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Items: 37

1.

Hyaluronan-CD44 interactions mediate contractility and migration in periodontal ligament cells.

Al-Rekabi Z, Fura AM, Juhlin I, Yassin A, Popowics TE, Sniadecki NJ.

Cell Adh Migr. 2019 Jan 24:1-13. doi: 10.1080/19336918.2019.1568140. [Epub ahead of print]

PMID:
30676222
2.

Daclatasvir: A Review of Preclinical and Clinical Pharmacokinetics.

Gandhi Y, Eley T, Fura A, Li W, Bertz RJ, Garimella T.

Clin Pharmacokinet. 2018 Aug;57(8):911-928. doi: 10.1007/s40262-017-0624-3. Review.

PMID:
29353349
3.

Discovery of highly potent, selective, covalent inhibitors of JAK3.

Kempson J, Ovalle D, Guo J, Wrobleski ST, Lin S, Spergel SH, Duan JJ, Jiang B, Lu Z, Das J, Yang BV, Hynes J Jr, Wu H, Tokarski J, Sack JS, Khan J, Schieven G, Blatt Y, Chaudhry C, Salter-Cid LM, Fura A, Barrish JC, Carter PH, Pitts WJ.

Bioorg Med Chem Lett. 2017 Oct 15;27(20):4622-4625. doi: 10.1016/j.bmcl.2017.09.023. Epub 2017 Sep 11.

PMID:
28927786
4.

Bruton's tyrosine kinase inhibitor BMS-986142 in experimental models of rheumatoid arthritis enhances efficacy of agents representing clinical standard-of-care.

Gillooly KM, Pulicicchio C, Pattoli MA, Cheng L, Skala S, Heimrich EM, McIntyre KW, Taylor TL, Kukral DW, Dudhgaonkar S, Nagar J, Banas D, Watterson SH, Tino JA, Fura A, Burke JR.

PLoS One. 2017 Jul 24;12(7):e0181782. doi: 10.1371/journal.pone.0181782. eCollection 2017.

5.

Identification of a Potent, Selective, and Efficacious Phosphatidylinositol 3-Kinase δ (PI3Kδ) Inhibitor for the Treatment of Immunological Disorders.

Liu Q, Shi Q, Marcoux D, Batt DG, Cornelius L, Qin LY, Ruan Z, Neels J, Beaudoin-Bertrand M, Srivastava AS, Li L, Cherney RJ, Gong H, Watterson SH, Weigelt C, Gillooly KM, McIntyre KW, Xie JH, Obermeier MT, Fura A, Sleczka B, Stefanski K, Fancher RM, Padmanabhan S, Rp T, Kundu I, Rajareddy K, Smith R, Hennan JK, Xing D, Fan J, Levesque PC, Ruan Q, Pitt S, Zhang R, Pedicord D, Pan J, Yarde M, Lu H, Lippy J, Goldstine C, Skala S, Rampulla RA, Mathur A, Gupta A, Arunachalam PN, Sack JS, Muckelbauer JK, Cvijic ME, Salter-Cid LM, Bhide RS, Poss MA, Hynes J, Carter PH, Macor JE, Ruepp S, Schieven GL, Tino JA.

J Med Chem. 2017 Jun 22;60(12):5193-5208. doi: 10.1021/acs.jmedchem.7b00618. Epub 2017 Jun 5.

PMID:
28541707
6.

Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.

Hynes J Jr, Wu H, Kempson J, Duan JJ, Lu Z, Jiang B, Stachura S, Tokarski JS, Sack JS, Khan JA, Lippy JS, Zhang RF, Pitt S, Shen G, Gillooly K, McIntyre K, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, Fura A, Schieven GL, Pitts WJ, Wrobleski ST.

Bioorg Med Chem Lett. 2017 Jul 15;27(14):3101-3106. doi: 10.1016/j.bmcl.2017.05.043. Epub 2017 May 15.

PMID:
28539220
7.

Discovery of 6-Fluoro-5-(R)-(3-(S)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)-2-methylphenyl)-2-(S)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1H-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton's Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.

Watterson SH, De Lucca GV, Shi Q, Langevine CM, Liu Q, Batt DG, Beaudoin Bertrand M, Gong H, Dai J, Yip S, Li P, Sun D, Wu DR, Wang C, Zhang Y, Traeger SC, Pattoli MA, Skala S, Cheng L, Obermeier MT, Vickery R, Discenza LN, D'Arienzo CJ, Zhang Y, Heimrich E, Gillooly KM, Taylor TL, Pulicicchio C, McIntyre KW, Galella MA, Tebben AJ, Muckelbauer JK, Chang C, Rampulla R, Mathur A, Salter-Cid L, Barrish JC, Carter PH, Fura A, Burke JR, Tino JA.

