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Items: 1 to 20 of 98

1.

Use of a Conformational-Switching Mechanism to Modulate Exposed Polarity: Discovery of CCR2 Antagonist BMS-741672.

Yang MG, Xiao Z, Cherney RJ, Tebben AJ, Batt DG, Brown GD, Chen J, Cvijic ME, Dabros M, Duncia JV, Galella M, Gardner DS, Khandelwal P, Ko SS, Malley MF, Mo R, Pang J, Rose AV, Santella JB 3rd, Shi H, Srivastava A, Traeger SC, Wang B, Xu S, Zhao R, Barrish JC, Mandlekar S, Zhao Q, Carter PH.

ACS Med Chem Lett. 2019 Jan 16;10(3):300-305. doi: 10.1021/acsmedchemlett.8b00439. eCollection 2019 Mar 14.

PMID:
30891130
2.

Structure of CC chemokine receptor 2 with orthosteric and allosteric antagonists.

Zheng Y, Qin L, Zacarías NV, de Vries H, Han GW, Gustavsson M, Dabros M, Zhao C, Cherney RJ, Carter P, Stamos D, Abagyan R, Cherezov V, Stevens RC, IJzerman AP, Heitman LH, Tebben A, Kufareva I, Handel TM.

Nature. 2016 Dec 15;540(7633):458-461. doi: 10.1038/nature20605. Epub 2016 Dec 7.

3.

The discovery of BMS-457, a potent and selective CCR1 antagonist.

Gardner DS, Santella JB 3rd, Duncia JV, Carter PH, Dhar TG, Wu H, Guo W, Cavallaro C, Van Kirk K, Yarde M, Briceno SW, Grafstrom RR, Liu R, Patel SR, Tebben AJ, Camac D, Khan J, Watson A, Yang G, Rose A, Foster WR, Cvijic ME, Davies P, Hynes J Jr.

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3833-40. doi: 10.1016/j.bmcl.2013.04.079. Epub 2013 May 7.

PMID:
23707259
4.

Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.

Carter PH, Brown GD, Cherney RJ, Batt DG, Chen J, Clark CM, Cvijic ME, Duncia JV, Ko SS, Mandlekar S, Mo R, Nelson DJ, Pang J, Rose AV, Santella JB 3rd, Tebben AJ, Traeger SC, Xu S, Zhao Q, Barrish JC.

ACS Med Chem Lett. 2015 Mar 4;6(4):439-44. doi: 10.1021/ml500505q. eCollection 2015 Apr 9.

5.

Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344.

Brodmerkel CM, Huber R, Covington M, Diamond S, Hall L, Collins R, Leffet L, Gallagher K, Feldman P, Collier P, Stow M, Gu X, Baribaud F, Shin N, Thomas B, Burn T, Hollis G, Yeleswaram S, Solomon K, Friedman S, Wang A, Xue CB, Newton RC, Scherle P, Vaddi K.

J Immunol. 2005 Oct 15;175(8):5370-8.

6.

Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2.

Xue CB, Wang A, Meloni D, Zhang K, Kong L, Feng H, Glenn J, Huang T, Zhang Y, Cao G, Anand R, Zheng C, Xia M, Han Q, Robinson DJ, Storace L, Shao L, Li M, Brodmerkel CM, Covington M, Scherle P, Diamond S, Yeleswaram S, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7473-8. doi: 10.1016/j.bmcl.2010.10.020. Epub 2010 Oct 13.

PMID:
21036044
7.

Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.

Xue CB, Feng H, Cao G, Huang T, Glenn J, Anand R, Meloni D, Zhang K, Kong L, Wang A, Zhang Y, Zheng C, Xia M, Chen L, Tanaka H, Han Q, Robinson DJ, Modi D, Storace L, Shao L, Sharief V, Li M, Galya LG, Covington M, Scherle P, Diamond S, Emm T, Yeleswaram S, Contel N, Vaddi K, Newton R, Hollis G, Friedman S, Metcalf B.

ACS Med Chem Lett. 2011 Mar 31;2(6):450-4. doi: 10.1021/ml200030q. eCollection 2011 Jun 9.

8.

Structure prediction and molecular dynamics simulations of a G-protein coupled receptor: human CCR2 receptor.

Singh R, Sobhia ME.

J Biomol Struct Dyn. 2013;31(7):694-715. doi: 10.1080/07391102.2012.707460. Epub 2012 Aug 22.

PMID:
22909007
9.

Crystal Structure of CC Chemokine Receptor 2A in Complex with an Orthosteric Antagonist Provides Insights for the Design of Selective Antagonists.

Apel AK, Cheng RKY, Tautermann CS, Brauchle M, Huang CY, Pautsch A, Hennig M, Nar H, Schnapp G.

Structure. 2019 Mar 5;27(3):427-438.e5. doi: 10.1016/j.str.2018.10.027. Epub 2018 Dec 20.

