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Items: 29

1.

Using Target Engagement Biomarkers to Predict Clinical Efficacy of MetAP2 Inhibitors.

Farrell PJ, Zopf CJ, Huang HJ, Balakrishna D, Holub C, Bilakovics J, Fanjul A, Matuszkiewicz J, Plonowski A, Rolzin P, Banerjee U, Ermolieff J, Cheruvallath ZS, McBride C, Bartkowski D, Mazur C, Pachori A, Larson CJ.

J Pharmacol Exp Ther. 2019 Nov;371(2):299-308. doi: 10.1124/jpet.119.259028. Epub 2019 Sep 19.

PMID:
31537613
2.

MetAP2 inhibition increases energy expenditure through direct action on brown adipocytes.

Huang HJ, Holub C, Rolzin P, Bilakovics J, Fanjul A, Satomi Y, Plonowski A, Larson CJ, Farrell PJ.

J Biol Chem. 2019 Jun 14;294(24):9567-9575. doi: 10.1074/jbc.RA118.007302. Epub 2019 May 2.

PMID:
31048375
3.

CX3CL1-Fc treatment prevents atherosclerosis in Ldlr KO mice.

Riopel M, Vassallo M, Ehinger E, Pattison J, Bowden K, Winkels H, Wilson M, de Jong R, Patel S, Balakrishna D, Bilakovics J, Fanjul A, Plonowski A, Larson CJ, Ley K, Cabrales P, Witztum JL, Olefsky JM, Lee YS.

Mol Metab. 2019 Feb;20:89-101. doi: 10.1016/j.molmet.2018.11.011. Epub 2018 Dec 2.

4.

Chronic fractalkine administration improves glucose tolerance and pancreatic endocrine function.

Riopel M, Seo JB, Bandyopadhyay GK, Li P, Wollam J, Chung H, Jung SR, Murphy A, Wilson M, de Jong R, Patel S, Balakrishna D, Bilakovics J, Fanjul A, Plonowski A, Koh DS, Larson CJ, Olefsky JM, Lee YS.

J Clin Invest. 2018 Apr 2;128(4):1458-1470. doi: 10.1172/JCI94330. Epub 2018 Mar 5.

5.

Acute toxicity, bioaccumulation and effects of dietary transfer of silver from brine shrimp exposed to PVP/PEI-coated silver nanoparticles to zebrafish.

Lacave JM, Fanjul Á, Bilbao E, Gutierrez N, Barrio I, Arostegui I, Cajaraville MP, Orbea A.

Comp Biochem Physiol C Toxicol Pharmacol. 2017 Sep;199:69-80. doi: 10.1016/j.cbpc.2017.03.008. Epub 2017 Mar 18.

PMID:
28323199
6.

Structure-based drug design of novel ASK1 inhibitors using an integrated lead optimization strategy.

Gibson TS, Johnson B, Fanjul A, Halkowycz P, Dougan DR, Cole D, Swann S.

Bioorg Med Chem Lett. 2017 Apr 15;27(8):1709-1713. doi: 10.1016/j.bmcl.2017.02.079. Epub 2017 Mar 2.

PMID:
28291695
7.

A novel antiandrogen, Compound 30, suppresses castration-resistant and MDV3100-resistant prostate cancer growth in vitro and in vivo.

Kuruma H, Matsumoto H, Shiota M, Bishop J, Lamoureux F, Thomas C, Briere D, Los G, Gleave M, Fanjul A, Zoubeidi A.

Mol Cancer Ther. 2013 May;12(5):567-76. doi: 10.1158/1535-7163.MCT-12-0798. Epub 2013 Mar 14.

8.

N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites.

Nair SK, Matthews JJ, Cripps SJ, Cheng H, Hoffman JE, Smith C, Kupchinsky S, Siu M, Taylor WD, Wang Y, Johnson TO, Dress KR, Edwards MP, Zhou S, Hosea NA, Lapaglia A, Kang P, Castro A, Ermolieff J, Fanjul A, Vogel JE, Rejto P, Dalvie D.

Bioorg Med Chem Lett. 2013 Apr 15;23(8):2344-8. doi: 10.1016/j.bmcl.2013.02.066. Epub 2013 Feb 24.

PMID:
23489629
9.

Dose-dependent effects of small-molecule antagonists on the genomic landscape of androgen receptor binding.

Zhu Z, Shi M, Hu W, Estrella H, Engebretsen J, Nichols T, Briere D, Hosea N, Los G, Rejto PA, Fanjul A.

BMC Genomics. 2012 Jul 31;13:355. doi: 10.1186/1471-2164-13-355.

10.

From sequence to molecular pathology, and a mechanism driving the neuroendocrine phenotype in prostate cancer.

Lapuk AV, Wu C, Wyatt AW, McPherson A, McConeghy BJ, Brahmbhatt S, Mo F, Zoubeidi A, Anderson S, Bell RH, Haegert A, Shukin R, Wang Y, Fazli L, Hurtado-Coll A, Jones EC, Hach F, Hormozdiari F, Hajirasouliha I, Boutros PC, Bristow RG, Zhao Y, Marra MA, Fanjul A, Maher CA, Chinnaiyan AM, Rubin MA, Beltran H, Sahinalp SC, Gleave ME, Volik SV, Collins CC.

J Pathol. 2012 Jul;227(3):286-97. doi: 10.1002/path.4047.

11.