J Med Chem. 2016 Oct 13;59(19):9173-9200. Epub 2016 Sep 19.

PMID:
27583770
8.

Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177).

De Lucca GV, Shi Q, Liu Q, Batt DG, Beaudoin Bertrand M, Rampulla R, Mathur A, Discenza L, D'Arienzo C, Dai J, Obermeier M, Vickery R, Zhang Y, Yang Z, Marathe P, Tebben AJ, Muckelbauer JK, Chang CJ, Zhang H, Gillooly K, Taylor T, Pattoli MA, Skala S, Kukral DW, McIntyre KW, Salter-Cid L, Fura A, Burke JR, Barrish JC, Carter PH, Tino JA.

J Med Chem. 2016 Sep 8;59(17):7915-35. doi: 10.1021/acs.jmedchem.6b00722. Epub 2016 Aug 26.

PMID:
27531604
9.

Glycoprotein Ib-IX-V Complex Transmits Cytoskeletal Forces That Enhance Platelet Adhesion.

Feghhi S, Munday AD, Tooley WW, Rajsekar S, Fura AM, Kulman JD, López JA, Sniadecki NJ.

Biophys J. 2016 Aug 9;111(3):601-608. doi: 10.1016/j.bpj.2016.06.023.

10.

Discovery of the Selective CYP17A1 Lyase Inhibitor BMS-351 for the Treatment of Prostate Cancer.

Huang A, Jayaraman L, Fura A, Vite GD, Trainor GL, Gottardis MM, Spires TE, Spires VM, Rizzo CA, Obermeier MT, Elzinga PA, Todderud G, Fan Y, Newitt JA, Beyer SM, Zhu Y, Warrack BM, Goodenough AK, Tebben AJ, Doweyko AM, Gold DL, Balog A.

ACS Med Chem Lett. 2015 Dec 2;7(1):40-5. doi: 10.1021/acsmedchemlett.5b00310. eCollection 2016 Jan 14.

11.

Activation of the IGF1 pathway mediates changes in cellular contractility and motility in single-suture craniosynostosis.

Al-Rekabi Z, Wheeler MM, Leonard A, Fura AM, Juhlin I, Frazar C, Smith JD, Park SS, Gustafson JA, Clarke CM, Cunningham ML, Sniadecki NJ.

J Cell Sci. 2016 Feb 1;129(3):483-91. doi: 10.1242/jcs.175976. Epub 2015 Dec 11.

12.

Discovery of pyrrolo[1,2-b]pyridazine-3-carboxamides as Janus kinase (JAK) inhibitors.

Duan JJ, Lu Z, Jiang B, Yang BV, Doweyko LM, Nirschl DS, Haque LE, Lin S, Brown G, Hynes J Jr, Tokarski JS, Sack JS, Khan J, Lippy JS, Zhang RF, Pitt S, Shen G, Pitts WJ, Carter PH, Barrish JC, Nadler SG, Salter-Cid LM, McKinnon M, Fura A, Schieven GL, Wrobleski ST.

Bioorg Med Chem Lett. 2014 Dec 15;24(24):5721-5726. doi: 10.1016/j.bmcl.2014.10.061. Epub 2014 Oct 24.

PMID:
25453808
13.

Hepatitis C virus NS5A replication complex inhibitors: the discovery of daclatasvir.

Belema M, Nguyen VN, Bachand C, Deon DH, Goodrich JT, James CA, Lavoie R, Lopez OD, Martel A, Romine JL, Ruediger EH, Snyder LB, St Laurent DR, Yang F, Zhu J, Wong HS, Langley DR, Adams SP, Cantor GH, Chimalakonda A, Fura A, Johnson BM, Knipe JO, Parker DD, Santone KS, Fridell RA, Lemm JA, O'Boyle DR 2nd, Colonno RJ, Gao M, Meanwell NA, Hamann LG.

J Med Chem. 2014 Mar 13;57(5):2013-32. doi: 10.1021/jm401836p. Epub 2014 Feb 12.

PMID:
24521299
14.

Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778).

Devasthale P, Wang Y, Wang W, Fevig J, Feng J, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Moulin F, Li YX, Zahler R, Kirby MS, Hamann LG.

J Med Chem. 2013 Sep 26;56(18):7343-57. doi: 10.1021/jm4008906. Epub 2013 Sep 9.

PMID:
23964740
15.

Attribution of the discrepancy between ELISA and LC-MS/MS assay results of a PEGylated scaffold protein in post-dose monkey plasma samples due to the presence of anti-drug antibodies.

Wang SJ, Wu ST, Gokemeijer J, Fura A, Krishna M, Morin P, Chen G, Price K, Wang-Iverson D, Olah T, Weiner R, Tymiak A, Jemal M.

