18.

Diaryl substituted pyrazoles as potent CCR2 receptor antagonists.

Pinkerton AB, Huang D, Cube RV, Hutchinson JH, Struthers M, Ayala JM, Vicario PP, Patel SR, Wisniewski T, DeMartino JA, Vernier JM.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):807-13. Epub 2006 Oct 25.

PMID:
17088058
19.

Methylxanthine drugs are chitinase inhibitors: investigation of inhibition and binding modes.

Rao FV, Andersen OA, Vora KA, Demartino JA, van Aalten DM.

Chem Biol. 2005 Sep;12(9):973-80.

20.

Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties.

Kim D, Wang L, Hale JJ, Lynch CL, Budhu RJ, Maccoss M, Mills SG, Malkowitz L, Gould SL, DeMartino JA, Springer MS, Hazuda D, Miller M, Kessler J, Hrin RC, Carver G, Carella A, Henry K, Lineberger J, Schleif WA, Emini EA.

Bioorg Med Chem Lett. 2005 Apr 15;15(8):2129-34.

PMID:
15808483
21.

Synthesis and evaluation of CCR5 antagonists containing modified 4-piperidinyl-2-phenyl-1-(phenylsulfonylamino)-butane.

Shah SK, Chen N, Guthikonda RN, Mills SG, Malkowitz L, Springer MS, Gould SL, Demartino JA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA, MacCoss M.

Bioorg Med Chem Lett. 2005 Feb 15;15(4):977-82.

PMID:
15686896
22.

A unique pattern of up- and down-regulation of chemokine receptor CXCR3 on inflammation-inducing Th1 cells.

Chen J, Vistica BP, Takase H, Ham DI, Fariss RN, Wawrousek EF, Chan CC, DeMartino JA, Farber JM, Gery I.

Eur J Immunol. 2004 Oct;34(10):2885-94.

23.

Chemokine receptor-directed agents as novel anti-HIV-1 therapies.

Mills SG, DeMartino JA.

Curr Top Med Chem. 2004;4(10):1017-33. Review.

PMID:
15193136
24.

Syntheses and biological evaluation of 5-(piperidin-1-yl)-3-phenyl-pentylsulfones as CCR5 antagonists.

Shankaran K, Donnelly KL, Shah SK, Caldwell CG, Chen P, Finke PE, Oates B, MacCoss M, Mills SG, DeMartino JA, Gould SL, Malkowitz L, Siciliano SJ, Springer MS, Kwei G, Carella A, Carver G, Danzeisen R, Hazuda D, Holmes K, Kessler J, Lineberger J, Miller MD, Emini EA, Schleif WA.

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3589-93.

PMID:
15177481
25.

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 3: SAR studies on the benzylpyrazole segment.

Shu M, Loebach JL, Parker KA, Mills SG, Chapman KT, Shen DM, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Salvo JD, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):947-52.

PMID:
15012999
26.

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 2: Discovery of potent, selective, and orally bioavailable compounds.

Shen DM, Shu M, Willoughby CA, Shah S, Lynch CL, Hale JJ, Mills SG, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Lyons K, Pivnichny JV, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):941-5.

PMID:
15012998
27.

Antagonists of human CCR5 receptor containing 4-(pyrazolyl)piperidine side chains. Part 1: Discovery and SAR study of 4-pyrazolylpiperidine side chains.

Shen DM, Shu M, Mills SG, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Kwei GY, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller MD, Emini EA.

Bioorg Med Chem Lett. 2004 Feb 23;14(4):935-9.

PMID:
15012997
28.

Use of a small molecule CCR5 inhibitor in macaques to treat simian immunodeficiency virus infection or prevent simian-human immunodeficiency virus infection.

Veazey RS, Klasse PJ, Ketas TJ, Reeves JD, Piatak M Jr, Kunstman K, Kuhmann SE, Marx PA, Lifson JD, Dufour J, Mefford M, Pandrea I, Wolinsky SM, Doms RW, DeMartino JA, Siciliano SJ, Lyons K, Springer MS, Moore JP.

J Exp Med. 2003 Nov 17;198(10):1551-62.

29.

CCR5 antagonists: 3-(pyrrolidin-1-yl)propionic acid analogues with potent anti-HIV activity.

Lynch CL, Hale JJ, Budhu RJ, Gentry AL, Finke PE, Caldwell CG, Mills SG, MacCoss M, Shen DM, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini E.

Org Lett. 2003 Jul 10;5(14):2473-5.

PMID:
12841758
30.

Expression and characterization of the chemokine receptor CCR2B from rhesus monkey.

