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Items: 1 to 50 of 59

1.

Structure-Guided Design and Procognitive Assessment of a Potent and Selective Phosphodiesterase 2A Inhibitor.

Stachel SJ, Berger R, Nomland AB, Ginnetti AT, Paone DV, Wang D, Puri V, Lange H, Drott J, Lu J, Marcus J, Dwyer MP, Suon S, Uslaner JM, Smith SM.

ACS Med Chem Lett. 2018 Jul 26;9(8):815-820. doi: 10.1021/acsmedchemlett.8b00214. eCollection 2018 Aug 9.

2.

Indole acids as a novel PDE2 inhibitor chemotype that demonstrate pro-cognitive activity in multiple species.

Stachel SJ, Egbertson MS, Wai J, Machacek M, Toolan DM, Swestock J, Eddins DM, Puri V, McGaughey G, Su HP, Perlow D, Wang D, Ma L, Parthasarathy G, Reid JC, Abeywickrema PD, Smith SM, Uslaner JM.

Bioorg Med Chem Lett. 2018 Apr 1;28(6):1122-1126. doi: 10.1016/j.bmcl.2018.01.039. Epub 2018 Feb 10.

PMID:
29534798
3.

The identification of a novel lead class for phosphodiesterase 2 inhibition by fragment-based drug design.

Forster AB, Abeywickrema P, Bunda J, Cox CD, Cabalu TD, Egbertson M, Fay J, Getty K, Hall D, Kornienko M, Lu J, Parthasarathy G, Reid J, Sharma S, Shipe WD, Smith SM, Soisson S, Stachel SJ, Su HP, Wang D, Berger R.

Bioorg Med Chem Lett. 2017 Dec 1;27(23):5167-5171. doi: 10.1016/j.bmcl.2017.10.054. Epub 2017 Oct 23.

PMID:
29113762
4.

Development of a pharmacodynamic biomarker to measure target engagement from inhibition of the NGF-TrkA pathway.

Price EA, Krasowska-Zoladek A, Nanda KK, Stachel SJ, Henze DA.

J Neurosci Methods. 2017 Apr 15;282:34-42. doi: 10.1016/j.jneumeth.2017.03.001. Epub 2017 Mar 7.

PMID:
28279735
5.

Identification and in Vivo Evaluation of Liver X Receptor β-Selective Agonists for the Potential Treatment of Alzheimer's Disease.

Stachel SJ, Zerbinatti C, Rudd MT, Cosden M, Suon S, Nanda KK, Wessner K, DiMuzio J, Maxwell J, Wu Z, Uslaner JM, Michener MS, Szczerba P, Brnardic E, Rada V, Kim Y, Meissner R, Wuelfing P, Yuan Y, Ballard J, Holahan M, Klein DJ, Lu J, Fradera X, Parthasarathy G, Uebele VN, Chen Z, Li Y, Li J, Cooke AJ, Bennett DJ, Bilodeau MT, Renger J.

J Med Chem. 2016 Apr 14;59(7):3489-98. doi: 10.1021/acs.jmedchem.6b00176. Epub 2016 Apr 1.

PMID:
27011007
6.

Methyl-substitution of an iminohydantoin spiropiperidine β-secretase (BACE-1) inhibitor has a profound effect on its potency.

Egbertson M, McGaughey GB, Pitzenberger SM, Stauffer SR, Coburn CA, Stachel SJ, Yang W, Barrow JC, Neilson LA, McWherter M, Perlow D, Fahr B, Munshi S, Allison TJ, Holloway K, Selnick HG, Yang Z, Swestock J, Simon AJ, Sankaranarayanan S, Colussi D, Tugusheva K, Lai MT, Pietrak B, Haugabook S, Jin L, Chen IW, Holahan M, Stranieri-Michener M, Cook JJ, Vacca J, Graham SL.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4812-4819. doi: 10.1016/j.bmcl.2015.06.082. Epub 2015 Jun 29.

PMID:
26195137
7.

Chondroitin sulfate promotes activation of cathepsin K.

Lemaire PA, Huang L, Zhuo Y, Lu J, Bahnck C, Stachel SJ, Carroll SS, Duong LT.

J Biol Chem. 2014 Aug 1;289(31):21562-72. doi: 10.1074/jbc.M114.559898. Epub 2014 Jun 23.

8.

Maximizing diversity from a kinase screen: identification of novel and selective pan-Trk inhibitors for chronic pain.

Stachel SJ, Sanders JM, Henze DA, Rudd MT, Su HP, Li Y, Nanda KK, Egbertson MS, Manley PJ, Jones KL, Brnardic EJ, Green A, Grobler JA, Hanney B, Leitl M, Lai MT, Munshi V, Murphy D, Rickert K, Riley D, Krasowska-Zoladek A, Daley C, Zuck P, Kane SA, Bilodeau MT.