Design of oxobenzimidazoles and oxindoles as novel androgen receptor antagonists.

Guo C, Pairish M, Linton A, Kephart S, Ornelas M, Nagata A, Burke B, Dong L, Engebretsen J, Fanjul AN.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2572-8. doi: 10.1016/j.bmcl.2012.01.116. Epub 2012 Feb 7.

PMID:
22377517
12.

Discovery of 3-aryloxy-lactam analogs as potent androgen receptor full antagonists for treating castration resistant prostate cancer.

Guo C, Kephart S, Ornelas M, Gonzalez J, Linton A, Pairish M, Nagata A, Greasley S, Elleraas J, Hosea N, Engebretsen J, Fanjul AN.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1230-6. doi: 10.1016/j.bmcl.2011.11.068. Epub 2011 Dec 9.

PMID:
22197140
13.

Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists.

Guo C, Linton A, Kephart S, Ornelas M, Pairish M, Gonzalez J, Greasley S, Nagata A, Burke BJ, Edwards M, Hosea N, Kang P, Hu W, Engebretsen J, Briere D, Shi M, Gukasyan H, Richardson P, Dack K, Underwood T, Johnson P, Morell A, Felstead R, Kuruma H, Matsimoto H, Zoubeidi A, Gleave M, Los G, Fanjul AN.

J Med Chem. 2011 Nov 10;54(21):7693-704. doi: 10.1021/jm201059s. Epub 2011 Oct 7.

PMID:
21936524
14.

The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.

Cheng H, Hoffman J, Le P, Nair SK, Cripps S, Matthews J, Smith C, Yang M, Kupchinsky S, Dress K, Edwards M, Cole B, Walters E, Loh C, Ermolieff J, Fanjul A, Bhat GB, Herrera J, Pauly T, Hosea N, Paderes G, Rejto P.

Bioorg Med Chem Lett. 2010 May 1;20(9):2897-902. doi: 10.1016/j.bmcl.2010.03.032. Epub 2010 Mar 10.

PMID:
20363126
15.

N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275.

Siu M, Johnson TO, Wang Y, Nair SK, Taylor WD, Cripps SJ, Matthews JJ, Edwards MP, Pauly TA, Ermolieff J, Castro A, Hosea NA, LaPaglia A, Fanjul AN, Vogel JE.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3493-7. doi: 10.1016/j.bmcl.2009.05.011. Epub 2009 May 7.

PMID:
19473839
16.

A novel selective 11beta-hydroxysteroid dehydrogenase type 1 inhibitor prevents human adipogenesis.

Bujalska IJ, Gathercole LL, Tomlinson JW, Darimont C, Ermolieff J, Fanjul AN, Rejto PA, Stewart PM.

J Endocrinol. 2008 May;197(2):297-307. doi: 10.1677/JOE-08-0050.

17.
18.

A selective retinoid with high activity against an androgen-resistant prostate cancer cell type.

Lu XP, Fanjul A, Picard N, Shroot B, Pfahl M.

Int J Cancer. 1999 Jan 18;80(2):272-8.

19.

Apoptosis induction and potent antiestrogen receptor-negative breast cancer activity in vivo by a retinoid antagonist.

Fanjul AN, Piedrafita FJ, Al-Shamma H, Pfahl M.

Cancer Res. 1998 Oct 15;58(20):4607-10.

20.

Novel retinoid-related molecules as apoptosis inducers and effective inhibitors of human lung cancer cells in vivo.

Lu XP, Fanjul A, Picard N, Pfahl M, Rungta D, Nared-Hood K, Carter B, Piedrafita J, Tang S, Fabbrizio E, Pfahl M.

Nat Med. 1997 Jun;3(6):686-90.

PMID:
9176499
21.

4-Hydroxyphenyl retinamide is a highly selective activator of retinoid receptors.

Fanjul AN, Delia D, Pierotti MA, Rideout D, Yu JQ, Pfahl M.

J Biol Chem. 1996 Sep 13;271(37):22441-6. Erratum in: J Biol Chem 1996 Dec 27;271(52):33705. Qiu J [corrected to Yu JQ].

22.
23.

A new class of retinoids with selective inhibition of AP-1 inhibits proliferation.

Fanjul A, Dawson MI, Hobbs PD, Jong L, Cameron JF, Harlev E, Graupner G, Lu XP, Pfahl M.

Nature. 1994 Nov 3;372(6501):107-11.

PMID:
7969403
24.

Nuclear retinoid receptors and their mechanism of action.

Pfahl M, Apfel R, Bendik I, Fanjul A, Graupner G, Lee MO, La-Vista N, Lu XP, Piedrafita J, Ortiz MA, et al.

Vitam Horm. 1994;49:327-82. Review. No abstract available.

PMID:
7810073
25.

Retinoic acid receptors and retinoid X receptor-alpha down-regulate the transforming growth factor-beta 1 promoter by antagonizing AP-1 activity.

Salbert G, Fanjul A, Piedrafita FJ, Lu XP, Kim SJ, Tran P, Pfahl M.

Mol Endocrinol. 1993 Oct;7(10):1347-56.

PMID:
8264664
28.

Retinoids selective for retinoid X receptor response pathways.

Lehmann JM, Jong L, Fanjul A, Cameron JF, Lu XP, Haefner P, Dawson MI, Pfahl M.

Science. 1992 Dec 18;258(5090):1944-6.

PMID:
1335166

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