Jin H, Vicario PP, Zweerink H, Goyal S, Hanlon WA, Dorn CP, Mills SG, DeMartino JA, Cascieri MA, Struthers M.

Biochem Pharmacol. 2003 Jul 15;66(2):321-30.

PMID:
12826275
31.

Impaired neuropathic pain responses in mice lacking the chemokine receptor CCR2.

Abbadie C, Lindia JA, Cumiskey AM, Peterson LB, Mudgett JS, Bayne EK, DeMartino JA, MacIntyre DE, Forrest MJ.

Proc Natl Acad Sci U S A. 2003 Jun 24;100(13):7947-52. Epub 2003 Jun 13.

32.

Antibody-mediated blockade of the CXCR3 chemokine receptor results in diminished recruitment of T helper 1 cells into sites of inflammation.

Xie JH, Nomura N, Lu M, Chen SL, Koch GE, Weng Y, Rosa R, Di Salvo J, Mudgett J, Peterson LB, Wicker LS, DeMartino JA.

J Leukoc Biol. 2003 Jun;73(6):771-80.

PMID:
12773510
33.

Binding of 2-aryl-4-(piperidin-1-yl)butanamines and 1,3,4-trisubstituted pyrrolidines to human CCR5: a molecular modeling-guided mutagenesis study of the binding pocket.

Castonguay LA, Weng Y, Adolfsen W, Di Salvo J, Kilburn R, Caldwell CG, Daugherty BL, Finke PE, Hale JJ, Lynch CL, Mills SG, MacCoss M, Springer MS, DeMartino JA.

Biochemistry. 2003 Feb 18;42(6):1544-50.

PMID:
12578367
34.

1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.

Willoughby CA, Rosauer KG, Hale JJ, Budhu RJ, Mills SG, Chapman KT, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.

Bioorg Med Chem Lett. 2003 Feb 10;13(3):427-31.

PMID:
12565944
35.

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.

Lynch CL, Willoughby CA, Hale JJ, Holson EJ, Budhu RJ, Gentry AL, Rosauer KG, Caldwell CG, Chen P, Mills SG, MacCoss M, Berk S, Chen L, Chapman KT, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.

Bioorg Med Chem Lett. 2003 Jan 6;13(1):119-23.

PMID:
12467630
36.

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 4: synthesis of N-1 acidic functionality affording analogues with enhanced antiviral activity against HIV.

Lynch CL, Hale JJ, Budhu RJ, Gentry AL, Mills SG, Chapman KT, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):3001-4.

PMID:
12270193
37.

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity.

Hale JJ, Budhu RJ, Mills SG, MacCoss M, Gould SL, DeMartino JA, Springer MS, Siciliano SJ, Malkowitz L, Schleif WA, Hazuda D, Miller M, Kessler J, Danzeisen R, Holmes K, Lineberger J, Carella A, Carver G, Emini EA.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2997-3000.

PMID:
12270192
38.

The CXC chemokine murine monokine induced by IFN-gamma (CXC chemokine ligand 9) is made by APCs, targets lymphocytes including activated B cells, and supports antibody responses to a bacterial pathogen in vivo.

Park MK, Amichay D, Love P, Wick E, Liao F, Grinberg A, Rabin RL, Zhang HH, Gebeyehu S, Wright TM, Iwasaki A, Weng Y, DeMartino JA, Elkins KL, Farber JM.

J Immunol. 2002 Aug 1;169(3):1433-43.

39.

Photochemical preparation of a pyridone containing tetracycle: a Jak protein kinase inhibitor.

Thompson JE, Cubbon RM, Cummings RT, Wicker LS, Frankshun R, Cunningham BR, Cameron PM, Meinke PT, Liverton N, Weng Y, DeMartino JA.

Bioorg Med Chem Lett. 2002 Apr 22;12(8):1219-23.

PMID:
11934592
40.

CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines.

Lynch CL, Gentry AL, Hale JJ, Mills SG, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Doss G, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.

Bioorg Med Chem Lett. 2002 Feb 25;12(4):677-9.

PMID:
11844699
41.

Design, synthesis, and SAR of heterocycle-containing antagonists of the human CCR5 receptor for the treatment of HIV-1 infection.

Kim D, Wang L, Caldwell CG, Chen P, Finke PE, Oates B, MacCoss M, Mills SG, Malkowitz L, Gould SL, DeMartino JA, Springer MS, Hazuda D, Miller M, Kessler J, Danzeisen R, Carver G, Carella A, Holmes K, Lineberger J, Schleif WA, Emini EA.

