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Items: 33

1.

Discovery of a First-in-Class Receptor Interacting Protein 2 (RIP2) Kinase Specific Clinical Candidate, 2-((4-(Benzo[d]thiazol-5-ylamino)-6-(tert-butylsulfonyl)quinazolin-7-yl)oxy)ethyl Dihydrogen Phosphate, for the Treatment of Inflammatory Diseases.

Haile PA, Casillas LN, Votta BJ, Wang GZ, Charnley AK, Dong X, Bury MJ, Romano JJ, Mehlmann JF, King BW, Erhard KF, Hanning CR, Lipshutz DB, Desai BM, Capriotti CA, Schaeffer MC, Berger SB, Mahajan MK, Reilly MA, Nagilla R, Rivera EJ, Sun HH, Kenna JK, Beal AM, Ouellette MT, Kelly M, Stemp G, Convery MA, Vossenkämper A, MacDonald TT, Gough PJ, Bertin J, Marquis RW.

J Med Chem. 2019 Jul 25;62(14):6482-6494. doi: 10.1021/acs.jmedchem.9b00575. Epub 2019 Jul 2.

PMID:
31265286
2.

Discovery of a Novel 2,6-Disubstituted Glucosamine Series of Potent and Selective Hexokinase 2 Inhibitors.

Lin H, Zeng J, Xie R, Schulz MJ, Tedesco R, Qu J, Erhard KF, Mack JF, Raha K, Rendina AR, Szewczuk LM, Kratz PM, Jurewicz AJ, Cecconie T, Martens S, McDevitt PJ, Martin JD, Chen SB, Jiang Y, Nickels L, Schwartz BJ, Smallwood A, Zhao B, Campobasso N, Qian Y, Briand J, Rominger CM, Oleykowski C, Hardwicke MA, Luengo JI.

ACS Med Chem Lett. 2015 Dec 28;7(3):217-22. doi: 10.1021/acsmedchemlett.5b00214. eCollection 2016 Mar 10.

3.

Nascent transcription affected by RNA polymerase IV in Zea mays.

Erhard KF Jr, Talbot JE, Deans NC, McClish AE, Hollick JB.

Genetics. 2015 Apr;199(4):1107-25. doi: 10.1534/genetics.115.174714. Epub 2015 Feb 4.

4.

Maize RNA polymerase IV defines trans-generational epigenetic variation.

Erhard KF Jr, Parkinson SE, Gross SM, Barbour JE, Lim JP, Hollick JB.

Plant Cell. 2013 Mar;25(3):808-19. doi: 10.1105/tpc.112.107680. Epub 2013 Mar 19.

5.

Paramutation: a process for acquiring trans-generational regulatory states.

Erhard KF Jr, Hollick JB.

Curr Opin Plant Biol. 2011 Apr;14(2):210-6. doi: 10.1016/j.pbi.2011.02.005. Epub 2011 Mar 17. Review.

PMID:
21420347
6.

Ectopic T cell receptor-α locus control region activity in B cells is suppressed by direct linkage to two flanking genes at once.

Knirr S, Gomos-Klein J, Andino BE, Harrow F, Erhard KF, Kovalovsky D, Sant'Angelo DB, Ortiz BD.

PLoS One. 2010 Nov 22;5(11):e15527. doi: 10.1371/journal.pone.0015527.

7.

Diversity of Pol IV function is defined by mutations at the maize rmr7 locus.

Stonaker JL, Lim JP, Erhard KF Jr, Hollick JB.

PLoS Genet. 2009 Nov;5(11):e1000706. doi: 10.1371/journal.pgen.1000706. Epub 2009 Nov 20.

8.

Production and processing of siRNA precursor transcripts from the highly repetitive maize genome.

Hale CJ, Erhard KF Jr, Lisch D, Hollick JB.

PLoS Genet. 2009 Aug;5(8):e1000598. doi: 10.1371/journal.pgen.1000598. Epub 2009 Aug 14.

