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Items: 47

1.

Neutralization of Pathogenic Fungi with Small-Molecule Immunotherapeutics.

Chirkin E, Muthusamy V, Mann P, Roemer T, Nantermet PG, Spiegel DA.

Angew Chem Int Ed Engl. 2017 Oct 9;56(42):13036-13040. doi: 10.1002/anie.201707536. Epub 2017 Sep 11.

PMID:
28793176
2.

Synthesis of Complex Druglike Molecules by the Use of Highly Functionalized Bench-Stable Organozinc Reagents.

Greshock TJ, Moore KP, McClain RT, Bellomo A, Chung CK, Dreher SD, Kutchukian PS, Peng Z, Davies IW, Vachal P, Ellwart M, Manolikakes SM, Knochel P, Nantermet PG.

Angew Chem Int Ed Engl. 2016 Oct 24;55(44):13714-13718. doi: 10.1002/anie.201604652. Epub 2016 Sep 30.

PMID:
27690172
3.

Discovery of MK-8718, an HIV Protease Inhibitor Containing a Novel Morpholine Aspartate Binding Group.

Bungard CJ, Williams PD, Ballard JE, Bennett DJ, Beaulieu C, Bahnck-Teets C, Carroll SS, Chang RK, Dubost DC, Fay JF, Diamond TL, Greshock TJ, Hao L, Holloway MK, Felock PJ, Gesell JJ, Su HP, Manikowski JJ, McKay DJ, Miller M, Min X, Molinaro C, Moradei OM, Nantermet PG, Nadeau C, Sanchez RI, Satyanarayana T, Shipe WD, Singh SK, Truong VL, Vijayasaradhi S, Wiscount CM, Vacca JP, Crane SN, McCauley JA.

ACS Med Chem Lett. 2016 May 9;7(7):702-7. doi: 10.1021/acsmedchemlett.6b00135. eCollection 2016 Jul 14.

4.

Organic chemistry. Nanomole-scale high-throughput chemistry for the synthesis of complex molecules.

Buitrago Santanilla A, Regalado EL, Pereira T, Shevlin M, Bateman K, Campeau LC, Schneeweis J, Berritt S, Shi ZC, Nantermet P, Liu Y, Helmy R, Welch CJ, Vachal P, Davies IW, Cernak T, Dreher SD.

Science. 2015 Jan 2;347(6217):49-53. doi: 10.1126/science.1259203. Epub 2014 Nov 20.

5.

Modeling a crowdsourced definition of molecular complexity.

Sheridan RP, Zorn N, Sherer EC, Campeau LC, Chang CZ, Cumming J, Maddess ML, Nantermet PG, Sinz CJ, O'Shea PD.

J Chem Inf Model. 2014 Jun 23;54(6):1604-16. doi: 10.1021/ci5001778. Epub 2014 May 20.

PMID:
24802889
6.

Attenuation of scratch-induced reactive astrogliosis by novel EphA4 kinase inhibitors.

Parmentier-Batteur S, Finger EN, Krishnan R, Rajapakse HA, Sanders JM, Kandpal G, Zhu H, Moore KP, Regan CP, Sharma S, Hess JF, Williams TM, Reynolds IJ, Vacca JP, Mark RJ, Nantermet PG.

J Neurochem. 2011 Sep;118(6):1016-31. doi: 10.1111/j.1471-4159.2011.07375.x. Epub 2011 Aug 16.

7.

A rate-limiting role for Dickkopf-1 in bone formation and the remediation of bone loss in mouse and primate models of postmenopausal osteoporosis by an experimental therapeutic antibody.

Glantschnig H, Scott K, Hampton R, Wei N, McCracken P, Nantermet P, Zhao JZ, Vitelli S, Huang L, Haytko P, Lu P, Fisher JE, Sandhu P, Cook J, Williams D, Strohl W, Flores O, Kimmel D, Wang F, An Z.

J Pharmacol Exp Ther. 2011 Aug;338(2):568-78. doi: 10.1124/jpet.111.181404. Epub 2011 Apr 29.

PMID:
21531794
8.

Strategies towards improving the pharmacokinetic profile of ε-substituted lysinol-derived HIV protease inhibitors.

Rajapakse HA, Walji AM, Moore KP, Zhu H, Mitra AW, Gregro AR, Tinney E, Burlein C, Touch S, Paton BL, Carroll SS, DiStefano DJ, Lai MT, Grobler JA, Sanchez RI, Williams TM, Vacca JP, Nantermet PG.

