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Items: 39

1.

Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy.

Miller MM, Banville J, Friends TJ, Gagnon M, Hangeland JJ, Lavallée JF, Martel A, O'Grady H, Rémillard R, Ruediger E, Tremblay F, Posy SL, Allegretto NJ, Guarino VR, Harden DG, Harper TW, Hartl K, Josephs J, Malmstrom S, Watson C, Yang Y, Zhang G, Wong P, Yang J, Bouvier M, Seiffert DA, Wexler RR, Lawrence RM, Priestley ES, Marinier A.

J Med Chem. 2019 Aug 22;62(16):7400-7416. doi: 10.1021/acs.jmedchem.9b00186. Epub 2019 Aug 5.

PMID:
31246024
2.

Triazolopyrimidines identified as reversible myeloperoxidase inhibitors.

Duclos F, Abell LM, Harden DG, Pike K, Nowak K, Locke GA, Duke GJ, Liu X, Fernando G, Shaw SA, Vokits BP, Wurtz NR, Viet A, Valente MN, Stachura S, Sleph P, Khan JA, Gao J, Dongre AR, Zhao L, Wexler RR, Gordon DA, Kick EK.

Medchemcomm. 2017 Oct 26;8(11):2093-2099. doi: 10.1039/c7md00268h. eCollection 2017 Nov 1.

3.

Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding.

Wong PC, Seiffert D, Bird JE, Watson CA, Bostwick JS, Giancarli M, Allegretto N, Hua J, Harden D, Guay J, Callejo M, Miller MM, Lawrence RM, Banville J, Guy J, Maxwell BD, Priestley ES, Marinier A, Wexler RR, Bouvier M, Gordon DA, Schumacher WA, Yang J.

Sci Transl Med. 2017 Jan 4;9(371). pii: eaaf5294. doi: 10.1126/scitranslmed.aaf5294.

PMID:
28053157
4.

A Small Molecule Inhibitor Selectively Induces Apoptosis in Cells Transformed by High Risk Human Papilloma Viruses.

Sheaffer AK, Lee MS, Qi H, Chaniewski S, Zheng X, Farr GA, Esposito K, Harden D, Lei M, Schweizer L, Friborg J, Agler M, McPhee F, Gentles R, Beno BR, Chupak L, Mason S.

PLoS One. 2016 Jun 9;11(6):e0155909. doi: 10.1371/journal.pone.0155909. eCollection 2016.

5.

Just-in-Time Compound Pooling Increases Primary Screening Capacity without Compromising Screening Quality.

Elkin LL, Harden DG, Saldanha S, Ferguson H, Cheney DL, Pieniazek SN, Maloney DP, Zewinski J, O'Connell J, Banks M.

J Biomol Screen. 2015 Jun;20(5):577-87. doi: 10.1177/1087057115572988. Epub 2015 Feb 26.

PMID:
25722344
6.

Identification and Preclinical Pharmacology of the γ-Secretase Modulator BMS-869780.

Toyn JH, Thompson LA, Lentz KA, Meredith JE Jr, Burton CR, Sankaranararyanan S, Guss V, Hall T, Iben LG, Krause CM, Krause R, Lin XA, Pierdomenico M, Polson C, Robertson AS, Denton RR, Grace JE, Morrison J, Raybon J, Zhuo X, Snow K, Padmanabha R, Agler M, Esposito K, Harden D, Prack M, Varma S, Wong V, Zhu Y, Zvyaga T, Gerritz S, Marcin LR, Higgins MA, Shi J, Wei C, Cantone JL, Drexler DM, Macor JE, Olson RE, Ahlijanian MK, Albright CF.

Int J Alzheimers Dis. 2014;2014:431858. doi: 10.1155/2014/431858. Epub 2014 Jul 8.

7.

In vitro Characterization of a small molecule inhibitor of the alanine serine cysteine transporter -1 (SLC7A10).

Brown JM, Hunihan L, Prack MM, Harden DG, Bronson J, Dzierba CD, Gentles RG, Hendricson A, Krause R, Macor JE, Westphal RS.

J Neurochem. 2014 Apr;129(2):275-83. doi: 10.1111/jnc.12618. Epub 2013 Dec 10.

8.

Identification of small molecules that selectively inhibit diacylglycerol lipase-α activity.

Appiah KK, Blat Y, Robertson BJ, Pearce BC, Pedicord DL, Gentles RG, Yu XC, Mseeh F, Nguyen N, Swaffield JC, Harden DG, Westphal RS, Banks MN, O'Connell JC.

J Biomol Screen. 2014 Apr;19(4):595-605. doi: 10.1177/1087057113511111. Epub 2013 Nov 15.

PMID:
24241710
9.

