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Items: 46

1.

A new method for determining levels of sedation in dogs: A pilot study with propofol and a novel neuroactive steroid anesthetic.

Youngblood BL, Ueyama Y, Muir WW, Belfort GM, Hammond RH, Dai J, Salituro FG, Robichaud AJ, Doherty JJ.

J Neurosci Methods. 2018 Jul 15;305:82-88. doi: 10.1016/j.jneumeth.2018.05.006. Epub 2018 May 23.

PMID:
29772269
2.

Discovery of AG-120 (Ivosidenib): A First-in-Class Mutant IDH1 Inhibitor for the Treatment of IDH1 Mutant Cancers.

Popovici-Muller J, Lemieux RM, Artin E, Saunders JO, Salituro FG, Travins J, Cianchetta G, Cai Z, Zhou D, Cui D, Chen P, Straley K, Tobin E, Wang F, David MD, Penard-Lacronique V, Quivoron C, Saada V, de Botton S, Gross S, Dang L, Yang H, Utley L, Chen Y, Kim H, Jin S, Gu Z, Yao G, Luo Z, Lv X, Fang C, Yan L, Olaharski A, Silverman L, Biller S, Su SM, Yen K.

ACS Med Chem Lett. 2018 Jan 19;9(4):300-305. doi: 10.1021/acsmedchemlett.7b00421. eCollection 2018 Apr 12.

3.

Breakthroughs in neuroactive steroid drug discovery.

Blanco MJ, La D, Coughlin Q, Newman CA, Griffin AM, Harrison BL, Salituro FG.

Bioorg Med Chem Lett. 2018 Jan 15;28(2):61-70. doi: 10.1016/j.bmcl.2017.11.043. Epub 2017 Dec 2. Review.

PMID:
29223589
4.

Neuroactive Steroids. 2. 3α-Hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1'-yl)-19-nor-5β-pregnan-20-one (SAGE-217): A Clinical Next Generation Neuroactive Steroid Positive Allosteric Modulator of the (γ-Aminobutyric Acid)A Receptor.

Martinez Botella G, Salituro FG, Harrison BL, Beresis RT, Bai Z, Blanco MJ, Belfort GM, Dai J, Loya CM, Ackley MA, Althaus AL, Grossman SJ, Hoffmann E, Doherty JJ, Robichaud AJ.

J Med Chem. 2017 Sep 28;60(18):7810-7819. doi: 10.1021/acs.jmedchem.7b00846. Epub 2017 Aug 17.

PMID:
28753313
5.

Anticonvulsant profile of the neuroactive steroid, SGE-516, in animal models.

Hammond RS, Althaus AL, Ackley MA, Maciag C, Martinez Botella G, Salituro FG, Robichaud AJ, Doherty JJ.

Epilepsy Res. 2017 Aug;134:16-25. doi: 10.1016/j.eplepsyres.2017.05.001. Epub 2017 May 7.

PMID:
28521115
6.

AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations.

Yen K, Travins J, Wang F, David MD, Artin E, Straley K, Padyana A, Gross S, DeLaBarre B, Tobin E, Chen Y, Nagaraja R, Choe S, Jin L, Konteatis Z, Cianchetta G, Saunders JO, Salituro FG, Quivoron C, Opolon P, Bawa O, Saada V, Paci A, Broutin S, Bernard OA, de Botton S, Marteyn BS, Pilichowska M, Xu Y, Fang C, Jiang F, Wei W, Jin S, Silverman L, Liu W, Yang H, Dang L, Dorsch M, Penard-Lacronique V, Biller SA, Su SM.

Cancer Discov. 2017 May;7(5):478-493. doi: 10.1158/2159-8290.CD-16-1034. Epub 2017 Feb 13.

7.

Rescue of deficient amygdala tonic γ-aminobutyric acidergic currents in the Fmr-/y mouse model of fragile X syndrome by a novel γ-aminobutyric acid type A receptor-positive allosteric modulator.

Martin BS, Martinez-Botella G, Loya CM, Salituro FG, Robichaud AJ, Huntsman MM, Ackley MA, Doherty JJ, Corbin JG.