Anal Bioanal Chem. 2012 Jan;402(3):1229-39. doi: 10.1007/s00216-011-5527-9. Epub 2011 Dec 1.

PMID:
22130720
16.

7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site.

Wang W, Devasthale P, Wang A, Harrity T, Egan D, Morgan N, Cap M, Fura A, Klei HE, Kish K, Weigelt C, Sun L, Levesque P, Li YX, Zahler R, Kirby MS, Hamann LG.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6646-51. doi: 10.1016/j.bmcl.2011.09.074. Epub 2011 Sep 24.

PMID:
21996520
17.

Discovery of 6-(aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors.

Meng W, Brigance RP, Chao HJ, Fura A, Harrity T, Marcinkeviciene J, O'Connor SP, Tamura JK, Xie D, Zhang Y, Klei HE, Kish K, Weigelt CA, Turdi H, Wang A, Zahler R, Kirby MS, Hamann LG.

J Med Chem. 2010 Aug 12;53(15):5620-8. doi: 10.1021/jm100634a.

PMID:
20684603
18.

Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes.

Brigance RP, Meng W, Fura A, Harrity T, Wang A, Zahler R, Kirby MS, Hamann LG.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4395-8. doi: 10.1016/j.bmcl.2010.06.063. Epub 2010 Jun 15.

PMID:
20598534
19.

N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.

Nirschl AA, Zou Y, Krystek SR Jr, Sutton JC, Simpkins LM, Lupisella JA, Kuhns JE, Seethala R, Golla R, Sleph PG, Beehler BC, Grover GJ, Egan D, Fura A, Vyas VP, Li YX, Sack JS, Kish KF, An Y, Bryson JA, Gougoutas JZ, DiMarco J, Zahler R, Ostrowski J, Hamann LG.

J Med Chem. 2009 May 14;52(9):2794-8. doi: 10.1021/jm801583j.

PMID:
19351168
20.

Pharmacokinetics of the dipeptidyl peptidase 4 inhibitor saxagliptin in rats, dogs, and monkeys and clinical projections.

Fura A, Khanna A, Vyas V, Koplowitz B, Chang SY, Caporuscio C, Boulton DW, Christopher LJ, Chadwick KD, Hamann LG, Humphreys WG, Kirby M.

Drug Metab Dispos. 2009 Jun;37(6):1164-71. doi: 10.1124/dmd.108.026088. Epub 2009 Feb 27.

PMID:
19251818
21.

Prediction of human oral pharmacokinetics using nonclinical data: examples involving four proprietary compounds.

Fura A, Vyas V, Humphreys W, Chimalokonda A, Rodrigues D.

Biopharm Drug Dispos. 2008 Nov;29(8):455-68. doi: 10.1002/bdd.632.

PMID:
18989850
22.

Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.

Salvati ME, Balog A, Shan W, Rampulla R, Giese S, Mitt T, Furch JA, Vite GD, Attar RM, Jure-Kunkel M, Geng J, Rizzo CA, Gottardis MM, Krystek SR, Gougoutas J, Galella MA, Obermeier M, Fura A, Chandrasena G.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1910-5. doi: 10.1016/j.bmcl.2008.02.006. Epub 2008 Feb 8.

PMID:
18291644
23.

Discovery of potent and muscle selective androgen receptor modulators through scaffold modifications.

Li JJ, Sutton JC, Nirschl A, Zou Y, Wang H, Sun C, Pi Z, Johnson R, Krystek SR Jr, Seethala R, Golla R, Sleph PG, Beehler BC, Grover GJ, Fura A, Vyas VP, Li CY, Gougoutas JZ, Galella MA, Zahler R, Ostrowski J, Hamann LG.

J Med Chem. 2007 Jun 28;50(13):3015-25. Epub 2007 Jun 7.

PMID:
17552509
24.

Tandem optimization of target activity and elimination of mutagenic potential in a potent series of N-aryl bicyclic hydantoin-based selective androgen receptor modulators.

Hamann LG, Manfredi MC, Sun C, Krystek SR Jr, Huang Y, Bi Y, Augeri DJ, Wang T, Zou Y, Betebenner DA, Fura A, Seethala R, Golla R, Kuhns JE, Lupisella JA, Darienzo CJ, Custer LL, Price JL, Johnson JM, Biller SA, Zahler R, Ostrowski J.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):1860-4. Epub 2007 Jan 27.

PMID:
17292608
25.

Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold.

Sun C, Robl JA, Wang TC, Huang Y, Kuhns JE, Lupisella JA, Beehler BC, Golla R, Sleph PG, Seethala R, Fura A, Krystek SR Jr, An Y, Malley MF, Sack JS, Salvati ME, Grover GJ, Ostrowski J, Hamann LG.