Discovery of (S,E)-3-(2-fluorophenyl)-N-(1-(3-(pyridin-3-yloxy)phenyl)ethyl)-acrylamide as a potent and efficacious KCNQ2 (Kv7.2) opener for the treatment of neuropathic pain.

Wu YJ, Conway CM, Sun LQ, Machet F, Chen J, Chen P, He H, Bourin C, Calandra V, Polino JL, Davis CD, Heman K, Gribkoff VK, Boissard CG, Knox RJ, Thompson MW, Fitzpatrick W, Weaver D, Harden DG, Natale J, Dworetzky SI, Starrett JE Jr.

Bioorg Med Chem Lett. 2013 Nov 15;23(22):6188-91. doi: 10.1016/j.bmcl.2013.08.092. Epub 2013 Sep 8.

PMID:
24070783
10.

Discovery of a novel series of quinolone α7 nicotinic acetylcholine receptor agonists.

McDonald IM, Mate RA, Zusi FC, Huang H, Post-Munson DJ, Ferrante MA, Gallagher L, Bertekap RL Jr, Knox RJ, Robertson BJ, Harden DG, Morgan DG, Lodge NJ, Dworetzky SI, Olson RE, Macor JE.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1684-8. doi: 10.1016/j.bmcl.2013.01.070. Epub 2013 Jan 29.

PMID:
23414838
11.

Development of industrially feasible concentrated 30% and 40% nanoemulsions for intravenous drug delivery.

Müller RH, Harden D, Keck CM.

Drug Dev Ind Pharm. 2012 Apr;38(4):420-30. doi: 10.3109/03639045.2011.608681. Epub 2011 Nov 16.

PMID:
22088169
12.

Reduced cytotoxicity of polyhexamethylene biguanide hydrochloride (PHMB) by egg phosphatidylcholine while maintaining antimicrobial efficacy.

Müller G, Kramer A, Schmitt J, Harden D, Koburger T.

Chem Biol Interact. 2011 Apr 25;190(2-3):171-8. doi: 10.1016/j.cbi.2011.02.024. Epub 2011 Feb 26.

PMID:
21356204
13.

Preliminary SAR studies on non-apamin-displacing 4-(aminomethylaryl)pyrrazolopyrimidine K(Ca) channel blockers.

Gentles RG, Hu S, Huang Y, Grant-Young K, Poss MA, Andres C, Fiedler T, Knox R, Lodge N, Weaver CD, Harden DG.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5694-7. doi: 10.1016/j.bmcl.2008.08.026. Epub 2008 Aug 14.

PMID:
18824351
14.

Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.

Gentles RG, Grant-Young K, Hu S, Huang Y, Poss MA, Andres C, Fiedler T, Knox R, Lodge N, Weaver CD, Harden DG.

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5316-9. doi: 10.1016/j.bmcl.2008.08.023. Epub 2008 Aug 14.

PMID:
18774291
15.

Characterization of the 5-HT2b receptor in evaluation of aequorin detection of calcium mobilization for miniaturized GPCR high-throughput screening.

Gilchrist MA 2nd, Cacace A, Harden DG.

J Biomol Screen. 2008 Jul;13(6):486-93. doi: 10.1177/1087057108319212. Epub 2008 Jun 19.

PMID:
18566482
16.

A thallium-sensitive, fluorescence-based assay for detecting and characterizing potassium channel modulators in mammalian cells.

Weaver CD, Harden D, Dworetzky SI, Robertson B, Knox RJ.

J Biomol Screen. 2004 Dec;9(8):671-7.

PMID:
15634793
17.

BL-1249 [(5,6,7,8-tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine]: a putative potassium channel opener with bladder-relaxant properties.

Tertyshnikova S, Knox RJ, Plym MJ, Thalody G, Griffin C, Neelands T, Harden DG, Signor L, Weaver D, Myers RA, Lodge NJ.

J Pharmacol Exp Ther. 2005 Apr;313(1):250-9. Epub 2004 Dec 17.

PMID:
15608074
18.

(S,E)-N-[1-(3-heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: synthesis and KCNQ2 potassium channel opener activity.

L'Heureux A, Martel A, He H, Chen J, Sun LQ, Starrett JE, Natale J, Dworetzky SI, Knox RJ, Harden DG, Weaver D, Thompson MW, Wu YJ.

Bioorg Med Chem Lett. 2005 Jan 17;15(2):363-6.

PMID:
15603955
19.

Synthesis and KCNQ2 opener activity of N-(1-benzo[1,3]dioxol-5-yl-ethyl, N-[1-(2,3-dihydro-benzofuran-5-yl)-ethyl, and N-[1-(2,3-dihydro-1H-indol-5-yl)-ethyl acrylamides.