9.

RNA polymerase IV functions in paramutation in Zea mays.

Erhard KF Jr, Stonaker JL, Parkinson SE, Lim JP, Hale CJ, Hollick JB.

Science. 2009 Feb 27;323(5918):1201-5. doi: 10.1126/science.1164508.

10.

Benzyl 2-cyano-3,3-dimethyl-1-pyrrolidinecarboxylate, a versatile intermediate for the synthesis of 3,3-dimethylproline derivatives.

Medina JR, Blackledge CW, Erhard KF, Axten JM, Miller WH.

J Org Chem. 2008 May 16;73(10):3946-9. doi: 10.1021/jo7027163. Epub 2008 Apr 23.

PMID:
18429635
11.

2-Aminomethyl piperidines as novel urotensin-II receptor antagonists.

Jin J, Wang Y, Wang F, Shi D, Erhard KF, Wu Z, Guida BF, Lawrence SK, Behm DJ, Disa J, Vaidya KS, Evans C, McMillan LJ, Rivero RA, Neeb MJ, Douglas SA.

Bioorg Med Chem Lett. 2008 May 1;18(9):2860-4. doi: 10.1016/j.bmcl.2008.03.078. Epub 2008 Apr 8.

PMID:
18420409
12.

Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.

Yamashita DS, Marquis RW, Xie R, Nidamarthy SD, Oh HJ, Jeong JU, Erhard KF, Ward KW, Roethke TJ, Smith BR, Cheng HY, Geng X, Lin F, Offen PH, Wang B, Nevins N, Head MS, Haltiwanger RC, Narducci Sarjeant AA, Liable-Sands LM, Zhao B, Smith WW, Janson CA, Gao E, Tomaszek T, McQueney M, James IE, Gress CJ, Zembryki DL, Lark MW, Veber DF.

J Med Chem. 2006 Mar 9;49(5):1597-612.

PMID:
16509577
13.

Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists.

Miller WH, Manley PJ, Cousins RD, Erhard KF, Heerding DA, Kwon C, Ross ST, Samanen JM, Takata DT, Uzinskas IN, Yuan CC, Haltiwanger RC, Gress CJ, Lark MW, Hwang SM, James IE, Rieman DJ, Willette RN, Yue TL, Azzarano LM, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF.

Bioorg Med Chem Lett. 2003 Apr 17;13(8):1483-6.

PMID:
12668017
14.

Potent and selective inhibition of human cathepsin K leads to inhibition of bone resorption in vivo in a nonhuman primate.

Stroup GB, Lark MW, Veber DF, Bhattacharyya A, Blake S, Dare LC, Erhard KF, Hoffman SJ, James IE, Marquis RW, Ru Y, Vasko-Moser JA, Smith BR, Tomaszek T, Gowen M.

J Bone Miner Res. 2001 Oct;16(10):1739-46.

15.

Identification of a selective nonpeptide antagonist of the anaphylatoxin C3a receptor that demonstrates antiinflammatory activity in animal models.

Ames RS, Lee D, Foley JJ, Jurewicz AJ, Tornetta MA, Bautsch W, Settmacher B, Klos A, Erhard KF, Cousins RD, Sulpizio AC, Hieble JP, McCafferty G, Ward KW, Adams JL, Bondinell WE, Underwood DC, Osborn RR, Badger AM, Sarau HM.

J Immunol. 2001 May 15;166(10):6341-8.

16.

Azepanone-based inhibitors of human and rat cathepsin K.

Marquis RW, Ru Y, LoCastro SM, Zeng J, Yamashita DS, Oh HJ, Erhard KF, Davis LD, Tomaszek TA, Tew D, Salyers K, Proksch J, Ward K, Smith B, Levy M, Cummings MD, Haltiwanger RC, Trescher G, Wang B, Hemling ME, Quinn CJ, Cheng HY, Lin F, Smith WW, Janson CA, Zhao B, McQueney MS, D'Alessio K, Lee CP, Marzulli A, Dodds RA, Blake S, Hwang SM, James IE, Gress CJ, Bradley BR, Lark MW, Gowen M, Veber DF.

