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Items: 39

1.

Optimized Translocator Protein Ligand for Optical Molecular Imaging and Screening.

Li J, Smith JA, Dawson ES, Fu A, Nickels ML, Schulte ML, Manning HC.

Bioconjug Chem. 2017 Apr 19;28(4):1016-1023. doi: 10.1021/acs.bioconjchem.6b00711. Epub 2017 Feb 13.

PMID:
28156095
2.

2-Substituted Nγ-glutamylanilides as novel probes of ASCT2 with improved potency.

Schulte ML, Dawson ES, Saleh SA, Cuthbertson ML, Manning HC.

Bioorg Med Chem Lett. 2015 Jan 1;25(1):113-6. doi: 10.1016/j.bmcl.2014.10.098. Epub 2014 Nov 11.

3.

A peptide-based positron emission tomography probe for in vivo detection of caspase activity in apoptotic cells.

Hight MR, Cheung YY, Nickels ML, Dawson ES, Zhao P, Saleh S, Buck JR, Tang D, Washington MK, Coffey RJ, Manning HC.

Clin Cancer Res. 2014 Apr 15;20(8):2126-35. doi: 10.1158/1078-0432.CCR-13-2444. Epub 2014 Feb 26.

4.

An Overview of the Challenges in Designing, Integrating, and Delivering BARD: A Public Chemical-Biology Resource and Query Portal for Multiple Organizations, Locations, and Disciplines.

de Souza A, Bittker JA, Lahr DL, Brudz S, Chatwin S, Oprea TI, Waller A, Yang JJ, Southall N, Guha R, Schürer SC, Vempati UD, Southern MR, Dawson ES, Clemons PA, Chung TD.

J Biomol Screen. 2014 Jun;19(5):614-27. doi: 10.1177/1087057113517139. Epub 2014 Jan 17. Review.

5.

Scaffold Hopping Affords a Highly Selective in vitro and in vivo T-Type Calcium Inhibitor Probe Free From IP Issues.

Xie X, Brogan JT, Schulte ML, Mi D, Yu H, Dawson ES, Li M, McManus O, Engers J, Lewis LM, Thompson A, Jones CK, Weaver CD, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Mar 31 [updated 2013 Mar 22].

6.

Discovery of a Small Molecule Activator of the Hypoxia Inducible Factor Pathway.

Theriault JR, Perez J, Gilbert S, Palmer M, Schreiber SL, Lindsley CW, Dawson ES, Engers JL, Felts AS, Bates BS, Emmitte KA.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Mar 31 [updated 2013 Mar 14].

7.

Pure Positive Allosteric Modulators (PAMs) of mGlu5 with Competitive MPEP-Site Interaction.

Zhou Y, Chun A, Gogliotti RD, Dawson ES, Vinson PN, Niswender CM, Noetzel MJ, Rook JM, Bridges TM, Daniels JS, Jones C, Conn PJ, Lindsley CW, Stauffer SR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Oct 31 [updated 2013 Mar 7].

8.

Development of the First Selective mGlu3 NAM from an mGlu5 PAM Hit.

Sheffler DJ, Wenthur CJ, Brunner JA, Daniels JS, Morrison RD, Blobaum AL, Dawson ES, Engers JL, Niswender CM, Conn PJ, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 9 [updated 2013 Mar 14].

9.

Discovery and Characterization of a Selective Activator of the G-Protein Activated Inward-Rectifying Potassium (GIRK) Channel.

Days E, Kaufmann K, Romaine I, Niswender C, Lewis M, Utley T, Du Y, Sliwoski G, Morrison R, Dawson ES, Engers JL, Denton J, Daniels JS, Sulikowski GA, Lindsley CW, Weaver CD.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 6 [updated 2013 Mar 14].

10.

Extended Probe Characterization: Development of an M4 PAM with Improved Activity and Brain Exposure, while Avoiding Species Bias.

Niswender CM, Rodriguez AL, Sheffler DJ, Utley TJ, Vinson PN, Dawson ES, Jones CK, Wood MR, Daniels JS, Conn PJ, Engers JL, Le UM, Melancon BJ, Hopkins CR, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Oct 31 [updated 2013 Mar 7].

11.

Development of a Selective, Allosteric PLD2 Inhibitor.

Scott SA, O’Reilly MC, Daniels JS, Morrison R, Ptak R, Dawson ES, Tower N, Engers JL, Engers DW, Oguin T, Thomas P, White L, Brown HA, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 5 [updated 2013 Mar 14].

12.

Identification of a Selective Allosteric Agonist of mGlu5.

Manka J, Zhou Y, Chun A, Dawson ES, Vinson PN, Niswender CM, Noetzel MJ, Rook JM, Bridges TM, Daniels JS, Jones C, Conn PJ, Lindsley CW, Stauffer SR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Dec 16 [updated 2013 Mar 7].

13.

Development of a Selective, Allosteric PLD1/2 Inhibitor in a Novel Scaffold.