ChemMedChem. 2011 Feb 7;6(2):253-7. doi: 10.1002/cmdc.201000395. Epub 2010 Dec 29. No abstract available.

PMID:
21275047
9.

Generation and selection of novel fully human monoclonal antibodies that neutralize Dickkopf-1 (DKK1) inhibitory function in vitro and increase bone mass in vivo.

Glantschnig H, Hampton RA, Lu P, Zhao JZ, Vitelli S, Huang L, Haytko P, Cusick T, Ireland C, Jarantow SW, Ernst R, Wei N, Nantermet P, Scott KR, Fisher JE, Talamo F, Orsatti L, Reszka AA, Sandhu P, Kimmel D, Flores O, Strohl W, An Z, Wang F.

J Biol Chem. 2010 Dec 17;285(51):40135-47. doi: 10.1074/jbc.M110.166892. Epub 2010 Oct 7.

10.

Discovery of the selective androgen receptor modulator MK-0773 using a rational development strategy based on differential transcriptional requirements for androgenic anabolism versus reproductive physiology.

Schmidt A, Kimmel DB, Bai C, Scafonas A, Rutledge S, Vogel RL, McElwee-Witmer S, Chen F, Nantermet PV, Kasparcova V, Leu CT, Zhang HZ, Duggan ME, Gentile MA, Hodor P, Pennypacker B, Masarachia P, Opas EE, Adamski SA, Cusick TE, Wang J, Mitchell HJ, Kim Y, Prueksaritanont T, Perkins JJ, Meissner RS, Hartman GD, Freedman LP, Harada S, Ray WJ.

J Biol Chem. 2010 May 28;285(22):17054-64. doi: 10.1074/jbc.M109.099002. Epub 2010 Mar 31.

11.

SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.

Rajapakse HA, Nantermet PG, Selnick HG, Barrow JC, McGaughey GB, Munshi S, Lindsley SR, Young MB, Ngo PL, Holloway MK, Lai MT, Espeseth AS, Shi XP, Colussi D, Pietrak B, Crouthamel MC, Tugusheva K, Huang Q, Xu M, Simon AJ, Kuo L, Hazuda DJ, Graham S, Vacca JP.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1885-9. doi: 10.1016/j.bmcl.2010.01.137. Epub 2010 Feb 4.

PMID:
20176482
12.

Rapid P1 SAR of brain penetrant tertiary carbinamine derived BACE inhibitors.

Zhu H, Young MB, Nantermet PG, Graham SL, Colussi D, Lai MT, Pietrak B, Price EA, Sankaranarayanan S, Shi XP, Tugusheva K, Holahan MA, Michener MS, Cook JJ, Simon A, Hazuda DJ, Vacca JP, Rajapakse HA.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1779-82. doi: 10.1016/j.bmcl.2010.01.005. Epub 2010 Jan 11.

PMID:
20122828
13.

Identification of anabolic selective androgen receptor modulators with reduced activities in reproductive tissues and sebaceous glands.

Schmidt A, Harada S, Kimmel DB, Bai C, Chen F, Rutledge SJ, Vogel RL, Scafonas A, Gentile MA, Nantermet PV, McElwee-Witmer S, Pennypacker B, Masarachia P, Sahoo SP, Kim Y, Meissner RS, Hartman GD, Duggan ME, Rodan GA, Towler DA, Ray WJ.

J Biol Chem. 2009 Dec 25;284(52):36367-76. doi: 10.1074/jbc.M109.049734. Epub 2009 Oct 21.

14.

Androgen-mediated improvement of body composition and muscle function involves a novel early transcriptional program including IGF1, mechano growth factor, and induction of {beta}-catenin.

Gentile MA, Nantermet PV, Vogel RL, Phillips R, Holder D, Hodor P, Cheng C, Dai H, Freedman LP, Ray WJ.

J Mol Endocrinol. 2010 Jan;44(1):55-73. doi: 10.1677/JME-09-0048. Epub 2009 Sep 2.

PMID:
19726620
15.

Control of rat tail skin temperature regulation by estrogen receptor-beta selective ligand.

Opas EE, Scafonas A, Nantermet PV, Wilkening RR, Birzin ET, Wilkinson H, Colwell LF, Schaeffer JM, Towler DA, Rodan GA, Schmidt A.

Maturitas. 2009 Sep 20;64(1):46-51. doi: 10.1016/j.maturitas.2009.07.007. Epub 2009 Aug 12.

PMID:
19679413
16.

Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).