J Med Chem. 2001 Apr 26;44(9):1380-95.

PMID:
11311061
17.

Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic.

Miller WH, Alberts DP, Bhatnagar PK, Bondinell WE, Callahan JF, Calvo RR, Cousins RD, Erhard KF, Heerding DA, Keenan RM, Kwon C, Manley PJ, Newlander KA, Ross ST, Samanen JM, Uzinskas IN, Venslavsky JW, Yuan CC, Haltiwanger RC, Gowen M, Hwang SM, James IE, Lark MW, Rieman DJ, Stroup GB, Azzarano LM, Salyers KL, Smith BR, Ward KW, Johanson KO, Huffman WF.

J Med Chem. 2000 Jan 13;43(1):22-6. No abstract available.

PMID:
10633035
18.

Design and characterization of orally active Arg-Gly-Asp peptidomimetic vitronectin receptor antagonist SB 265123 for prevention of bone loss in osteoporosis.

Lark MW, Stroup GB, Hwang SM, James IE, Rieman DJ, Drake FH, Bradbeer JN, Mathur A, Erhard KF, Newlander KA, Ross ST, Salyers KL, Smith BR, Miller WH, Huffman WF, Gowen M.

J Pharmacol Exp Ther. 1999 Nov;291(2):612-7.

PMID:
10525079
19.

Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model.

Miller WH, Bondinell WE, Cousins RD, Erhard KF, Jakas DR, Keenan RM, Ku TW, Newlander KA, Ross ST, Haltiwanger RC, Bradbeer J, Drake FH, Gowen M, Hoffman SJ, Hwang SM, James IE, Lark MW, Lechowska B, Rieman DJ, Stroup GB, Vasko-Moser JA, Zembryki DL, Azzarano LM, Adams PC, Huffman WF, et al.

Bioorg Med Chem Lett. 1999 Jul 5;9(13):1807-12.

PMID:
10406646
20.

Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.

Marquis RW, Yamashita DS, Ru Y, LoCastro SM, Oh HJ, Erhard KF, DesJarlais RL, Head MS, Smith WW, Zhao B, Janson CA, Abdel-Meguid SS, Tomaszek TA, Levy MA, Veber DF.

J Med Chem. 1998 Sep 10;41(19):3563-7. No abstract available.

PMID:
9733481
21.

Regulation of stress-induced cytokine production by pyridinylimidazoles; inhibition of CSBP kinase.

Gallagher TF, Seibel GL, Kassis S, Laydon JT, Blumenthal MJ, Lee JC, Lee D, Boehm JC, Fier-Thompson SM, Abt JW, Soreson ME, Smietana JM, Hall RF, Garigipati RS, Bender PE, Erhard KF, Krog AJ, Hofmann GA, Sheldrake PL, McDonnell PC, Kumar S, Young PR, Adams JL.

Bioorg Med Chem. 1997 Jan;5(1):49-64.

PMID:
9043657
22.

Potent non-peptide fibrinogen receptor antagonists which present an alternative pharmacophore.

Ku TW, Miller WH, Bondinell WE, Erhard KF, Keenan RM, Nichols AJ, Peishoff CE, Samanen JM, Wong AS, Huffman WF.

J Med Chem. 1995 Jan 6;38(1):9-12. No abstract available.

PMID:
7837245
23.

Design of a potent and orally active nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist.

Bondinell WE, Keenan RM, Miller WH, Ali FE, Allen AC, de Brosse CW, Eggleston DS, Erhard KF, Haltiwanger RC, Huffman WF, et al.

Bioorg Med Chem. 1994 Sep;2(9):897-908.

PMID:
7712125
24.

1,3-Diarylindan-2-carboxylic acids, potent and selective non-peptide endothelin receptor antagonists.