J Neurosci Res. 2016 Jun;94(6):568-78. doi: 10.1002/jnr.23632. Epub 2015 Aug 26.

8.

Discovery of VX-509 (Decernotinib): A Potent and Selective Janus Kinase 3 Inhibitor for the Treatment of Autoimmune Diseases.

Farmer LJ, Ledeboer MW, Hoock T, Arnost MJ, Bethiel RS, Bennani YL, Black JJ, Brummel CL, Chakilam A, Dorsch WA, Fan B, Cochran JE, Halas S, Harrington EM, Hogan JK, Howe D, Huang H, Jacobs DH, Laitinen LM, Liao S, Mahajan S, Marone V, Martinez-Botella G, McCarthy P, Messersmith D, Namchuk M, Oh L, Penney MS, Pierce AC, Raybuck SA, Rugg A, Salituro FG, Saxena K, Shannon D, Shlyakter D, Swenson L, Tian SK, Town C, Wang J, Wang T, Wannamaker MW, Winquist RJ, Zuccola HJ.

J Med Chem. 2015 Sep 24;58(18):7195-216. doi: 10.1021/acs.jmedchem.5b00301. Epub 2015 Sep 10.

PMID:
26230873
9.

Allopregnanolone preclinical acute pharmacokinetic and pharmacodynamic studies to predict tolerability and efficacy for Alzheimer's disease.

Irwin RW, Solinsky CM, Loya CM, Salituro FG, Rodgers KE, Bauer G, Rogawski MA, Brinton RD.

PLoS One. 2015 Jun 3;10(6):e0128313. doi: 10.1371/journal.pone.0128313. eCollection 2015. Erratum in: PLoS One. 2015;10(6):e0132210.

10.

Neuroactive Steroids. 1. Positive Allosteric Modulators of the (γ-Aminobutyric Acid)A Receptor: Structure-Activity Relationships of Heterocyclic Substitution at C-21.

Martinez Botella G, Salituro FG, Harrison BL, Beresis RT, Bai Z, Shen K, Belfort GM, Loya CM, Ackley MA, Grossman SJ, Hoffmann E, Jia S, Wang J, Doherty JJ, Robichaud AJ.

J Med Chem. 2015 Apr 23;58(8):3500-11. doi: 10.1021/acs.jmedchem.5b00032. Epub 2015 Apr 14.

PMID:
25799373
11.

VX-509 (decernotinib) is a potent and selective janus kinase 3 inhibitor that attenuates inflammation in animal models of autoimmune disease.

Mahajan S, Hogan JK, Shlyakhter D, Oh L, Salituro FG, Farmer L, Hoock TC.

J Pharmacol Exp Ther. 2015 May;353(2):405-14. doi: 10.1124/jpet.114.221176. Epub 2015 Mar 11.

PMID:
25762693
12.

Discovery of a novel, first-in-class, orally bioavailable azaindole inhibitor (VX-787) of influenza PB2.

Clark MP, Ledeboer MW, Davies I, Byrn RA, Jones SM, Perola E, Tsai A, Jacobs M, Nti-Addae K, Bandarage UK, Boyd MJ, Bethiel RS, Court JJ, Deng H, Duffy JP, Dorsch WA, Farmer LJ, Gao H, Gu W, Jackson K, Jacobs DH, Kennedy JM, Ledford B, Liang J, Maltais F, Murcko M, Wang T, Wannamaker MW, Bennett HB, Leeman JR, McNeil C, Taylor WP, Memmott C, Jiang M, Rijnbrand R, Bral C, Germann U, Nezami A, Zhang Y, Salituro FG, Bennani YL, Charifson PS.

J Med Chem. 2014 Aug 14;57(15):6668-78. doi: 10.1021/jm5007275. Epub 2014 Jul 24.

PMID:
25019388
13.

Dual p38/JNK mitogen activated protein kinase inhibitors prevent ozone-induced airway hyperreactivity in guinea pigs.

Verhein KC, Salituro FG, Ledeboer MW, Fryer AD, Jacoby DB.