Mitchell HJ, Dankulich WP, Hartman GD, Prueksaritanont T, Schmidt A, Vogel RL, Bai C, McElwee-Witmer S, Zhang HZ, Chen F, Leu CT, Kimmel DB, Ray WJ, Nantermet P, Gentile MA, Duggan ME, Meissner RS.

J Med Chem. 2009 Aug 13;52(15):4578-81. doi: 10.1021/jm900880r.

PMID:
19606870
17.

Evolution of tertiary carbinamine BACE-1 inhibitors: Abeta reduction in rhesus CSF upon oral dosing.

Nantermet PG, Rajapakse HA, Stanton MG, Stauffer SR, Barrow JC, Gregro AR, Moore KP, Steinbeiser MA, Swestock J, Selnick HG, Graham SL, McGaughey GB, Colussi D, Lai MT, Sankaranarayanan S, Simon AJ, Munshi S, Cook JJ, Holahan MA, Michener MS, Vacca JP.

ChemMedChem. 2009 Jan;4(1):37-40. doi: 10.1002/cmdc.200800308. No abstract available.

PMID:
19085994
18.

First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates.

Sankaranarayanan S, Holahan MA, Colussi D, Crouthamel MC, Devanarayan V, Ellis J, Espeseth A, Gates AT, Graham SL, Gregro AR, Hazuda D, Hochman JH, Holloway K, Jin L, Kahana J, Lai MT, Lineberger J, McGaughey G, Moore KP, Nantermet P, Pietrak B, Price EA, Rajapakse H, Stauffer S, Steinbeiser MA, Seabrook G, Selnick HG, Shi XP, Stanton MG, Swestock J, Tugusheva K, Tyler KX, Vacca JP, Wong J, Wu G, Xu M, Cook JJ, Simon AJ.

J Pharmacol Exp Ther. 2009 Jan;328(1):131-40. doi: 10.1124/jpet.108.143628. Epub 2008 Oct 14.

PMID:
18854490
19.

Gene expression analyses in cynomolgus monkeys provides mechanistic insight into high-density lipoprotein-cholesterol reduction by androgens in primates.

Nantermet P, Harada S, Liu Y, Cheng S, Johnson C, Yu Y, Kimme D, Holder D, Hodor P, Phillips R, Ray WJ.

Endocrinology. 2008 Apr;149(4):1551-61. doi: 10.1210/en.2007-1151. Epub 2008 Jan 10.

PMID:
18187556
20.

Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.

Moore KP, Zhu H, Rajapakse HA, McGaughey GB, Colussi D, Price EA, Sankaranarayanan S, Simon AJ, Pudvah NT, Hochman JH, Allison T, Munshi SK, Graham SL, Vacca JP, Nantermet PG.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5831-5. Epub 2007 Aug 23.

PMID:
17827011
21.

A regulatory circuit mediating convergence between Nurr1 transcriptional regulation and Wnt signaling.

Kitagawa H, Ray WJ, Glantschnig H, Nantermet PV, Yu Y, Leu CT, Harada S, Kato S, Freedman LP.

Mol Cell Biol. 2007 Nov;27(21):7486-96. Epub 2007 Aug 20. Retraction in: Mol Cell Biol. 2014 Mar;34(5):917.

22.

Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.

Stanton MG, Stauffer SR, Gregro AR, Steinbeiser M, Nantermet P, Sankaranarayanan S, Price EA, Wu G, Crouthamel MC, Ellis J, Lai MT, Espeseth AS, Shi XP, Jin L, Colussi D, Pietrak B, Huang Q, Xu M, Simon AJ, Graham SL, Vacca JP, Selnick H.

J Med Chem. 2007 Jul 26;50(15):3431-3. Epub 2007 Jun 21.

PMID:
17583334
23.

Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.

Lindsley SR, Moore KP, Rajapakse HA, Selnick HG, Young MB, Zhu H, Munshi S, Kuo L, McGaughey GB, Colussi D, Crouthamel MC, Lai MT, Pietrak B, Price EA, Sankaranarayanan S, Simon AJ, Seabrook GR, Hazuda DJ, Pudvah NT, Hochman JH, Graham SL, Vacca JP, Nantermet PG.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):4057-61. Epub 2007 Apr 27.

PMID:
17482814
24.

Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation.

Stauffer SR, Stanton MG, Gregro AR, Steinbeiser MA, Shaffer JR, Nantermet PG, Barrow JC, Rittle KE, Collusi D, Espeseth AS, Lai MT, Pietrak BL, Holloway MK, McGaughey GB, Munshi SK, Hochman JH, Simon AJ, Selnick HG, Graham SL, Vacca JP.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1788-92. Epub 2006 Dec 21.

