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Items: 34

1.

Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase Inhibitors.

Grimster NP, Anderson E, Alimzhanov M, Bebernitz G, Bell K, Chuaqui C, Deegan T, Ferguson AD, Gero T, Harsch A, Huszar D, Kawatkar A, Kettle JG, Lyne P, Read JA, Rivard Costa C, Ruston L, Schroeder P, Shi J, Su Q, Throner S, Toader D, Vasbinder M, Woessner R, Wang H, Wu A, Ye M, Zheng W, Zinda M.

J Med Chem. 2018 Jun 28;61(12):5235-5244. doi: 10.1021/acs.jmedchem.8b00076. Epub 2018 Jun 13.

PMID:
29856615
2.

MARK inhibitors: Declaring a No-Go decision on a chemical series based on extensive DMPK experimentation.

Haidle AM, Childers KK, Zabierek AA, Katz JD, Jewell JP, Hou Y, Altman MD, Szewczak A, Chen D, Harsch A, Hayashi M, Warren L, Hutton M, Nuthall H, Stanton MG, Davies IW, Munoz B, Northrup A.

Bioorg Med Chem Lett. 2017 Jan 1;27(1):109-113. doi: 10.1016/j.bmcl.2016.08.066. Epub 2016 Aug 25.

PMID:
27894874
3.

Structure guided design of a series of selective pyrrolopyrimidinone MARK inhibitors.

Katz JD, Haidle A, Childers KK, Zabierek AA, Jewell JP, Hou Y, Altman MD, Szewczak A, Chen D, Harsch A, Hayashi M, Warren L, Hutton M, Nuthall H, Su HP, Munshi S, Stanton MG, Davies IW, Munoz B, Northrup A.

Bioorg Med Chem Lett. 2017 Jan 1;27(1):114-120. doi: 10.1016/j.bmcl.2016.08.068. Epub 2016 Oct 22.

PMID:
27816515
4.

Delayed and Prolonged Histone Hyperacetylation with a Selective HDAC1/HDAC2 Inhibitor.

Methot JL, Hoffman DM, Witter DJ, Stanton MG, Harrington P, Hamblett C, Siliphaivanh P, Wilson K, Hubbs J, Heidebrecht R, Kral AM, Ozerova N, Fleming JC, Wang H, Szewczak AA, Middleton RE, Hughes B, Cruz JC, Haines BB, Chenard M, Kenific CM, Harsch A, Secrist JP, Miller TA.

ACS Med Chem Lett. 2014 Jan 2;5(4):340-5. doi: 10.1021/ml4004233. eCollection 2014 Apr 10.

5.

Characterizing individual differences in functional connectivity using dual-regression and seed-based approaches.

Smith DV, Utevsky AV, Bland AR, Clement N, Clithero JA, Harsch AE, McKell Carter R, Huettel SA.

Neuroimage. 2014 Jul 15;95:1-12. doi: 10.1016/j.neuroimage.2014.03.042. Epub 2014 Mar 21.

6.

Use of flexible bronchoscopy in pediatric patients receiving extracorporeal membrane oxygenation (ECMO) support.

Kamat PP, Popler J, Davis J, Leong T, Piland SC, Simon D, Harsch A, Teague WG, Fortenberry JD.

Pediatr Pulmonol. 2011 Nov;46(11):1108-13. doi: 10.1002/ppul.21480. Epub 2011 Aug 3.

PMID:
21815274
7.

Direct determination of the ratio of unbound fraction in plasma to unbound fraction in microsomal system (fu p/fu mic) for refined prediction of phase I mediated metabolic hepatic clearance.

Deshmukh SV, Harsch A.

J Pharmacol Toxicol Methods. 2011 Jan-Feb;63(1):35-9. doi: 10.1016/j.vascn.2010.04.003. Epub 2010 Apr 28.

PMID:
20433934
8.

Exploring the pharmacokinetic properties of phosphorus-containing selective HDAC 1 and 2 inhibitors (SHI-1:2).

