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Items: 17

1.

[3H]BMT-046091 a potent and selective radioligand to determine AAK1 distribution and target engagement.

Louis JV, Lu Y, Pieschl R, Tian Y, Hong Y, Dandapani K, Naidu S, Vikramadithyan RK, Dzierba C, Sarvasiddhi SK, Nara SJ, Bronson J, Macor JE, Albright C, Kostich W, Li YW.

Neuropharmacology. 2017 May 15;118:167-174. doi: 10.1016/j.neuropharm.2017.03.015. Epub 2017 Mar 15.

PMID:
28315351
2.

Asymmetric Synthesis of the Major Metabolite of a Calcitonin Gene-Related Peptide Receptor Antagonist and Mechanism of Epoxide Hydrogenolysis.

Luo G, Chen L, Conway CM, Kostich W, Johnson BM, Ng A, Macor JE, Dubowchik GM.

J Org Chem. 2017 Apr 7;82(7):3710-3720. doi: 10.1021/acs.joc.7b00052. Epub 2017 Mar 28.

PMID:
28306261
3.

Triazolopyridine ethers as potent, orally active mGlu2 positive allosteric modulators for treating schizophrenia.

Higgins MA, Marcin LR, Christopher Zusi F, Gentles R, Ding M, Pearce BC, Easton A, Kostich WA, Seager MA, Bourin C, Bristow LJ, Johnson KA, Miller R, Hogan J, Whiterock V, Gulianello M, Ferrante M, Huang Y, Hendricson A, Alt A, Macor JE, Bronson JJ.

Bioorg Med Chem. 2017 Jan 15;25(2):496-513. doi: 10.1016/j.bmc.2016.11.018. Epub 2016 Nov 14.

PMID:
27914948
4.

Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.

Kostich W, Hamman BD, Li YW, Naidu S, Dandapani K, Feng J, Easton A, Bourin C, Baker K, Allen J, Savelieva K, Louis JV, Dokania M, Elavazhagan S, Vattikundala P, Sharma V, Das ML, Shankar G, Kumar A, Holenarsipur VK, Gulianello M, Molski T, Brown JM, Lewis M, Huang Y, Lu Y, Pieschl R, O'Malley K, Lippy J, Nouraldeen A, Lanthorn TH, Ye G, Wilson A, Balakrishnan A, Denton R, Grace JE, Lentz KA, Santone KS, Bi Y, Main A, Swaffield J, Carson K, Mandlekar S, Vikramadithyan RK, Nara SJ, Dzierba C, Bronson J, Macor JE, Zaczek R, Westphal R, Kiss L, Bristow L, Conway CM, Zambrowicz B, Albright CF.

J Pharmacol Exp Ther. 2016 Sep;358(3):371-86. doi: 10.1124/jpet.116.235333. Epub 2016 Jul 13.

5.

Asymmetric Synthesis of Heterocyclic Analogues of a CGRP Receptor Antagonist for Treating Migraine.

Luo G, Chen L, Conway CM, Kostich W, Macor JE, Dubowchik GM.

Org Lett. 2015 Dec 18;17(24):5982-5. doi: 10.1021/acs.orglett.5b02921. Epub 2015 Dec 9.

PMID:
26650258
6.

Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists.

Tora G, Degnan AP, Conway CM, Kostich WA, Davis CD, Pin SS, Schartman R, Xu C, Widmann KA, Macor JE, Dubowchik GM.

Bioorg Med Chem Lett. 2013 Oct 15;23(20):5684-8. doi: 10.1016/j.bmcl.2013.08.031. Epub 2013 Aug 13.

PMID:
23993336
7.

Discovery of (5S,6S,9R)-5-amino-6-(2,3-difluorophenyl)-6,7,8,9-tetrahydro-5H-cyclohepta[b]pyridin-9-yl 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (BMS-927711): an oral calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraine.

Luo G, Chen L, Conway CM, Denton R, Keavy D, Signor L, Kostich W, Lentz KA, Santone KS, Schartman R, Browning M, Tong G, Houston JG, Dubowchik GM, Macor JE.

J Med Chem. 2012 Dec 13;55(23):10644-51. doi: 10.1021/jm3013147. Epub 2012 Nov 15.