PMID:
17257835
25.

Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).

Rajapakse HA, Nantermet PG, Selnick HG, Munshi S, McGaughey GB, Lindsley SR, Young MB, Lai MT, Espeseth AS, Shi XP, Colussi D, Pietrak B, Crouthamel MC, Tugusheva K, Huang Q, Xu M, Simon AJ, Kuo L, Hazuda DJ, Graham S, Vacca JP.

J Med Chem. 2006 Dec 14;49(25):7270-3.

PMID:
17149856
26.

Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites.

McGaughey GB, Colussi D, Graham SL, Lai MT, Munshi SK, Nantermet PG, Pietrak B, Rajapakse HA, Selnick HG, Stauffer SR, Holloway MK.

Bioorg Med Chem Lett. 2007 Feb 15;17(4):1117-21. Epub 2006 Nov 6.

PMID:
17112725
27.

P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold.

Nantermet PG, Burgey CS, Robinson KA, Pellicore JM, Newton CL, Deng JZ, Selnick HG, Lewis SD, Lucas BJ, Krueger JA, Miller-Stein C, White RB, Wong B, McMasters DR, Wallace AA, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP, Lyle TA.

Bioorg Med Chem Lett. 2005 Jun 2;15(11):2771-5.

PMID:
15911253
28.

9-hydroxyazafluorenes and their use in thrombin inhibitors.

Stauffer KJ, Williams PD, Selnick HG, Nantermet PG, Newton CL, Homnick CF, Zrada MM, Lewis SD, Lucas BJ, Krueger JA, Pietrak BL, Lyle EA, Singh R, Miller-Stein C, White RB, Wong B, Wallace AA, Sitko GR, Cook JJ, Holahan MA, Stranieri-Michener M, Leonard YM, Lynch JJ Jr, McMasters DR, Yan Y.

J Med Chem. 2005 Apr 7;48(7):2282-93.

PMID:
15801822
29.

Androgenic induction of growth and differentiation in the rodent uterus involves the modulation of estrogen-regulated genetic pathways.

Nantermet PV, Masarachia P, Gentile MA, Pennypacker B, Xu J, Holder D, Gerhold D, Towler D, Schmidt A, Kimmel DB, Freedman LP, Harada S, Ray WJ.

Endocrinology. 2005 Feb;146(2):564-78. Epub 2004 Oct 21.

PMID:
15498879
30.

Non-peptidic small-molecule antagonists of the human platelet thrombin receptor PAR-1.

Selnick HG, Barrow JC, Nantermet PG, Connolly TM.

Curr Med Chem Cardiovasc Hematol Agents. 2003 Mar;1(1):47-59. Review.

PMID:
15317290
31.

Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.

Young MB, Barrow JC, Glass KL, Lundell GF, Newton CL, Pellicore JM, Rittle KE, Selnick HG, Stauffer KJ, Vacca JP, Williams PD, Bohn D, Clayton FC, Cook JJ, Krueger JA, Kuo LC, Lewis SD, Lucas BJ, McMasters DR, Miller-Stein C, Pietrak BL, Wallace AA, White RB, Wong B, Yan Y, Nantermet PG.

J Med Chem. 2004 Jun 3;47(12):2995-3008.

PMID:
15163182
32.

Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group.

Nantermet PG, Barrow JC, Lindsley SR, Young M, Mao SS, Carroll S, Bailey C, Bosserman M, Colussi D, McMasters DR, Vacca JP, Selnick HG.

Bioorg Med Chem Lett. 2004 May 3;14(9):2141-5.

PMID:
15080996
33.

Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics.

Barrow JC, Nantermet PG, Stauffer SR, Ngo PL, Steinbeiser MA, Mao SS, Carroll SS, Bailey C, Colussi D, Bosserman M, Burlein C, Cook JJ, Sitko G, Tiller PR, Miller-Stein CM, Rose M, McMasters DR, Vacca JP, Selnick HG.

J Med Chem. 2003 Dec 4;46(25):5294-7.

PMID:
14640538
34.

Identification of genetic pathways activated by the androgen receptor during the induction of proliferation in the ventral prostate gland.

Nantermet PV, Xu J, Yu Y, Hodor P, Holder D, Adamski S, Gentile MA, Kimmel DB, Harada S, Gerhold D, Freedman LP, Ray WJ.

J Biol Chem. 2004 Jan 9;279(2):1310-22. Epub 2003 Oct 23.

35.

Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position.