Wu YJ, Sun LQ, He H, Chen J, Starrett JE Jr, Dextraze P, Daris JP, Boissard CG, Pieschl RL, Gribkoff VK, Natale J, Knox RJ, Harden DG, Thompson MW, Fitzpatrick W, Weaver D, Wu D, Gao Q, Dworetzky SI.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4533-7.

PMID:
15357987
20.

(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons.

Wu YJ, Boissard CG, Chen J, Fitzpatrick W, Gao Q, Gribkoff VK, Harden DG, He H, Knox RJ, Natale J, Pieschl RL, Starrett JE Jr, Sun LQ, Thompson M, Weaver D, Wu D, Dworetzky SI.

Bioorg Med Chem Lett. 2004 Apr 19;14(8):1991-5.

PMID:
15050644
22.

Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.

Wu YJ, Davis CD, Dworetzky S, Fitzpatrick WC, Harden D, He H, Knox RJ, Newton AE, Philip T, Polson C, Sivarao DV, Sun LQ, Tertyshnikova S, Weaver D, Yeola S, Zoeckler M, Sinz MW.

J Med Chem. 2003 Aug 28;46(18):3778-81.

PMID:
12930139
23.

(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.

Wu YJ, Boissard CG, Greco C, Gribkoff VK, Harden DG, He H, L'Heureux A, Kang SH, Kinney GG, Knox RJ, Natale J, Newton AE, Lehtinen-Oboma S, Sinz MW, Sivarao DV, Starrett JE Jr, Sun LQ, Tertyshnikova S, Thompson MW, Weaver D, Wong HS, Zhang L, Dworetzky SI.

J Med Chem. 2003 Jul 17;46(15):3197-200.

PMID:
12852750
24.

Teledermatology: an intraobserver diagnostic correlation study, Part II.

Pak HS, Harden D, Cruess D, Welch ML, Poropatich R; National Capital Area Teledermatology Consortium.

Cutis. 2003 Jun;71(6):476-80.

PMID:
12839260
25.

Teledermatology: an intraobserver diagnostic correlation study, part I.

Pak HS, Harden D, Cruess D, Welch ML, Poropatich R; National Capital Area Teledermatology Consortium.

Cutis. 2003 May;71(5):399-403.

PMID:
12769408
26.

Papular and nodular lesions of the scalp, face, and neck.

Harden D, Keeling JH.

Arch Fam Med. 1999 Sep-Oct;8(5):373. No abstract available.

PMID:
10500505
27.
28.

Papular and nodular lesions of the scalp, face, and neck. Secondary syphilis.

Harden D, Keeling JH.

Arch Dermatol. 1997 Aug;133(8):1027, 1030. No abstract available.

PMID:
9267250
30.
32.

Quantitative structure-activity relationship analysis of cation-substituted polyaromatic compounds as potentiators (amplifiers) of bleomycin-mediated degradation of DNA.

Strekowski L, Wilson WD, Mokrosz JL, Mokrosz MJ, Harden DB, Tanious FA, Wydra RL, Crow SA Jr.

J Med Chem. 1991 Feb;34(2):580-8.

PMID:
1704921
33.

Modelling of drug absorption in rabbit intestinal brush border membrane vesicles.

Wood C, Lawrence MJ, Harden D.

Biochem Soc Trans. 1990 Oct;18(5):875-6. No abstract available.

PMID:
2083706
34.

Molecular basis for potentiation of bleomycin-mediated degradation of DNA by polyamines. Experimental and molecular mechanical studies.

Strekowski L, Harden DB, Wydra RL, Stewart KD, Wilson WD.

J Mol Recognit. 1989 Dec;2(4):158-66.

PMID:
2484026
35.

Interaction of unfused tricyclic aromatic cations with DNA: a new class of intercalators.

Wilson WD, Tanious FA, Watson RA, Barton HJ, Strekowska A, Harden DB, Strekowski L.

Biochemistry. 1989 Mar 7;28(5):1984-92.

PMID:
2719941
36.

Molecular basis for bleomycin amplification: conformational and stereoelectronic effects in unfused amplifiers.

Strekowski L, Mokrosz JL, Tanious FA, Watson RA, Harden D, Mokrosz M, Edwards WD, Wilson WD.

J Med Chem. 1988 Jun;31(6):1231-40.

PMID:
2453673
37.

Assessing the driving potential of the handicapped.

Gurgold GD, Harden DH.

Am J Occup Ther. 1978 Jan;32(1):41-6.

PMID:
147010
38.

Device for loading a wheelchair into an automobile trunk.

Harden DH, Nyboer VJ.

Arch Phys Med Rehabil. 1972 Feb;53(2):85-6. No abstract available.

PMID:
5019062
39.

Effects of negative air ions, noise, sex and age on maze learning in rats.

Terry RA, Harden DG, Mayyasi AM.

Int J Biometeorol. 1969 Jun;13(1):39-49. No abstract available.

PMID:
5383469

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