PMID:
30581043
10.

Pharmacological characterization and appetite suppressive properties of BMS-193885, a novel and selective neuropeptide Y(1) receptor antagonist.

Antal-Zimanyi I, Bruce MA, Leboulluec KL, Iben LG, Mattson GK, McGovern RT, Hogan JB, Leahy CL, Flowers SC, Stanley JA, Ortiz AA, Poindexter GS.

Eur J Pharmacol. 2008 Aug 20;590(1-3):224-32. doi: 10.1016/j.ejphar.2008.06.032. Epub 2008 Jun 12.

PMID:
18573246
11.

Multiple binding sites for small-molecule antagonists at the CC chemokine receptor 2.

Zweemer AJ, Nederpelt I, Vrieling H, Hafith S, Doornbos ML, de Vries H, Abt J, Gross R, Stamos D, Saunders J, Smit MJ, Ijzerman AP, Heitman LH.

Mol Pharmacol. 2013 Oct;84(4):551-61. doi: 10.1124/mol.113.086850. Epub 2013 Jul 22.

PMID:
23877010
12.

When structure-affinity relationships meet structure-kinetics relationships: 3-((Inden-1-yl)amino)-1-isopropyl-cyclopentane-1-carboxamides as CCR2 antagonists.

Vilums M, Zweemer AJ, Barmare F, van der Gracht AM, Bleeker DC, Yu Z, de Vries H, Gross R, Clemens J, Krenitsky P, Brussee J, Stamos D, Saunders J, Heitman LH, IJzerman AP.

Eur J Med Chem. 2015 Mar 26;93:121-34. doi: 10.1016/j.ejmech.2015.01.063. Epub 2015 Feb 2.

PMID:
25666912
13.

Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.

Xue CB, Wang A, Han Q, Zhang Y, Cao G, Feng H, Huang T, Zheng C, Xia M, Zhang K, Kong L, Glenn J, Anand R, Meloni D, Robinson DJ, Shao L, Storace L, Li M, Hughes RO, Devraj R, Morton PA, Rogier DJ, Covington M, Scherle P, Diamond S, Emm T, Yeleswaram S, Contel N, Vaddi K, Newton R, Hollis G, Metcalf B.

ACS Med Chem Lett. 2011 Oct 5;2(12):913-8. doi: 10.1021/ml200199c. eCollection 2011 Dec 8.

14.

Emerging issues of connexin channels: biophysics fills the gap.

Harris AL.

Q Rev Biophys. 2001 Aug;34(3):325-472. Review. Erratum in: Q Rev Biophys 2002 Feb;35(1):109.

PMID:
11838236
15.

High-content analysis of CCR2 antagonists on human primary monocytes.

Kredel S, Wolff M, Hobbie S, Bieler M, Gierschik P, Heilker R.

J Biomol Screen. 2011 Aug;16(7):683-93. doi: 10.1177/1087057111406884. Epub 2011 May 3.

PMID:
21540351
16.

Progress in the discovery of CC chemokine receptor 2 antagonists, 2009 - 2012.

Carter PH.

Expert Opin Ther Pat. 2013 May;23(5):549-68. doi: 10.1517/13543776.2013.771168. Epub 2013 Feb 22. Review.

PMID:
23428142
17.

Isolation and structures of novel fungal metabolites as chemokine receptor (CCR2) antagonists.

Herath KB, Jayasuriya H, Ondeyka JG, Polishook JD, Bills GF, Dombrowski AW, Cabello A, Vicario PP, Zweerink H, Guan Z, Singh SB.

J Antibiot (Tokyo). 2005 Nov;58(11):686-94.

PMID:
16466022
18.

Discovery and synthesis of cyclohexenyl derivatives as modulators of CC chemokine receptor 2 activity.

Brown GD, Shi Q, Delucca GV, Batt DG, Galella MA, Cvijic ME, Liu RQ, Qiu F, Zhao Q, Barrish JC, Carter PH.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):662-666. doi: 10.1016/j.bmcl.2015.11.051. Epub 2015 Nov 17.

PMID:
26631321
19.

Discovery of a 4-Azetidinyl-1-thiazoyl-cyclohexane CCR2 Antagonist as a Development Candidate.

Zhang X, Hou C, Hufnagel H, Singer M, Opas E, McKenney S, Johnson D, Sui Z.

ACS Med Chem Lett. 2012 Oct 8;3(12):1039-44. doi: 10.1021/ml300260s. eCollection 2012 Dec 13.

20.

Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle.

Mirzadegan T, Diehl F, Ebi B, Bhakta S, Polsky I, McCarley D, Mulkins M, Weatherhead GS, Lapierre JM, Dankwardt J, Morgans D Jr, Wilhelm R, Jarnagin K.

J Biol Chem. 2000 Aug 18;275(33):25562-71.

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