Scott SA, O’Reilly MC, Daniels JS, Morrison R, Ptak R, Dawson ES, Tower N, Engers JL, Engers DW, Oguin T, Thomas P, White L, Brown HA, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Apr 5 [updated 2013 Mar 14].

14.

Discovery, synthesis, and structure-based optimization of a series of N-(tert-butyl)-2-(N-arylamido)-2-(pyridin-3-yl) acetamides (ML188) as potent noncovalent small molecule inhibitors of the severe acute respiratory syndrome coronavirus (SARS-CoV) 3CL protease.

Jacobs J, Grum-Tokars V, Zhou Y, Turlington M, Saldanha SA, Chase P, Eggler A, Dawson ES, Baez-Santos YM, Tomar S, Mielech AM, Baker SC, Lindsley CW, Hodder P, Mesecar A, Stauffer SR.

J Med Chem. 2013 Jan 24;56(2):534-46. doi: 10.1021/jm301580n. Epub 2013 Jan 3.

15.

Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold.

Rodriguez AL, Zhou Y, Williams R, Weaver CD, Vinson PN, Dawson ES, Steckler T, Lavreysen H, Mackie C, Bartolomé JM, Macdonald GJ, Daniels JS, Niswender CM, Jones CK, Conn PJ, Lindsley CW, Stauffer SR.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7388-92. doi: 10.1016/j.bmcl.2012.10.068. Epub 2012 Oct 23.

16.

Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators.

Mueller R, Dawson ES, Niswender CM, Butkiewicz M, Hopkins CR, Weaver CD, Lindsley CW, Conn PJ, Meiler J.

J Mol Model. 2012 Sep;18(9):4437-46. doi: 10.1007/s00894-012-1441-0. Epub 2012 May 17.

17.

The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease.

Xiang Z, Thompson AD, Brogan JT, Schulte ML, Melancon BJ, Mi D, Lewis LM, Zou B, Yang L, Morrison R, Santomango T, Byers F, Brewer K, Aldrich JS, Yu H, Dawson ES, Li M, McManus O, Jones CK, Daniels JS, Hopkins CR, Xie XS, Conn PJ, Weaver CD, Lindsley CW.

ACS Chem Neurosci. 2011 Dec 21;2(12):730-742.

18.

Discovery of 2-(2-benzoxazoyl amino)-4-aryl-5-cyanopyrimidine as negative allosteric modulators (NAMs) of metabotropic glutamate receptor 5 (mGlu₅): from an artificial neural network virtual screen to an in vivo tool compound.

Mueller R, Dawson ES, Meiler J, Rodriguez AL, Chauder BA, Bates BS, Felts AS, Lamb JP, Menon UN, Jadhav SB, Kane AS, Jones CK, Gregory KJ, Niswender CM, Conn PJ, Olsen CM, Winder DG, Emmitte KA, Lindsley CW.

ChemMedChem. 2012 Mar 5;7(3):406-14. doi: 10.1002/cmdc.201100510. Epub 2012 Jan 20. No abstract available.

19.

Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.

Theriault JR, Felts AS, Bates BS, Perez JR, Palmer M, Gilbert SR, Dawson ES, Engers JL, Lindsley CW, Emmitte KA.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):76-81. doi: 10.1016/j.bmcl.2011.11.077. Epub 2011 Nov 28.

20.

A conserved asparagine residue in transmembrane segment 1 (TM1) of serotonin transporter dictates chloride-coupled neurotransmitter transport.

Henry LK, Iwamoto H, Field JR, Kaufmann K, Dawson ES, Jacobs MT, Adams C, Felts B, Zdravkovic I, Armstrong V, Combs S, Solis E, Rudnick G, Noskov SY, DeFelice LJ, Meiler J, Blakely RD.

J Biol Chem. 2011 Sep 2;286(35):30823-36. doi: 10.1074/jbc.M111.250308. Epub 2011 Jul 5.

21.

Selective inhibition of the K(ir)2 family of inward rectifier potassium channels by a small molecule probe: the discovery, SAR, and pharmacological characterization of ML133.

Wang HR, Wu M, Yu H, Long S, Stevens A, Engers DW, Sackin H, Daniels JS, Dawson ES, Hopkins CR, Lindsley CW, Li M, McManus OB.

ACS Chem Biol. 2011 Aug 19;6(8):845-56. doi: 10.1021/cb200146a. Epub 2011 Jun 13.

22.

Discovery and development of a second highly selective M1 Positive Allosteric Modulator (PAM).

Bridges TM, Reid PR, Lewis LM, Dawson ES, Weaver CD, Wood MR, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Mar 31 [updated 2010 Oct 29].

23.

Discovery and development of the a highly selective M1 Positive Allosteric Modulator (PAM).

Bridges TM, Lewis LM, Dawson ES, Weaver CD, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Feb 26 [updated 2010 Oct 20].

24.