Rittle KE, Barrow JC, Cutrona KJ, Glass KL, Krueger JA, Kuo LC, Lewis SD, Lucas BJ, McMasters DR, Morrissette MM, Nantermet PG, Newton CL, Sanders WM, Yan Y, Vacca JP, Selnick HG.

Bioorg Med Chem Lett. 2003 Oct 20;13(20):3477-82.

PMID:
14505652
36.

Design and synthesis of potent and selective macrocyclic thrombin inhibitors.

Nantermet PG, Barrow JC, Newton CL, Pellicore JM, Young M, Lewis SD, Lucas BJ, Krueger JA, McMasters DR, Yan Y, Kuo LC, Vacca JP, Selnick HG.

Bioorg Med Chem Lett. 2003 Aug 18;13(16):2781-4.

PMID:
12873514
37.

Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1 N-benzylamides.

Burgey CS, Robinson KA, Lyle TA, Nantermet PG, Selnick HG, Isaacs RC, Lewis SD, Lucas BJ, Krueger JA, Singh R, Miller-Stein C, White RB, Wong B, Lyle EA, Stranieri MT, Cook JJ, McMasters DR, Pellicore JM, Pal S, Wallace AA, Clayton FC, Bohn D, Welsh DC, Lynch JJ Jr, Yan Y, Chen Z, Kuo L, Gardell SJ, Shafer JA, Vacca JP.

Bioorg Med Chem Lett. 2003 Apr 7;13(7):1353-7.

PMID:
12657281
38.

Discovery of a nonpeptidic small molecule antagonist of the human platelet thrombin receptor (PAR-1).

Nantermet PG, Barrow JC, Lundell GF, Pellicore JM, Rittle KE, Young M, Freidinger RM, Connolly TM, Condra C, Karczewski J, Bednar RA, Gaul SL, Gould RJ, Prendergast K, Selnick HG.

Bioorg Med Chem Lett. 2002 Feb 11;12(3):319-23.

PMID:
11814787
39.

Discovery and initial structure-activity relationships of trisubstituted ureas as thrombin receptor (PAR-1) antagonists.

Barrow JC, Nantermet PG, Selnick HG, Glass KL, Ngo PL, Young MB, Pellicore JM, Breslin MJ, Hutchinson JH, Freidinger RM, Condra C, Karczewski J, Bednar RA, Gaul SL, Stern A, Gould R, Connolly TM.

Bioorg Med Chem Lett. 2001 Oct 22;11(20):2691-6.

PMID:
11591503
40.

Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.

Nantermet PG, Barrow JC, Selnick HG, Homnick CF, Freidinger RM, Chang RS, O'Malley SS, Reiss DR, Broten TP, Ransom RW, Pettibone DJ, Olah T, Forray C.

Bioorg Med Chem Lett. 2000 Aug 7;10(15):1625-8.

PMID:
10937710
41.

In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia.

Barrow JC, Nantermet PG, Selnick HG, Glass KL, Rittle KE, Gilbert KF, Steele TG, Homnick CF, Freidinger RM, Ransom RW, Kling P, Reiss D, Broten TP, Schorn TW, Chang RS, O'Malley SS, Olah TV, Ellis JD, Barrish A, Kassahun K, Leppert P, Nagarathnam D, Forray C.

J Med Chem. 2000 Jul 13;43(14):2703-18.

PMID:
10893308
42.

Human HtrA, an evolutionarily conserved serine protease identified as a differentially expressed gene product in osteoarthritic cartilage.

Hu SI, Carozza M, Klein M, Nantermet P, Luk D, Crowl RM.

J Biol Chem. 1998 Dec 18;273(51):34406-12.

43.

The p2 domain of human immunodeficiency virus type 1 Gag regulates sequential proteolytic processing and is required to produce fully infectious virions.

Pettit SC, Moody MD, Wehbie RS, Kaplan AH, Nantermet PV, Klein CA, Swanstrom R.

J Virol. 1994 Dec;68(12):8017-27.

44.
45.

Total synthesis of taxol.

Nicolaou KC, Yang Z, Liu JJ, Ueno H, Nantermet PG, Guy RK, Claiborne CF, Renaud J, Couladouros EA, Paulvannan K, et al.

Nature. 1994 Feb 17;367(6464):630-4.

PMID:
7906395
46.

Analysis of human immunodeficiency virus type 1 nef gene sequences present in vivo.

Shugars DC, Smith MS, Glueck DH, Nantermet PV, Seillier-Moiseiwitsch F, Swanstrom R.

J Virol. 1993 Aug;67(8):4639-50. Erratum in: J Virol 1994 Aug;68(8):5335.

47.

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