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Items: 17

1.

Rationally Designed, Conformationally Constrained Inverse Agonists of RORγt-Identification of a Potent, Selective Series with Biologic-Like in Vivo Efficacy.

Marcoux D, Duan JJ, Shi Q, Cherney RJ, Srivastava AS, Cornelius L, Batt DG, Liu Q, Beaudoin-Bertrand M, Weigelt CA, Khandelwal P, Vishwakrishnan S, Selvakumar K, Karmakar A, Gupta AK, Basha M, Ramlingam S, Manjunath N, Vanteru S, Karmakar S, Maddala N, Vetrichelvan M, Gupta A, Rampulla RA, Mathur A, Yip S, Li P, Wu DR, Khan J, Ruzanov M, Sack JS, Wang J, Yarde M, Cvijic ME, Li S, Shuster DJ, Borowski V, Xie JH, McIntyre KW, Obermeier MT, Fura A, Stefanski K, Cornelius G, Hynes J Jr, Tino JA, Macor JE, Salter-Cid L, Denton R, Zhao Q, Carter PH, Dhar TGM.

J Med Chem. 2019 Nov 14;62(21):9931-9946. doi: 10.1021/acs.jmedchem.9b01369. Epub 2019 Oct 31.

PMID:
31638797
2.

Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists.

Duan JJ, Lu Z, Jiang B, Stachura S, Weigelt CA, Sack JS, Khan J, Ruzanov M, Galella MA, Wu DR, Yarde M, Shen DR, Shuster DJ, Borowski V, Xie JH, Zhang L, Vanteru S, Gupta AK, Mathur A, Zhao Q, Foster W, Salter-Cid LM, Carter PH, Dhar TGM.

ACS Med Chem Lett. 2019 Feb 26;10(3):367-373. doi: 10.1021/acsmedchemlett.9b00010. eCollection 2019 Mar 14.

PMID:
30891142
3.

Identification and Preclinical Pharmacology of ((1 R,3 S)-1-Amino-3-(( S)-6-(2-methoxyphenethyl)-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986166): A Differentiated Sphingosine-1-phosphate Receptor 1 (S1P1) Modulator Advanced into Clinical Trials.

Gilmore JL, Xiao HY, Dhar TGM, Yang MG, Xiao Z, Xie J, Lehman-McKeeman LD, Gong L, Sun H, Lecureux L, Chen C, Wu DR, Dabros M, Yang X, Taylor TL, Zhou XD, Heimrich EM, Thomas R, McIntyre KW, Borowski V, Warrack BM, Li Y, Shi H, Levesque PC, Yang Z, Marino AM, Cornelius G, D'Arienzo CJ, Mathur A, Rampulla R, Gupta A, Pragalathan B, Shen DR, Cvijic ME, Salter-Cid LM, Carter PH, Dyckman AJ.

J Med Chem. 2019 Mar 14;62(5):2265-2285. doi: 10.1021/acs.jmedchem.8b01695. Epub 2019 Mar 6.

PMID:
30785748
4.

Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.

Gong H, Weinstein DS, Lu Z, Duan JJ, Stachura S, Haque L, Karmakar A, Hemagiri H, Raut DK, Gupta AK, Khan J, Camac D, Sack JS, Pudzianowski A, Wu DR, Yarde M, Shen DR, Borowski V, Xie JH, Sun H, D'Arienzo C, Dabros M, Galella MA, Wang F, Weigelt CA, Zhao Q, Foster W, Somerville JE, Salter-Cid LM, Barrish JC, Carter PH, Dhar TGM.

Bioorg Med Chem Lett. 2018 Jan 15;28(2):85-93. doi: 10.1016/j.bmcl.2017.12.006. Epub 2017 Dec 5.

PMID:
29233651
5.

Asymmetric Hydroboration Approach to the Scalable Synthesis of ((1R,3S)-1-Amino-3-((R)-6-hexyl-5,6,7,8-tetrahydronaphthalen-2-yl)cyclopentyl)methanol (BMS-986104) as a Potent S1P1 Receptor Modulator.

Yang MG, Xiao Z, Dhar TG, Xiao HY, Gilmore JL, Marcoux D, Xie JH, McIntyre KW, Taylor TL, Borowski V, Heimrich E, Li YW, Feng J, Fernandes A, Yang Z, Balimane P, Marino AM, Cornelius G, Warrack BM, Mathur A, Wu DR, Li P, Gupta A, Pragalathan B, Shen DR, Cvijic ME, Lehman-McKeeman LD, Salter-Cid L, Barrish JC, Carter PH, Dyckman AJ.

J Med Chem. 2016 Dec 22;59(24):11138-11147. doi: 10.1021/acs.jmedchem.6b01433. Epub 2016 Dec 7.

PMID:
28002964
6.

Discovery and Structure-Activity Relationship (SAR) of a Series of Ethanolamine-Based Direct-Acting Agonists of Sphingosine-1-phosphate (S1P1).

Gilmore JL, Sheppeck JE 2nd, Watterson SH, Haque L, Mukhopadhyay P, Tebben AJ, Galella MA, Shen DR, Yarde M, Cvijic ME, Borowski V, Gillooly K, Taylor T, McIntyre KW, Warrack B, Levesque PC, Li JP, Cornelius G, D'Arienzo C, Marino A, Balimane P, Salter-Cid L, Barrish JC, Pitts WJ, Carter PH, Xie J, Dyckman AJ.

J Med Chem. 2016 Jul 14;59(13):6248-64. doi: 10.1021/acs.jmedchem.6b00373. Epub 2016 Jul 1.

PMID:
27309907
7.