J Med Chem. 2014 Jul 10;57(13):5800-16. doi: 10.1021/jm5006429. Epub 2014 Jun 19.

PMID:
24914455
9.

(E)-Alkenes as replacements of amide bonds: development of novel and potent acyclic CGRP receptor antagonists.

Kim JJ, Wood MR, Stachel SJ, de Leon P, Nomland A, Stump CA, McWherter MA, Schirripa KM, Moore EL, Salvatore CA, Selnick HG.

Bioorg Med Chem Lett. 2014 Jan 1;24(1):258-61. doi: 10.1016/j.bmcl.2013.11.027. Epub 2013 Nov 20.

PMID:
24332093
10.

Discovery of pyrrolidine-based β-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.

Stachel SJ, Steele TG, Petrocchi A, Haugabook SJ, McGaughey G, Katharine Holloway M, Allison T, Munshi S, Zuck P, Colussi D, Tugasheva K, Wolfe A, Graham SL, Vacca JP.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):240-4. doi: 10.1016/j.bmcl.2011.11.024. Epub 2011 Nov 12.

PMID:
22130130
11.

A conformational constraint improves a beta-secretase inhibitor but for an unexpected reason.

Hills ID, Holloway MK, de León P, Nomland A, Zhu H, Rajapakse H, Allison TJ, Munshi SK, Colussi D, Pietrak BL, Toolan D, Haugabook SJ, Graham SL, Stachel SJ.

Bioorg Med Chem Lett. 2009 Sep 1;19(17):4993-5. doi: 10.1016/j.bmcl.2009.07.071. Epub 2009 Jul 17.

PMID:
19640712
12.

Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1.

Stachel SJ, Coburn CA, Rush D, Jones KL, Zhu H, Rajapakse H, Graham SL, Simon A, Katharine Holloway M, Allison TJ, Munshi SK, Espeseth AS, Zuck P, Colussi D, Wolfe A, Pietrak BL, Lai MT, Vacca JP.

Bioorg Med Chem Lett. 2009 Jun 1;19(11):2977-80. doi: 10.1016/j.bmcl.2009.04.033. Epub 2009 Apr 18.

PMID:
19409780
13.

Identification of a small molecule beta-secretase inhibitor that binds without catalytic aspartate engagement.

Steele TG, Hills ID, Nomland AA, de León P, Allison T, McGaughey G, Colussi D, Tugusheva K, Haugabook SJ, Espeseth AS, Zuck P, Graham SL, Stachel SJ.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):17-20. doi: 10.1016/j.bmcl.2008.11.027. Epub 2008 Nov 13.

PMID:
19036583
14.

In vivo beta-secretase 1 inhibition leads to brain Abeta lowering and increased alpha-secretase processing of amyloid precursor protein without effect on neuregulin-1.

Sankaranarayanan S, Price EA, Wu G, Crouthamel MC, Shi XP, Tugusheva K, Tyler KX, Kahana J, Ellis J, Jin L, Steele T, Stachel S, Coburn C, Simon AJ.

J Pharmacol Exp Ther. 2008 Mar;324(3):957-69. Epub 2007 Dec 21.

PMID:
18156464
15.

Inhibitors of pathogen intercellular signals as selective anti-infective compounds.

Lesic B, Lépine F, Déziel E, Zhang J, Zhang Q, Padfield K, Castonguay MH, Milot S, Stachel S, Tzika AA, Tompkins RG, Rahme LG.

PLoS Pathog. 2007 Sep 14;3(9):1229-39.

16.

Evaluating scoring functions for docking and designing beta-secretase inhibitors.

Katharine Holloway M, McGaughey GB, Coburn CA, Stachel SJ, Jones KG, Stanton EL, Gregro AR, Lai MT, Crouthamel MC, Pietrak BL, Munshi SK.

Bioorg Med Chem Lett. 2007 Feb 1;17(3):823-7. Epub 2006 Oct 25.

PMID:
17107793
17.

MvfR, a key Pseudomonas aeruginosa pathogenicity LTTR-class regulatory protein, has dual ligands.

Xiao G, Déziel E, He J, Lépine F, Lesic B, Castonguay MH, Milot S, Tampakaki AP, Stachel SE, Rahme LG.

Mol Microbiol. 2006 Dec;62(6):1689-99.

18.

Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.

Stachel SJ, Coburn CA, Sankaranarayanan S, Price EA, Wu G, Crouthamel M, Pietrak BL, Huang Q, Lineberger J, Espeseth AS, Jin L, Ellis J, Holloway MK, Munshi S, Allison T, Hazuda D, Simon AJ, Graham SL, Vacca JP.