Heidebrecht RW Jr, Chenard M, Close J, Dahlberg WK, Fleming J, Grimm JB, Hamill JE, Harsch A, Haines BB, Hughes B, Kral AM, Middleton RE, Mushti C, Ozerova N, Szewczak AA, Wang H, Wilson K, Witter DJ, Secrist JP, Miller TA.

Bioorg Med Chem Lett. 2009 Apr 1;19(7):2053-8. doi: 10.1016/j.bmcl.2009.02.009. Epub 2009 Feb 8.

PMID:
19268585
9.

Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization.

Kattar SD, Surdi LM, Zabierek A, Methot JL, Middleton RE, Hughes B, Szewczak AA, Dahlberg WK, Kral AM, Ozerova N, Fleming JC, Wang H, Secrist P, Harsch A, Hamill JE, Cruz JC, Kenific CM, Chenard M, Miller TA, Berk SC, Tempest P.

Bioorg Med Chem Lett. 2009 Feb 15;19(4):1168-72. doi: 10.1016/j.bmcl.2008.12.083. Epub 2008 Dec 25.

PMID:
19138845
10.

SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).

Methot JL, Hamblett CL, Mampreian DM, Jung J, Harsch A, Szewczak AA, Dahlberg WK, Middleton RE, Hughes B, Fleming JC, Wang H, Kral AM, Ozerova N, Cruz JC, Haines B, Chenard M, Kenific CM, Secrist JP, Miller TA.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6104-9. doi: 10.1016/j.bmcl.2008.10.052. Epub 2008 Oct 14.

PMID:
18951790
11.

Phenylglycine and phenylalanine derivatives as potent and selective HDAC1 inhibitors (SHI-1).

Wilson KJ, Witter DJ, Grimm JB, Siliphaivanh P, Otte KM, Kral AM, Fleming JC, Harsch A, Hamill JE, Cruz JC, Chenard M, Szewczak AA, Middleton RE, Hughes BL, Dahlberg WK, Secrist JP, Miller TA.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1859-63. doi: 10.1016/j.bmcl.2008.02.012. Epub 2008 Feb 10.

PMID:
18304810
12.

Identification of novel metabolites of colchicine in rat bile facilitated by enhanced online radiometric detection.

Xu L, Adams B, Jeliazkova-Mecheva VV, Trimble L, Kwei G, Harsch A.

Drug Metab Dispos. 2008 Apr;36(4):731-9. doi: 10.1124/dmd.107.019463. Epub 2008 Jan 28.

13.

Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).

Methot JL, Chakravarty PK, Chenard M, Close J, Cruz JC, Dahlberg WK, Fleming J, Hamblett CL, Hamill JE, Harrington P, Harsch A, Heidebrecht R, Hughes B, Jung J, Kenific CM, Kral AM, Meinke PT, Middleton RE, Ozerova N, Sloman DL, Stanton MG, Szewczak AA, Tyagarajan S, Witter DJ, Secrist JP, Miller TA.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):973-8. doi: 10.1016/j.bmcl.2007.12.031. Epub 2008 Jan 7.

PMID:
18182289
14.

The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors.

Hamblett CL, Methot JL, Mampreian DM, Sloman DL, Stanton MG, Kral AM, Fleming JC, Cruz JC, Chenard M, Ozerova N, Hitz AM, Wang H, Deshmukh SV, Nazef N, Harsch A, Hughes B, Dahlberg WK, Szewczak AA, Middleton RE, Mosley RT, Secrist JP, Miller TA.

Bioorg Med Chem Lett. 2007 Oct 1;17(19):5300-9. Epub 2007 Aug 16.

PMID:
17761416
15.

Design of novel histone deacetylase inhibitors.

Siliphaivanh P, Harrington P, Witter DJ, Otte K, Tempest P, Kattar S, Kral AM, Fleming JC, Deshmukh SV, Harsch A, Secrist PJ, Miller TA.

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4619-24. Epub 2007 May 27.

PMID:
17555962
16.

