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Items: 24

1.

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.

2.

Design, synthesis, and evaluation of phenylglycinols and phenyl amines as agonists of GPR88.

Dzierba CD, Bi Y, Dasgupta B, Hartz RA, Ahuja V, Cianchetta G, Kumi G, Dong L, Aleem S, Fink C, Garcia Y, Green M, Han J, Kwon S, Qiao Y, Wang J, Zhang Y, Liu Y, Zipp G, Liang Z, Burford N, Ferrante M, Bertekap R, Lewis M, Cacace A, Grace J, Wilson A, Nouraldeen A, Westphal R, Kimball D, Carson K, Bronson JJ, Macor JE.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1448-52. doi: 10.1016/j.bmcl.2015.01.036. Epub 2015 Jan 28.

PMID:
25690789
3.

Novel inhibitors of the high-affinity L-proline transporter as potential therapeutic agents for the treatment of cognitive disorders.

Zipp GG, Barbosa J, Green MA, Terranova KM, Fink C, Yu XC, Nouraldeen A, Wilson A, Savelieva K, Lanthorn TH, David Kimball S.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3886-90. doi: 10.1016/j.bmcl.2014.06.049. Epub 2014 Jul 1.

PMID:
25037917
4.

Genetic deletion of Mst1 alters T cell function and protects against autoimmunity.

Salojin KV, Hamman BD, Chang WC, Jhaver KG, Al-Shami A, Crisostomo J, Wilkins C, Digeorge-Foushee AM, Allen J, Patel N, Gopinathan S, Zhou J, Nouraldeen A, Jessop TC, Bagdanoff JT, Augeri DJ, Read R, Vogel P, Swaffield J, Wilson A, Platt KA, Carson KG, Main A, Zambrowicz BP, Oravecz T.

PLoS One. 2014 May 22;9(5):e98151. doi: 10.1371/journal.pone.0098151. eCollection 2014.

5.

Effect of LX4211 on glucose homeostasis and body composition in preclinical models.

Powell DR, DaCosta CM, Smith M, Doree D, Harris A, Buhring L, Heydorn W, Nouraldeen A, Xiong W, Yalamanchili P, Mseeh F, Wilson A, Shadoan M, Zambrowicz B, Ding ZM.

J Pharmacol Exp Ther. 2014 Aug;350(2):232-42. doi: 10.1124/jpet.114.214304. Epub 2014 May 21.

PMID:
24849925
6.

In vivo toxicology of excipients commonly employed in drug discovery in rats.

Gopinathan S, O'Neill E, Rodriguez LA, Champ R, Phillips M, Nouraldeen A, Wendt M, Wilson AGE, Kramer JA.

J Pharmacol Toxicol Methods. 2013 Sep-Oct;68(2):284-295. doi: 10.1016/j.vascn.2013.02.009. Epub 2013 Mar 14.

PMID:
23499653
7.

Evaluation of transporter-mediated hepatic uptake in a non-radioactive high-throughput assay: a study of kinetics, species difference and plasma protein effect.

Li L, Nouraldeen A, Wilson AG.

Xenobiotica. 2013 Mar;43(3):253-62. doi: 10.3109/00498254.2012.713146. Epub 2012 Aug 28.

PMID:
22928802
8.

Development and application of a high-throughput formulation screening strategy for oral administration in drug discovery.

Gopinathan S, Nouraldeen A, Wilson AG.

Future Med Chem. 2010 Sep;2(9):1391-8. doi: 10.4155/fmc.10.204. No abstract available.

9.

Inhibition of sphingosine 1-phosphate lyase for the treatment of rheumatoid arthritis: discovery of (E)-1-(4-((1R,2S,3R)-1,2,3,4-tetrahydroxybutyl)-1H-imidazol-2-yl)ethanone oxime (LX2931) and (1R,2S,3R)-1-(2-(isoxazol-3-yl)-1H-imidazol-4-yl)butane-1,2,3,4-tetraol (LX2932).

Bagdanoff JT, Donoviel MS, Nouraldeen A, Carlsen M, Jessop TC, Tarver J, Aleem S, Dong L, Zhang H, Boteju L, Hazelwood J, Yan J, Bednarz M, Layek S, Owusu IB, Gopinathan S, Moran L, Lai Z, Kramer J, Kimball SD, Yalamanchili P, Heydorn WE, Frazier KS, Brooks B, Brown P, Wilson A, Sonnenburg WK, Main A, Carson KG, Oravecz T, Augeri DJ.

J Med Chem. 2010 Dec 23;53(24):8650-62. doi: 10.1021/jm101183p. Epub 2010 Nov 22.

PMID:
21090716
10.

Early toxicology signal generation in the mouse.

Kramer JA, O'Neill E, Phillips ME, Bruce D, Smith T, Albright MM, Bellum S, Gopinathan S, Heydorn WE, Liu X, Nouraldeen A, Payne BJ, Read R, Vogel P, Yu XQ, Wilson AG.

Toxicol Pathol. 2010 Apr;38(3):452-71. doi: 10.1177/0192623310364025. Epub 2010 Mar 19.

PMID:
20305093
11.

Pharmacokinetic/pharmacodynamic modelling of 2-acetyl-4(5)-tetrahydroxybutyl imidazole-induced peripheral lymphocyte sequestration through increasing lymphoid sphingosine 1-phosphate.

Yu XQ, Kramer J, Moran L, O'Neill E, Nouraldeen A, Oravecz T, Wilson AG.

Xenobiotica. 2010 May;40(5):350-6. doi: 10.3109/00498251003611376.

PMID:
20175664
12.