PMID:
23153230
8.

Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine.

Luo G, Chen L, Conway CM, Denton R, Keavy D, Gulianello M, Huang Y, Kostich W, Lentz KA, Mercer SE, Schartman R, Signor L, Browning M, Macor JE, Dubowchik GM.

ACS Med Chem Lett. 2012 Feb 27;3(4):337-41. doi: 10.1021/ml300021s. eCollection 2012 Apr 12.

9.

Calcitonin gene-related peptide (CGRP) receptor antagonists: pyridine as a replacement for a core amide group.

Luo G, Chen L, Civiello R, Pin SS, Xu C, Kostich W, Kelley M, Conway CM, Macor JE, Dubowchik GM.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2917-21. doi: 10.1016/j.bmcl.2012.02.065. Epub 2012 Mar 3.

PMID:
22429470
10.

Design of an automated enhanced-throughput platform for functional characterization of positive allosteric modulator-induced leftward shifts in apparent agonist potency in vitro.

Hendricson A, Matchett M, Ferrante M, Ferrante C, Hunnicutt E, Westphal R, Kostich W, Huang Y, Masias N, Hong D, Bertekap R, Burford N, Watson J, Alt A, Myslik J, Zhang L, Knox R.

J Lab Autom. 2012 Apr;17(2):104-15. doi: 10.1177/2211068211435301. Epub 2012 Feb 1.

PMID:
22357567
11.

Small molecule receptor protein tyrosine phosphatase γ (RPTPγ) ligands that inhibit phosphatase activity via perturbation of the tryptophan-proline-aspartate (WPD) loop.

Sheriff S, Beno BR, Zhai W, Kostich WA, McDonnell PA, Kish K, Goldfarb V, Gao M, Kiefer SE, Yanchunas J, Huang Y, Shi S, Zhu S, Dzierba C, Bronson J, Macor JE, Appiah KK, Westphal RS, O'Connell J, Gerritz SW.

J Med Chem. 2011 Oct 13;54(19):6548-62. doi: 10.1021/jm2003766. Epub 2011 Sep 20.

PMID:
21882820
12.

Cloning, purification, crystallization and preliminary X-ray analysis of the catalytic domain of human receptor-like protein tyrosine phosphatase γ in three different crystal forms.

Kish K, McDonnell PA, Goldfarb V, Gao M, Metzler WJ, Langley DR, Bryson JW, Kiefer SE, Carpenter B, Kostich WA, Westphal RS, Sheriff S.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2011 Jul 1;67(Pt 7):768-74. doi: 10.1107/S1744309111017209. Epub 2011 Jun 30.

13.

A high-throughput screen for receptor protein tyrosine phosphatase-gamma selective inhibitors.

Appiah KK, Kostich WA, Gerritz SW, Huang Y, Hamman BD, Allen J, Zhang W, Lanthorn TH, Albright CF, Westphal R, Banks MN, O'Connell JC.

J Biomol Screen. 2011 Jun;16(5):476-85. doi: 10.1177/1087057111399336. Epub 2011 Mar 15.

PMID:
21406618
14.

Immunohistochemical visualization of corticotropin-releasing factor type 1 (CRF1) receptors in monkey brain.

Kostich WA, Grzanna R, Lu NZ, Largent BL.

J Comp Neurol. 2004 Oct 11;478(2):111-25.

PMID:
15349973
15.

High-affinity agonist binding correlates with efficacy (intrinsic activity) at the human serotonin 5-HT2A and 5-HT2C receptors: evidence favoring the ternary complex and two-state models of agonist action.

Fitzgerald LW, Conklin DS, Krause CM, Marshall AP, Patterson JP, Tran DP, Iyer G, Kostich WA, Largent BL, Hartig PR.

J Neurochem. 1999 May;72(5):2127-34.

16.

Molecular identification and analysis of a novel human corticotropin-releasing factor (CRF) receptor: the CRF2gamma receptor.

Kostich WA, Chen A, Sperle K, Largent BL.

Mol Endocrinol. 1998 Aug;12(8):1077-85.

PMID:
9717834
17.

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