PLoS One. 2013 Sep 18;8(9):e75351. doi: 10.1371/journal.pone.0075351. eCollection 2013.

14.

Targeted inhibition of mutant IDH2 in leukemia cells induces cellular differentiation.

Wang F, Travins J, DeLaBarre B, Penard-Lacronique V, Schalm S, Hansen E, Straley K, Kernytsky A, Liu W, Gliser C, Yang H, Gross S, Artin E, Saada V, Mylonas E, Quivoron C, Popovici-Muller J, Saunders JO, Salituro FG, Yan S, Murray S, Wei W, Gao Y, Dang L, Dorsch M, Agresta S, Schenkein DP, Biller SA, Su SM, de Botton S, Yen KE.

Science. 2013 May 3;340(6132):622-6. doi: 10.1126/science.1234769. Epub 2013 Apr 4.

15.

Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo.

Popovici-Muller J, Saunders JO, Salituro FG, Travins JM, Yan S, Zhao F, Gross S, Dang L, Yen KE, Yang H, Straley KS, Jin S, Kunii K, Fantin VR, Zhang S, Pan Q, Shi D, Biller SA, Su SM.

ACS Med Chem Lett. 2012 Sep 17;3(10):850-5. doi: 10.1021/ml300225h. eCollection 2012 Oct 11.

16.

Small molecule activation of PKM2 in cancer cells induces serine auxotrophy.

Kung C, Hixon J, Choe S, Marks K, Gross S, Murphy E, DeLaBarre B, Cianchetta G, Sethumadhavan S, Wang X, Yan S, Gao Y, Fang C, Wei W, Jiang F, Wang S, Qian K, Saunders J, Driggers E, Woo HK, Kunii K, Murray S, Yang H, Yen K, Liu W, Cantley LC, Vander Heiden MG, Su SM, Jin S, Salituro FG, Dang L.

Chem Biol. 2012 Sep 21;19(9):1187-98. doi: 10.1016/j.chembiol.2012.07.021.

17.

Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis.

Anastasiou D, Yu Y, Israelsen WJ, Jiang JK, Boxer MB, Hong BS, Tempel W, Dimov S, Shen M, Jha A, Yang H, Mattaini KR, Metallo CM, Fiske BP, Courtney KD, Malstrom S, Khan TM, Kung C, Skoumbourdis AP, Veith H, Southall N, Walsh MJ, Brimacombe KR, Leister W, Lunt SY, Johnson ZR, Yen KE, Kunii K, Davidson SM, Christofk HR, Austin CP, Inglese J, Harris MH, Asara JM, Stephanopoulos G, Salituro FG, Jin S, Dang L, Auld DS, Park HW, Cantley LC, Thomas CJ, Vander Heiden MG.

Nat Chem Biol. 2012 Oct;8(10):839-47. Erratum in: Nat Chem Biol. 2012 Dec;8(12):1008.

18.

The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor.

Duffy JP, Harrington EM, Salituro FG, Cochran JE, Green J, Gao H, Bemis GW, Evindar G, Galullo VP, Ford PJ, Germann UA, Wilson KP, Bellon SF, Chen G, Taslimi P, Jones P, Huang C, Pazhanisamy S, Wang YM, Murcko MA, Su MS.

ACS Med Chem Lett. 2011 Jul 28;2(10):758-63. doi: 10.1021/ml2001455. eCollection 2011 Oct 13.

19.

Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.

Wang T, Duffy JP, Wang J, Halas S, Salituro FG, Pierce AC, Zuccola HJ, Black JR, Hogan JK, Jepson S, Shlyakter D, Mahajan S, Gu Y, Hoock T, Wood M, Furey BF, Frantz JD, Dauffenbach LM, Germann UA, Fan B, Namchuk M, Bennani YL, Ledeboer MW.

J Med Chem. 2009 Dec 24;52(24):7938-41. doi: 10.1021/jm901383u.

PMID:
20014869
20.

A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors.