A new paradigm for improving oral absorption of drugs in discovery: role of physicochemical properties, different excipients and the pharmaceutical scientist.

Wilson AG, Nouraldeen A, Gopinathan S.

Future Med Chem. 2010 Jan;2(1):1-5. doi: 10.4155/fmc.09.146. No abstract available.

13.

Lead optimization and structure-based design of potent and bioavailable deoxycytidine kinase inhibitors.

Jessop TC, Tarver JE, Carlsen M, Xu A, Healy JP, Heim-Riether A, Fu Q, Taylor JA, Augeri DJ, Shen M, Stouch TR, Swanson RV, Tari LW, Hunter M, Hoffman I, Keyes PE, Yu XC, Miranda M, Liu Q, Swaffield JC, David Kimball S, Nouraldeen A, Wilson AG, Foushee AM, Jhaver K, Finch R, Anderson S, Oravecz T, Carson KG.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6784-7. doi: 10.1016/j.bmcl.2009.09.081. Epub 2009 Sep 25.

PMID:
19836232
14.

5-Fluorocytosine derivatives as inhibitors of deoxycytidine kinase.

Tarver JE, Jessop TC, Carlsen M, Augeri DJ, Fu Q, Healy JP, Heim-Riether A, Xu A, Taylor JA, Shen M, Keyes PE, David Kimball S, Yu XC, Miranda M, Liu Q, Swaffield JC, Nouraldeen A, Wilson AG, Finch R, Jhaver K, Foushee AM, Anderson S, Oravecz T, Carson KG.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6780-3. doi: 10.1016/j.bmcl.2009.09.082. Epub 2009 Sep 25.

PMID:
19836229
15.

Novel L-xylose derivatives as selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.

Goodwin NC, Mabon R, Harrison BA, Shadoan MK, Almstead ZY, Xie Y, Healy J, Buhring LM, DaCosta CM, Bardenhagen J, Mseeh F, Liu Q, Nouraldeen A, Wilson AG, Kimball SD, Powell DR, Rawlins DB.

J Med Chem. 2009 Oct 22;52(20):6201-4. doi: 10.1021/jm900951n.

PMID:
19785435
16.

Inhibition of sphingosine-1-phosphate lyase for the treatment of autoimmune disorders.

Bagdanoff JT, Donoviel MS, Nouraldeen A, Tarver J, Fu Q, Carlsen M, Jessop TC, Zhang H, Hazelwood J, Nguyen H, Baugh SD, Gardyan M, Terranova KM, Barbosa J, Yan J, Bednarz M, Layek S, Courtney LF, Taylor J, Digeorge-Foushee AM, Gopinathan S, Bruce D, Smith T, Moran L, O'Neill E, Kramer J, Lai Z, Kimball SD, Liu Q, Sun W, Yu S, Swaffield J, Wilson A, Main A, Carson KG, Oravecz T, Augeri DJ.

J Med Chem. 2009 Jul 9;52(13):3941-53. doi: 10.1021/jm900278w.

PMID:
19489538
17.

Modulation of peripheral serotonin levels by novel tryptophan hydroxylase inhibitors for the potential treatment of functional gastrointestinal disorders.

Shi ZC, Devasagayaraj A, Gu K, Jin H, Marinelli B, Samala L, Scott S, Stouch T, Tunoori A, Wang Y, Zang Y, Zhang C, Kimball SD, Main AJ, Sun W, Yang Q, Nouraldeen A, Yu XQ, Buxton E, Patel S, Nguyen N, Swaffield J, Powell DR, Wilson A, Liu Q.

J Med Chem. 2008 Jul 10;51(13):3684-7. doi: 10.1021/jm800338j. Epub 2008 Jun 17.

PMID:
18557609
18.

Chloroacetonitrile (CAN) induces glutathione depletion and 8-hydroxylation of guanine bases in rat gastric mucosa.

Ahmed AE, Jacob S, Nouraldeen AM.

J Biochem Mol Toxicol. 1999;13(3-4):119-26.

PMID:
10098896
19.
20.

Role of glutathione modulation in acrylonitrile-induced gastric DNA damage in rats.

Ahmed AE, Nouraldeen AM, Abdel-Rahman SZ, Rajaraman S.

Arch Toxicol. 1996;70(10):620-7.

PMID:
8870954
21.

Molecular interaction of [2,3-14C] acrylonitrile with DNA in gastric tissue of rat.

Abdel-Rahman SZ, Nouraldeen AM, Ahmed AE.

J Biochem Toxicol. 1994 Aug;9(4):191-8.

PMID:
7853353
22.

Acrylonitrile-induced reversible inhibition of uridine uptake by isolated rat intestinal epithelial cells.

Abdel-Rahman SZ, Nouraldeen AM, Abo-Elwafa AA, Ahmed AE.

Toxicol In Vitro. 1994 Apr;8(2):139-43.

PMID:
20692899
23.

Effect of glutathione modulation on molecular interaction of [14C]-chloroacetonitrile with maternal and fetal DNA in mice.

Abdel-Aziz AA, Abdel-Rahman SZ, Nouraldeen AM, Shouman SA, Loh JP, Ahmed AE.

Reprod Toxicol. 1993 May-Jun;7(3):263-72.

PMID:
8318758
24.

Pulmonary toxicity of acrylonitrile: covalent interaction and effect on replicative and unscheduled DNA synthesis in the lung.

Ahmed AE, Abdel-Aziz AH, Abdel-Rahman SZ, Haque AK, Nouraldeen AM, Shouman SA.

Toxicology. 1992 Nov 22;76(1):1-14.

PMID:
1475791

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