Dual Inhibition of Interleukin-23 and Interleukin-17 Offers Superior Efficacy in Mouse Models of Autoimmunity.

Mangan PR, Su LJ, Jenny V, Tatum AL, Picarillo C, Skala S, Ditto N, Lin Z, Yang X, Cotter PZ, Shuster DJ, Song Y, Borowski V, Thomas RL, Heimrich EM, Devaux B, Das Gupta R, Carvajal I, McIntyre KW, Xie J, Zhao Q, Struthers M, Salter-Cid LM.

J Pharmacol Exp Ther. 2015 Aug;354(2):152-65. doi: 10.1124/jpet.115.224246. Epub 2015 May 26.

PMID:
26015463
8.

Engineering of a novel anti-CD40L domain antibody for treatment of autoimmune diseases.

Xie JH, Yamniuk AP, Borowski V, Kuhn R, Susulic V, Rex-Rabe S, Yang X, Zhou X, Zhang Y, Gillooly K, Brosius R, Ravishankar R, Waggie K, Mink K, Price L, Rehfuss R, Tamura J, An Y, Cheng L, Abramczyk B, Ignatovich O, Drew P, Grant S, Bryson JW, Suchard S, Salter-Cid L, Nadler S, Suri A.

J Immunol. 2014 May 1;192(9):4083-92. doi: 10.4049/jimmunol.1303239. Epub 2014 Mar 26.

9.

A highly selective, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor has potent activity in vitro and in vivo.

LaMontagne KR, Butler J, Borowski VB, Fuentes-Pesquera AR, Blevitt JM, Huang S, Li R, Connolly PJ, Greenberger LM.

Angiogenesis. 2009;12(3):287-96. doi: 10.1007/s10456-009-9151-7. Epub 2009 Jun 21.

PMID:
19544081
10.

Cellular and in vivo activity of JNJ-28871063, a nonquinazoline pan-ErbB kinase inhibitor that crosses the blood-brain barrier and displays efficacy against intracranial tumors.

Emanuel SL, Hughes TV, Adams M, Rugg CA, Fuentes-Pesquera A, Connolly PJ, Pandey N, Moreno-Mazza S, Butler J, Borowski V, Middleton SA, Gruninger RH, Story JR, Napier C, Hollister B, Greenberger LM.

Mol Pharmacol. 2008 Feb;73(2):338-48. Epub 2007 Nov 1.

PMID:
17975007
11.

Delivery of G3139 using releasable PEG-linkers: impact on pharmacokinetic profile and anti-tumor efficacy.

Zhao H, Peng P, Longley C, Zhang Y, Borowski V, Mehlig M, Reddy P, Xia J, Borchard G, Lipman J, Benimetskaya L, Stein CA.

J Control Release. 2007 Jun 4;119(2):143-52. Epub 2006 Dec 29.

PMID:
17397960
12.

Engineering an arginine catabolizing bioconjugate: Biochemical and pharmacological characterization of PEGylated derivatives of arginine deiminase from Mycoplasma arthritidis.

Wang M, Basu A, Palm T, Hua J, Youngster S, Hwang L, Liu HC, Li X, Peng P, Zhang Y, Zhao H, Zhang Z, Longley C, Mehlig M, Borowski V, Sai P, Viswanathan M, Jang E, Petti G, Liu S, Yang K, Filpula D.

Bioconjug Chem. 2006 Nov-Dec;17(6):1447-59. Erratum in: Bioconjug Chem. 2007 Mar-Apr;18(2):605.

PMID:
17105223
13.

Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor.

Seamon JA, Rugg CA, Emanuel S, Calcagno AM, Ambudkar SV, Middleton SA, Butler J, Borowski V, Greenberger LM.

Mol Cancer Ther. 2006 Oct;5(10):2459-67.

14.

Structure-function engineering of interferon-beta-1b for improving stability, solubility, potency, immunogenicity, and pharmacokinetic properties by site-selective mono-PEGylation.

Basu A, Yang K, Wang M, Liu S, Chintala R, Palm T, Zhao H, Peng P, Wu D, Zhang Z, Hua J, Hsieh MC, Zhou J, Petti G, Li X, Janjua A, Mendez M, Liu J, Longley C, Zhang Z, Mehlig M, Borowski V, Viswanathan M, Filpula D.

Bioconjug Chem. 2006 May-Jun;17(3):618-30.

PMID:
16704199
15.

Antitumor activity of poly(ethylene glycol)-camptothecin conjugate: the inhibition of tumor growth in vivo.

Yu D, Peng P, Dharap SS, Wang Y, Mehlig M, Chandna P, Zhao H, Filpula D, Yang K, Borowski V, Borchard G, Zhang Z, Minko T.

J Control Release. 2005 Dec 10;110(1):90-102. Epub 2005 Nov 4.

PMID:
16271793
16.

Tailoring structure-function and pharmacokinetic properties of single-chain Fv proteins by site-specific PEGylation.

Yang K, Basu A, Wang M, Chintala R, Hsieh MC, Liu S, Hua J, Zhang Z, Zhou J, Li M, Phyu H, Petti G, Mendez M, Janjua H, Peng P, Longley C, Borowski V, Mehlig M, Filpula D.

Protein Eng. 2003 Oct;16(10):761-70.

PMID:
14600206
17.

Anticancer drug delivery systems: multi-loaded N4-acyl poly(ethylene glycol) prodrugs of ara-C. II. Efficacy in ascites and solid tumors.

Choe YH, Conover CD, Wu D, Royzen M, Gervacio Y, Borowski V, Mehlig M, Greenwald RB.

J Control Release. 2002 Feb 19;79(1-3):55-70.

PMID:
11853918

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