Bioorg Med Chem Lett. 2001 Dec 17;11(24):3103-6.

PMID:
11720852
42.

Discovery of human CCR5 antagonists containing hydantoins for the treatment of HIV-1 infection.

Kim D, Wang L, Caldwell CG, Chen P, Finke PE, Oates B, MacCoss M, Mills SG, Malkowitz L, Gould SL, DeMartino JA, Springer MS, Hazuda D, Miller M, Kessler J, Danzeisen R, Carver G, Carella A, Holmes K, Lineberger J, Schleif WA, Emini EA.

Bioorg Med Chem Lett. 2001 Dec 17;11(24):3099-102.

PMID:
11720851
43.

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity.

Hale JJ, Budhu RJ, Holson EB, Finke PE, Oates B, Mills SG, MacCoss M, Gould SL, DeMartino JA, Springer MS, Siciliano S, Malkowitz L, Schleif WA, Hazuda D, Miller M, Kessler J, Danzeisen R, Holmes K, Lineberger J, Carella A, Carver G, Emini E.

Bioorg Med Chem Lett. 2001 Oct 22;11(20):2741-5.

PMID:
11591514
44.

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 4: synthesis and structure-activity relationships for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-(4-(N-(alkyl)-N-(benzyloxycarbonyl)amino)piperidin-1-yl)butanes.

Finke PE, Oates B, Mills SG, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Carella A, Carver G, Holmes K, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Schleif WA, Emini EA.

Bioorg Med Chem Lett. 2001 Sep 17;11(18):2475-9.

PMID:
11549450
45.

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 3: a proposed pharmacophore model for 1-[N-(methyl)-N-(phenylsulfonyl)amino]-2-(phenyl)-4-[4-(substituted)piperidin-1-yl]butanes.

Finke PE, Meurer LC, Oates B, Shah SK, Loebach JL, Mills SG, MacCoss M, Castonguay L, Malkowitz L, Springer MS, Gould SL, DeMartino JA.

Bioorg Med Chem Lett. 2001 Sep 17;11(18):2469-73.

PMID:
11549449
46.

1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 1: discovery of the pyrrolidine scaffold and determination of its stereochemical requirements.

Hale JJ, Budhu RJ, Mills SG, MacCoss M, Malkowitz L, Siciliano S, Gould SL, DeMartino JA, Springer MS.

Bioorg Med Chem Lett. 2001 Jun 4;11(11):1437-40.

PMID:
11378372
47.

CCR5, CXCR4, and CD4 are clustered and closely apposed on microvilli of human macrophages and T cells.

Singer II, Scott S, Kawka DW, Chin J, Daugherty BL, DeMartino JA, DiSalvo J, Gould SL, Lineberger JE, Malkowitz L, Miller MD, Mitnaul L, Siciliano SJ, Staruch MJ, Williams HR, Zweerink HJ, Springer MS.

J Virol. 2001 Apr;75(8):3779-90.

48.

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. Part 2: structure-activity relationships for substituted 2-Aryl-1-[N-(methyl)-N-(phenylsulfonyl)amino]-4-(piperidin-1-yl)butanes.

Finke PE, Meurer LC, Oates B, Mills SG, MacCoss M, Malkowitz L, Springer MS, Daugherty BL, Gould SL, DeMartino JA, Siciliano SJ, Carella A, Carver G, Holmes K, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Schleif WA, Emini EA.

Bioorg Med Chem Lett. 2001 Jan 22;11(2):265-70.

PMID:
11206474
49.

Antagonists of the human CCR5 receptor as anti-HIV-1 agents. part 1: discovery and initial structure-activity relationships for 1 -amino-2-phenyl-4-(piperidin-1-yl)butanes.

Dorn CP, Finke PE, Oates B, Budhu RJ, Mills SG, MacCoss M, Malkowitz L, Springer MS, Daugherty BL, Gould SL, DeMartino JA, Siciliano SJ, Carella A, Carver G, Holmes K, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Schleif WA, Emini EA.

Bioorg Med Chem Lett. 2001 Jan 22;11(2):259-64.

PMID:
11206473
50.

The CXCR4 agonist ligand stromal derived factor-1 maintains high affinity for receptors in both Galpha(i)-coupled and uncoupled states.

Di Salvo J, Koch GE, Johnson KE, Blake AD, Daugherty BL, DeMartino JA, Sirotina-Meisher A, Liu Y, Springer MS, Cascieri MA, Sullivan KA.

Eur J Pharmacol. 2000 Dec 8;409(2):143-54.

PMID:
11104827

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