J Med Chem. 2006 Dec 28;49(26):7596-9.

PMID:
17181141
26.

Pharmacological and x-ray structural characterization of a novel selective androgen receptor modulator: potent hyperanabolic stimulation of skeletal muscle with hypostimulation of prostate in rats.

Ostrowski J, Kuhns JE, Lupisella JA, Manfredi MC, Beehler BC, Krystek SR Jr, Bi Y, Sun C, Seethala R, Golla R, Sleph PG, Fura A, An Y, Kish KF, Sack JS, Mookhtiar KA, Grover GJ, Hamann LG.

Endocrinology. 2007 Jan;148(1):4-12. Epub 2006 Sep 28.

PMID:
17008401
27.

Discovery and preclinical studies of (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5- methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan- 2-ol (BMS-540215), an in vivo active potent VEGFR-2 inhibitor.

Bhide RS, Cai ZW, Zhang YZ, Qian L, Wei D, Barbosa S, Lombardo LJ, Borzilleri RM, Zheng X, Wu LI, Barrish JC, Kim SH, Leavitt K, Mathur A, Leith L, Chao S, Wautlet B, Mortillo S, Jeyaseelan R Sr, Kukral D, Hunt JT, Kamath A, Fura A, Vyas V, Marathe P, D'Arienzo C, Derbin G, Fargnoli J.

J Med Chem. 2006 Apr 6;49(7):2143-6.

PMID:
16570908
28.

Role of pharmacologically active metabolites in drug discovery and development.

Fura A.

Drug Discov Today. 2006 Feb;11(3-4):133-42. Review.

PMID:
16533711
29.

Design, synthesis, and evaluation of orally active 4-(2,4-difluoro-5-(methoxycarbamoyl)phenylamino)pyrrolo[2,1-f][1,2,4]triazines as dual vascular endothelial growth factor receptor-2 and fibroblast growth factor receptor-1 inhibitors.

Borzilleri RM, Zheng X, Qian L, Ellis C, Cai ZW, Wautlet BS, Mortillo S, Jeyaseelan R Sr, Kukral DW, Fura A, Kamath A, Vyas V, Tokarski JS, Barrish JC, Hunt JT, Lombardo LJ, Fargnoli J, Bhide RS.

J Med Chem. 2005 Jun 16;48(12):3991-4008.

PMID:
15943473
30.

Synthesis and SAR of 4-(3-hydroxyphenylamino)pyrrolo[2,1-f][1,2,4]triazine based VEGFR-2 kinase inhibitors.

Borzilleri RM, Cai ZW, Ellis C, Fargnoli J, Fura A, Gerhardt T, Goyal B, Hunt JT, Mortillo S, Qian L, Tokarski J, Vyas V, Wautlet B, Zheng X, Bhide RS.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1429-33.

PMID:
15713401
31.

A novel calcium-sensing receptor antagonist transiently stimulates parathyroid hormone secretion in vivo.

Arey BJ, Seethala R, Ma Z, Fura A, Morin J, Swartz J, Vyas V, Yang W, Dickson JK Jr, Feyen JH.

Endocrinology. 2005 Apr;146(4):2015-22. Epub 2005 Jan 6.

PMID:
15637285
32.

Discovering drugs through biological transformation: role of pharmacologically active metabolites in drug discovery.

Fura A, Shu YZ, Zhu M, Hanson RL, Roongta V, Humphreys WG.

J Med Chem. 2004 Aug 26;47(18):4339-51. Review. No abstract available.

PMID:
15317447
33.

Shift in pH of biological fluids during storage and processing: effect on bioanalysis.

Fura A, Harper TW, Zhang H, Fung L, Shyu WC.

J Pharm Biomed Anal. 2003 Jul 14;32(3):513-22.

PMID:
14565556
35.

Angle-resolved neutralization-reionization mass spectrometry.

Fura A, Turecek F, McLafferty FW.

J Am Soc Mass Spectrom. 1991 Dec;2(6):492-6. doi: 10.1016/1044-0305(91)80037-8.

PMID:
24242772
36.

Protonated ethanol and its neutral counterparts.

Wesdemiotis C, Fura A, McLafferty FW.

J Am Soc Mass Spectrom. 1991 Dec;2(6):459-63. doi: 10.1016/1044-0305(91)80031-2.

PMID:
24242766
37.

[Dental caries and periodontal diseases and immunological responses in patients with hemophilia].

Cyprysiak G, Górska R, Mikulska B, Kwiatkowska A, Fura A, Ruszkowska I.

Czas Stomatol. 1985 Nov-Dec;38(11-12):737-43. Polish. No abstract available.

PMID:
3870368

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