Wang T, Ledeboer MW, Duffy JP, Salituro FG, Pierce AC, Zuccola HJ, Block E, Shlyakter D, Hogan JK, Bennani YL.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):153-6. doi: 10.1016/j.bmcl.2009.11.021. Epub 2009 Nov 12. Erratum in: Bioorg Med Chem Lett. 2010 Apr 15;20(8):2684. Salituro, Francesco G [added].

PMID:
19945871
21.

2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.

Ledeboer MW, Pierce AC, Duffy JP, Gao H, Messersmith D, Salituro FG, Nanthakumar S, Come J, Zuccola HJ, Swenson L, Shlyakter D, Mahajan S, Hoock T, Fan B, Tsai WJ, Kolaczkowski E, Carrier S, Hogan JK, Zessis R, Pazhanisamy S, Bennani YL.

Bioorg Med Chem Lett. 2009 Dec 1;19(23):6529-33. doi: 10.1016/j.bmcl.2009.10.053. Epub 2009 Oct 24.

PMID:
19857967
22.

Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK).

Farmer LJ, Bemis G, Britt SD, Cochran J, Connors M, Harrington EM, Hoock T, Markland W, Nanthakumar S, Taslimi P, Ter Haar E, Wang J, Zhaveri D, Salituro FG.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6231-5. doi: 10.1016/j.bmcl.2008.09.106. Epub 2008 Oct 7.

PMID:
18938080
23.

Kinase chemogenomics: targeting the human kinome for target validation and drug discovery.

ter Haar E, Walters WP, Pazhanisamy S, Taslimi P, Pierce AC, Bemis GW, Salituro FG, Harbeson SL.

Mini Rev Med Chem. 2004 Mar;4(3):235-53. Review.

PMID:
15032672
24.

Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds.

Spaltenstein A, Almond MR, Bock WJ, Cleary DG, Furfine ES, Hazen RJ, Kazmierski WM, Salituro FG, Tung RD, Wright LL.

Bioorg Med Chem Lett. 2000 Jun 5;10(11):1159-62.

PMID:
10866371
25.

Inhibitors of p38 MAP kinase: therapeutic intervention in cytokine-mediated diseases.

Salituro FG, Germann UA, Wilson KP, Bemis GW, Fox T, Su MS.

Curr Med Chem. 1999 Sep;6(9):807-23. Review.

PMID:
10495353
26.

Design and synthesis of novel conformationally restricted HIV protease inhibitors.

Salituro FG, Baker CT, Court JJ, Deininger DD, Kim EE, Li B, Novak PM, Rao BG, Pazhanisamy S, Porter MD, Schairer WC, Tung RD.

Bioorg Med Chem Lett. 1998 Dec 15;8(24):3637-42.

PMID:
9934485
27.

Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors.

Baker CT, Salituro FG, Court JJ, Deininger DD, Kim EE, Li B, Novak PM, Rao BG, Pazhanisamy S, Schairer WC, Tung RD.

Bioorg Med Chem Lett. 1998 Dec 15;8(24):3631-6.

PMID:
9934484
28.

Pharmacological characterization of MDL 105,519, an NMDA receptor glycine site antagonist.

Baron BM, Harrison BL, Kehne JH, Schmidt CJ, van Giersbergen PL, White HS, Siegel BW, Senyah Y, McCloskey TC, Fadayel GM, Taylor VL, Murawsky MK, Nyce P, Salituro FG.

Eur J Pharmacol. 1997 Apr 4;323(2-3):181-92.

PMID:
9128837
29.
30.

Depletion of estrogen receptor in human breast tumor cells by a novel substituted indole that does not bind to the hormone binding domain.

Bitonti AJ, Dumont JA, Salituro FG, McDonald IA, Jarvi ET, Frey LM, Wright PS, Baumann RJ.

J Steroid Biochem Mol Biol. 1996 Apr;58(1):21-30.

PMID:
8809183
31.

MDL 100,458 and MDL 102,288: two potent and selective glycine receptor antagonists with different functional profiles.

Kehne JH, Baron BM, Harrison BL, McCloskey TC, Palfreyman MG, Poirot M, Salituro FG, Siegel BW, Slone AL, Van Giersbergen PL, et al.