Stimulus history reliably shapes action potential waveforms of cortical neurons.

de Polavieja GG, Harsch A, Kleppe I, Robinson HP, Juusola M.

J Neurosci. 2005 Jun 8;25(23):5657-65.

17.

A 13C NMR approach to categorizing potential limitations of alpha,beta-unsaturated carbonyl systems in drug-like molecules.

Cusack KP, Arnold LD, Barberis CE, Chen H, Ericsson AM, Gaza-Bulseco GS, Gordon TD, Grinnell CM, Harsch A, Pellegrini M, Tarcsa E.

Bioorg Med Chem Lett. 2004 Nov 15;14(22):5503-7.

PMID:
15482913
18.
19.

Stages of spike time variability during neuronal responses to transient inputs.

Robinson HP, Harsch A.

Phys Rev E Stat Nonlin Soft Matter Phys. 2002 Dec;66(6 Pt 1):061902. Epub 2002 Dec 10.

PMID:
12513313
20.

HPLC-MS/MS identification of positionally isomeric benzo[c]phenanthrene diol epoxide adducts in duplex DNA.

Harsch A, Sayer JM, Jerina DM, Vouros P.

Chem Res Toxicol. 2000 Dec;13(12):1342-8.

PMID:
11123977
22.

Pulsed plasma deposition of allylamine on polysiloxane: a stable surface for neuronal cell adhesion.

Harsch A, Calderon J, Timmons RB, Gross GW.

J Neurosci Methods. 2000 Jun 1;98(2):135-44.

PMID:
10880827
23.
24.

Analysis of DNA adducts using high-performance separation techniques coupled to electrospray ionization mass spectrometry.

Andrews CL, Vouros P, Harsch A.

J Chromatogr A. 1999 Sep 24;856(1-2):515-26. Review.

PMID:
10526802
25.

Oligonucleotide sequencing using guanine-specific methylation and electrospray ionization ion trap mass spectrometry.

Marzilli LA, Barry JP, Sells T, Law SJ, Vouros P, Harsch A.

J Mass Spectrom. 1999 Apr;34(4):276-80.

PMID:
10226358
26.

Stability of plasma-polymerized allylamine films with sterilization by autoclaving.

Calderon JG, Harsch A, Gross GW, Timmons RB.

J Biomed Mater Res. 1998 Dec 15;42(4):597-603.

PMID:
9827684
27.

Effects of alpha-pompilidotoxin on synchronized firing in networks of rat cortical neurons.

Harsch A, Konno K, Takayama H, Kawai N, Robinson H.

Neurosci Lett. 1998 Aug 7;252(1):49-52.

PMID:
9756356
28.

Sequence-specific photomodification of DNA by an oligonucleotide-phenanthrodihydrodioxin conjugate.

Bendinskas KG, Harsch A, Wilson RM, Midden WR.

Bioconjug Chem. 1998 Sep-Oct;9(5):555-63.

PMID:
9736489
30.

Plastic bronchitis: an unusual complication associated with sickle cell disease and the acute chest syndrome.

Raghuram N, Pettignano R, Gal AA, Harsch A, Adamkiewicz TV.

Pediatrics. 1997 Jul;100(1):139-42. No abstract available.

PMID:
9200374
31.

Strychnine analysis with neuronal networks in vitro: extracellular array recording of network responses.

Harsch A, Ziegler C, Göpel W.

Biosens Bioelectron. 1997;12(8):827-35.

PMID:
9421890
32.

Odor, drug and toxin analysis with neuronal networks in vitro: extracellular array recording of network responses.

Gross GW, Harsch A, Rhoades BK, Göpel W.

Biosens Bioelectron. 1997;12(5):373-93.

PMID:
9228730
33.
34.

Preparation of isolated surface membranes from cystic fibrosis airway epithelial cells.

Harsch AD, Xu J, Bevins CL, Glick MC, Scanlin TF.

Chest. 1992 Mar;101(3 Suppl):58S-60S. No abstract available.

PMID:
1371735

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