J Med Chem. 2006 Oct 19;49(21):6147-50. Erratum in: J Med Chem. 2006 Nov 30;49(24):7252. Wu, Guoxin [added]; Crouthamel, Michelle [added].

PMID:
17034118
19.

BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.

Coburn CA, Stachel SJ, Jones KG, Steele TG, Rush DM, DiMuzio J, Pietrak BL, Lai MT, Huang Q, Lineberger J, Jin L, Munshi S, Katharine Holloway M, Espeseth A, Simon A, Hazuda D, Graham SL, Vacca JP.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3635-8. Epub 2006 May 11.

PMID:
16690314
20.

Conformationally biased P3 amide replacements of beta-secretase inhibitors.

Stachel SJ, Coburn CA, Steele TG, Crouthamel MC, Pietrak BL, Lai MT, Holloway MK, Munshi SK, Graham SL, Vacca JP.

Bioorg Med Chem Lett. 2006 Feb;16(3):641-4. Epub 2005 Nov 2.

PMID:
16263281
21.

Biochemical and cell-based assays for characterization of BACE-1 inhibitors.

Pietrak BL, Crouthamel MC, Tugusheva K, Lineberger JE, Xu M, DiMuzio JM, Steele T, Espeseth AS, Stachel SJ, Coburn CA, Graham SL, Vacca JP, Shi XP, Simon AJ, Hazuda DJ, Lai MT.

Anal Biochem. 2005 Jul 1;342(1):144-51.

PMID:
15958191
22.

Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).

Stachel SJ, Coburn CA, Steele TG, Jones KG, Loutzenhiser EF, Gregro AR, Rajapakse HA, Lai MT, Crouthamel MC, Xu M, Tugusheva K, Lineberger JE, Pietrak BL, Espeseth AS, Shi XP, Chen-Dodson E, Holloway MK, Munshi S, Simon AJ, Kuo L, Vacca JP.

J Med Chem. 2004 Dec 16;47(26):6447-50.

PMID:
15588077
23.

Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases.

Coburn CA, Stachel SJ, Li YM, Rush DM, Steele TG, Chen-Dodson E, Holloway MK, Xu M, Huang Q, Lai MT, DiMuzio J, Crouthamel MC, Shi XP, Sardana V, Chen Z, Munshi S, Kuo L, Makara GM, Annis DA, Tadikonda PK, Nash HM, Vacca JP, Wang T.

J Med Chem. 2004 Dec 2;47(25):6117-9.

PMID:
15566281
24.

Fluorogenic peptide sequences--transformation of short peptides into fluorophores under ambient photooxidative conditions.

Juskowiak GL, Stachel SJ, Tivitmahaisoon P, Van Vranken DL.

J Am Chem Soc. 2004 Jan 21;126(2):550-6.

PMID:
14719952
25.

Total synthesis as a resource in the discovery of potentially valuable antitumor agents: cycloproparadicicol.

Yamamoto K, Garbaccio RM, Stachel SJ, Solit DB, Chiosis G, Rosen N, Danishefsky SJ.

Angew Chem Int Ed Engl. 2003 Mar 17;42(11):1280-4. No abstract available.

PMID:
12645064
26.

Probing the SAR of dEpoB via chemical synthesis: a total synthesis evaluation of C26-(1,3-dioxolanyl)-12,13-desoxyepothilone B.

Chappell MD, Harris CR, Kuduk SD, Balog A, Wu Z, Zhang F, Lee CB, Stachel SJ, Danishefsky SJ, Chou TC, Guan Y.

J Org Chem. 2002 Nov 1;67(22):7730-6.

PMID:
12398496
27.

Concise asymmetric syntheses of radicicol and monocillin I.

Garbaccio RM, Stachel SJ, Baeschlin DK, Danishefsky SJ.

J Am Chem Soc. 2001 Nov 7;123(44):10903-8.

PMID:
11686693
28.

The epothilones, eleutherobins, and related types of molecules.

Stachel SJ, Biswas K, Danishefsky SJ.

Curr Pharm Des. 2001 Sep;7(13):1277-90. Review.

PMID:
11472267
29.

Insights into long-range structural effects on the stereochemistry of aldol condensations: a practical total synthesis of desoxyepothilone F.

Lee CB, Wu Z, Zhang F, Chappell MD, Stachel SJ, Chou TC, Guan Y, Danishefsky SJ.

J Am Chem Soc. 2001 Jun 6;123(22):5249-59.

PMID:
11457387
30.
31.

On the interactivity of complex synthesis and tumor pharmacology in the drug discovery process: total synthesis and comparative in vivo evaluations of the 15-aza epothilones.