A potent and selective small molecule Kir2.1 inhibitor.

Wu M, Wang H, Yu H, Makhina E, Xu J, Dawson ES, Hopkins CR, Lindsley CW, McManus OB, Li M.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2010 Feb 26 [updated 2010 Oct 20].

25.

Development of a selective small-molecule inhibitor of Kir1.1, the renal outer medullary potassium channel.

Bhave G, Chauder BA, Liu W, Dawson ES, Kadakia R, Nguyen TT, Lewis LM, Meiler J, Weaver CD, Satlin LM, Lindsley CW, Denton JS.

Mol Pharmacol. 2011 Jan;79(1):42-50. doi: 10.1124/mol.110.066928. Epub 2010 Oct 6.

26.

Folding and rescue of a cystic fibrosis transmembrane conductance regulator trafficking mutant identified using human-murine chimeric proteins.

Da Paula AC, Sousa M, Xu Z, Dawson ES, Boyd AC, Sheppard DN, Amaral MD.

J Biol Chem. 2010 Aug 27;285(35):27033-44. doi: 10.1074/jbc.M110.120352. Epub 2010 Jun 15.

27.

Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening.

Mueller R, Rodriguez AL, Dawson ES, Butkiewicz M, Nguyen TT, Oleszkiewicz S, Bleckmann A, Weaver CD, Lindsley CW, Conn PJ, Meiler J.

ACS Chem Neurosci. 2010 Apr 21;1(4):288-305. Epub 2010 Jan 28.

28.

Evaluation of the biosynthetic proposal for the synthesis of marineosins A and B.

Aldrich LN, Dawson ES, Lindsley CW.

Org Lett. 2010 Mar 5;12(5):1048-51. doi: 10.1021/ol100034p.

PMID:
20141121
29.

Streptomyces coelicolor A3(2) CYP102 protein, a novel fatty acid hydroxylase encoded as a heme domain without an N-terminal redox partner.

Lamb DC, Lei L, Zhao B, Yuan H, Jackson CJ, Warrilow AG, Skaug T, Dyson PJ, Dawson ES, Kelly SL, Hachey DL, Waterman MR.

Appl Environ Microbiol. 2010 Mar;76(6):1975-80. doi: 10.1128/AEM.03000-09. Epub 2010 Jan 22.

30.

Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system.

Lebois EP, Bridges TM, Lewis LM, Dawson ES, Kane AS, Xiang Z, Jadhav SB, Yin H, Kennedy JP, Meiler J, Niswender CM, Jones CK, Conn PJ, Weaver CD, Lindsley CW.

ACS Chem Neurosci. 2010;1(2):104-121.

31.

Disseminated dermal Trichophyton rubrum infection - an expression of dermatophyte dimorphism?

Lillis JV, Dawson ES, Chang R, White CR Jr.

J Cutan Pathol. 2010 Nov;37(11):1168-9. doi: 10.1111/j.1600-0560.2009.01355.x.

PMID:
19615031
32.

Structural determinants of species-selective substrate recognition in human and Drosophila serotonin transporters revealed through computational docking studies.

Kaufmann KW, Dawson ES, Henry LK, Field JR, Blakely RD, Meiler J.

Proteins. 2009 Feb 15;74(3):630-42. doi: 10.1002/prot.22178.

33.

A model for the solution structure of the rod arrestin tetramer.

Hanson SM, Dawson ES, Francis DJ, Van Eps N, Klug CS, Hubbell WL, Meiler J, Gurevich VV.

Structure. 2008 Jun;16(6):924-34. doi: 10.1016/j.str.2008.03.006.

34.

Chimeric constructs endow the human CFTR Cl- channel with the gating behavior of murine CFTR.

Scott-Ward TS, Cai Z, Dawson ES, Doherty A, Da Paula AC, Davidson H, Porteous DJ, Wainwright BJ, Amaral MD, Sheppard DN, Boyd AC.

Proc Natl Acad Sci U S A. 2007 Oct 9;104(41):16365-70. Epub 2007 Oct 3.

35.

Inhibition of protein phosphatase 2A activity by selective electrophile alkylation damage.

Codreanu SG, Adams DG, Dawson ES, Wadzinski BE, Liebler DC.

Biochemistry. 2006 Aug 22;45(33):10020-9.

PMID:
16906760
36.
37.

Measurement of intermolecular distances for the natural agonist Peptide docked at the cholecystokinin receptor expressed in situ using fluorescence resonance energy transfer.

Harikumar KG, Pinon DI, Wessels WS, Dawson ES, Lybrand TP, Prendergast FG, Miller LJ.

Mol Pharmacol. 2004 Jan;65(1):28-35.

PMID:
14722234
38.

Moleular models for cholecystokinin-A receptor.

Dawson ES, Henne RM, Miller LJ, Lybrand TP.

Pharmacol Toxicol. 2002 Dec;91(6):290-6. Review.

PMID:
12688371

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