Eur J Pharmacol. 1995 Sep 15;284(1-2):109-18.

PMID:
8549613
32.

Multisubstrate inhibition of 4-hydroxybenzoate 3-monooxygenase.

Salituro FG, Demeter DA, Weintraub HJ, Lippert BJ, Resvick RJ, McDonald IA.

J Med Chem. 1994 Nov 25;37(24):4076-8. No abstract available.

PMID:
7990107
33.

Enzyme-activated antagonists of the strychnine-insensitive glycine/NMDA receptor.

Salituro FG, Tomlinson RC, Baron BM, Palfreyman MG, McDonald IA, Schmidt W, Wu HQ, Guidetti P, Schwarcz R.

J Med Chem. 1994 Feb 4;37(3):334-6. No abstract available.

PMID:
8308859
34.

Potent indole- and quinoline-containing N-methyl-D-aspartate antagonists acting at the strychnine-insensitive glycine binding site.

Baron BM, Harrison BL, McDonald IA, Meldrum BS, Palfreyman MG, Salituro FG, Siegel BW, Slone AL, Turner JP, White HS.

J Pharmacol Exp Ther. 1992 Sep;262(3):947-56.

PMID:
1388205
35.

3-(2-Carboxyindol-3-yl)propionic acid-based antagonists of the N-methyl-D-aspartic acid receptor associated glycine binding site.

Salituro FG, Harrison BL, Baron BM, Nyce PL, Stewart KT, Kehne JH, White HS, McDonald IA.

J Med Chem. 1992 May 15;35(10):1791-9.

PMID:
1534125
36.

3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex.

Salituro FG, Harrison BL, Baron BM, Nyce PL, Stewart KT, McDonald IA.

J Med Chem. 1990 Nov;33(11):2944-6. No abstract available.

PMID:
2146391
37.

Activity of 5,7-dichlorokynurenic acid, a potent antagonist at the N-methyl-D-aspartate receptor-associated glycine binding site.

Baron BM, Harrison BL, Miller FP, McDonald IA, Salituro FG, Schmidt CJ, Sorensen SM, White HS, Palfreyman MG.

Mol Pharmacol. 1990 Oct;38(4):554-61.

PMID:
2172769
38.
39.

Inhibition of aspartic proteinases by peptides containing lysine and ornithine side-chain analogues of statine.

Salituro FG, Agarwal N, Hofmann T, Rich DH.

J Med Chem. 1987 Feb;30(2):286-95.

PMID:
3100801
40.

[125I]iododesethyl tamoxifen aziridine: synthesis and covalent labeling of the estrogen receptor with an iodine-labeled affinity label.

Salituro FG, Carlson KE, Elliston JF, Katzenellenbogen BS, Katzenellenbogen JA.

Steroids. 1986 Nov-Dec;48(5-6):287-313.

PMID:
3445283
41.

Pepsin-catalysed addition of water to a ketomethylene peptide isostere: observation of the tetrahedral species by 13C-nuclear-magnetic-resonance spectroscopy.

Holladay MW, Salituro FG, Schmidt PG, Rich DH.

Biochem Soc Trans. 1985 Dec;13(6):1046-8. No abstract available.

PMID:
3937753
42.

Inhibition of aspartic proteases by pepstatin and 3-methylstatine derivatives of pepstatin. Evidence for collected-substrate enzyme inhibition.

Rich DH, Bernatowicz MS, Agarwal NS, Kawai M, Salituro FG, Schmidt PG.

Biochemistry. 1985 Jun 18;24(13):3165-73.

PMID:
3927973
43.
44.
45.

Sensitive enzyme assays based on the production of chemiluminescent leaving groups.

Branchini BR, Hermes JD, Salituro FG, Post NJ, Claeson G.

Anal Biochem. 1981 Feb;111(1):87-96. No abstract available.

PMID:
7235245
46.

Highly sensitive assays for proteinases using immobilized luminogenic substrates.

Branchini BR, Salituro FG, Hermes JD, Post NJ.

Biochem Biophys Res Commun. 1980 Nov 17;97(1):334-9. No abstract available.

PMID:
7006607

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