Elliott JD, Lago MA, Cousins RD, Gao A, Leber JD, Erhard KF, Nambi P, Elshourbagy NA, Kumar C, Lee JA, et al.

J Med Chem. 1994 May 27;37(11):1553-7. No abstract available.

PMID:
8201588
25.

The crystal structure, absolute configuration, and phosphodiesterase inhibitory activity of (+)-1-(4-bromobenzyl)-4-(3-(cyclopentyloxy)- 4-methoxyphenyl)-pyrrolidin-2-one.

Baures PW, Eggleston DS, Erhard KF, Cieslinski LB, Torphy TJ, Christensen SB.

J Med Chem. 1993 Oct 29;36(22):3274-7.

PMID:
8230117
26.

Direct high-performance liquid chromatographic separation of enantiomeric peptidoleukotriene antagonists.

Chen TK, Erhard KF, Last T, Eggleston DS, Ho MY.

J Chromatogr. 1992 Apr 3;596(1):123-6.

PMID:
1522175
27.

Identification of fenoldopam prodrugs with prolonged renal vasodilator activity.

Brooks DP, DePalma PD, Cyronak MJ, Bryant MA, Karpinski K, Mico B, Gaitanopoulos DE, Chambers PA, Erhard KF, Weinstock J.

J Pharmacol Exp Ther. 1990 Sep;254(3):1084-9.

PMID:
1975620
28.

Purification of leukotriene B4 by semi-preparative high-performance liquid chromatography.

Erhard KF, Razgaitis KA, Bender PE.

J Chromatogr. 1987 Jul 10;398:360-5. No abstract available.

PMID:
2821042
29.

High-affinity leukotriene receptor antagonists. Synthesis and pharmacological characterization of 2-hydroxy-3-[(2-carboxyethyl)thio]-3-[2-(8-phenyloctyl)phenyl] propanoic acid.

Gleason JG, Hall RF, Perchonock CD, Erhard KF, Frazee JS, Ku TW, Kondrad K, McCarthy ME, Mong S, Crooke ST, et al.

J Med Chem. 1987 Jun;30(6):959-61. No abstract available.

PMID:
3035179
30.

Pharmacologic profile of SK&F 104353, a novel, highly potent and selective peptidoleukotriene antagonist.

Wasserman MA, Torphy TJ, Hay DW, Muccitelli RM, Tucker SS, Wilson KA, Osborn RR, Vickery-Clark L, Hall RF, Erhard KF, et al.

Adv Prostaglandin Thromboxane Leukot Res. 1987;17A:532-5. No abstract available.

PMID:
2821765
31.

Synthesis and structure-activity relationship studies of a series of 5-aryl-4,6-dithianonanedioic acids and related compounds: a novel class of leukotriene antagonists.

Perchonock CD, Uzinskas I, McCarthy ME, Erhard KF, Gleason JG, Wasserman MA, Muccitelli RM, DeVan JF, Tucker SS, Vickery LM, et al.

J Med Chem. 1986 Aug;29(8):1442-52.

PMID:
3016267
32.

Synthesis and pharmacological characterization of 5-(2-dodecylphenyl)-4,6-dithianonanedioic acid and 5-[2-(8-phenyloctyl)phenyl]-4,6-dithianonanedioic acid: prototypes of a novel class of leukotriene antagonists.

Perchonock CD, McCarthy ME, Erhard KF, Gleason JG, Wasserman MA, Muccitelli RM, DeVan JF, Tucker SS, Vickery LM, Kirchner T, et al.

J Med Chem. 1985 Sep;28(9):1145-7. No abstract available.

PMID:
2993610
33.

Adrenergic agents. 8.1 Synthesis and beta-adrenergic agonist activity of some 3-tert-butylamino-2-(substituted phenyl)-1-propanols.

Jen T, Frazee JS, Schwartz MS, Erhard KF, Kaiser C.

J Med Chem. 1977 Oct;20(10):1263-8.

PMID:
20504

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