Stachel SJ, Lee CB, Spassova M, Chappell MD, Bornmann WG, Danishefsky SJ, Chou TC, Guan Y.

J Org Chem. 2001 Jun 15;66(12):4369-78.

PMID:
11397179
32.

Total synthesis and antitumor activity of 12,13-desoxyepothilone F: an unexpected solvolysis problem at C15, mediated by remote substitution at C21.

Lee CB, Chou TC, Zhang XG, Wang ZG, Kuduk SD, Chappell MD, Stachel SJ, Danishefsky SJ.

J Org Chem. 2000 Oct 6;65(20):6525-33.

PMID:
11052097
33.

Xotx5b, a new member of the Otx gene family, may be involved in anterior and eye development in Xenopus laevis.

Vignali R, Colombetti S, Lupo G, Zhang W, Stachel S, Harland RM, Barsacchi G.

Mech Dev. 2000 Aug;96(1):3-13.

34.

On the total synthesis and preliminary biological evaluations of 15(R) and 15(S) aza-dEpoB: a Mitsunobu inversion at C15 in pre-epothilone fragments.

Stachel SJ, Chappell MD, Lee CB, Danishefsky SJ, Chou TC, He L, Horwitz SB.

Org Lett. 2000 Jun 1;2(11):1637-9.

PMID:
10841498
35.

En route to a plant scale synthesis of the promising antitumor agent 12,13-desoxyepothilone B.

Chappell MD, Stachel SJ, Lee CB, Danishefsky SJ.

Org Lett. 2000 Jun 1;2(11):1633-6.

PMID:
10841497
36.

The fluorescence of scorpions and cataractogenesis.

Stachel SJ, Stockwell SA, Van Vranken DL.

Chem Biol. 1999 Aug;6(8):531-9.

37.

Manipulation of the C(22)-C(27) region of rapamycin: stability issues and biological implications.

Nelson FC, Stachel SJ, Eng CP, Sehgal SN.

Bioorg Med Chem Lett. 1999 Jan 18;9(2):295-300.

PMID:
10021948
38.

Follistatin and noggin are excluded from the zebrafish organizer.

Bauer H, Meier A, Hild M, Stachel S, Economides A, Hazelett D, Harland RM, Hammerschmidt M.

Dev Biol. 1998 Dec 15;204(2):488-507.

39.

Activin-induced factors maintain goosecoid transcription through a paired homeodomain binding site.

McKendry R, Harland RM, Stachel SE.

Dev Biol. 1998 Dec 1;204(1):172-86.

40.

Stabilization of a C7 equatorial gamma turn in DMSO-d6 by a ditryptophan crosslink.

Stachel SJ, Hu H, Van QN, Shaka AJ, Van Vranken DL.

Bioorg Med Chem. 1998 Sep;6(9):1439-46.

PMID:
9801815
41.

Neural induction by the secreted polypeptide noggin.

Lamb TM, Knecht AK, Smith WC, Stachel SE, Economides AN, Stahl N, Yancopolous GD, Harland RM.

Science. 1993 Oct 29;262(5134):713-8.

PMID:
8235591
42.
43.
44.

Bacteria-yeast conjugation. Generic trans-kingdom sex?

Stachel SE, Zambryski PC.

Nature. 1989 Jul 20;340(6230):190-1. No abstract available.

PMID:
2666855
45.

Cloning of a lymphocyte homing receptor reveals a lectin domain.

Lasky LA, Singer MS, Yednock TA, Dowbenko D, Fennie C, Rodriguez H, Nguyen T, Stachel S, Rosen SD.

Cell. 1989 Mar 24;56(6):1045-55.

PMID:
2647302
46.

Characterization of Agrobacterium tumefaciens virulence proteins induced by the plant factor acetosyringone.

Engström P, Zambryski P, Van Montagu M, Stachel S.

J Mol Biol. 1987 Oct 20;197(4):635-45.

PMID:
3430596
48.

Site-Specific Nick in the T-DNA Border Sequence as a Result of Agrobacterium vir Gene Expression.

Wang K, Stachel SE, Timmerman B, VAN Montagu M, Zambryski PC.

Science. 1987 Jan 30;235(4788):587-91.

PMID:
17758248
49.

Characterization of the virE operon of the Agrobacterium Ti plasmid pTiA6.

Winans SC, Allenza P, Stachel SE, McBride KE, Nester EW.

Nucleic Acids Res. 1987 Jan 26;15(2):825-37.

50.

A gene essential for Agrobacterium virulence is homologous to a family of positive regulatory loci.

Winans SC, Ebert PR, Stachel SE, Gordon MP, Nester EW.

Proc Natl Acad Sci U S A. 1986 Nov;83(21):8278-82.

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