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Items: 26

1.

Author Correction: Dopamine D3 receptor antagonist reveals a cryptic pocket in aminergic GPCRs.

Ferruz N, Doerr S, Vanase-Frawley MA, Zou Y, Chen X, Marr ES, Nelson RT, Kormos BL, Wager TT, Hou X, Villalobos A, Sciabola S, De Fabritiis G.

Sci Rep. 2019 Apr 10;9(1):6076. doi: 10.1038/s41598-019-39694-1.

2.

In Vitro-In Vivo Extrapolation of Key Transporter Activity at the Blood-Brain Barrier.

Trapa PE, Troutman MD, Lau TY, Wager TT, Maurer TS, Patel NC, West MA, Umland JP, Carlo AA, Feng B, Liras JL.

Drug Metab Dispos. 2019 Apr;47(4):405-411. doi: 10.1124/dmd.118.083279. Epub 2019 Jan 25.

PMID:
30683809
3.

Late-Stage Microsomal Oxidation Reduces Drug-Drug Interaction and Identifies Phosphodiesterase 2A Inhibitor PF-06815189.

Stepan AF, Tran TP, Helal CJ, Brown MS, Chang C, O'Connor RE, De Vivo M, Doran SD, Fisher EL, Jenkinson S, Karanian D, Kormos BL, Sharma R, Walker GS, Wright AS, Yang EX, Brodney MA, Wager TT, Verhoest PR, Obach RS.

ACS Med Chem Lett. 2018 Jan 4;9(2):68-72. doi: 10.1021/acsmedchemlett.7b00343. eCollection 2018 Feb 8.

4.

Dopamine D3 receptor antagonist reveals a cryptic pocket in aminergic GPCRs.

Ferruz N, Doerr S, Vanase-Frawley MA, Zou Y, Chen X, Marr ES, Nelson RT, Kormos BL, Wager TT, Hou X, Villalobos A, Sciabola S, De Fabritiis G.

Sci Rep. 2018 Jan 17;8(1):897. doi: 10.1038/s41598-018-19345-7. Erratum in: Sci Rep. 2019 Apr 10;9(1):6076.

5.

Identification and Profiling of a Selective and Brain Penetrant Radioligand for in Vivo Target Occupancy Measurement of Casein Kinase 1 (CK1) Inhibitors.

Wager TT, Galatsis P, Chandrasekaran RY, Butler TW, Li J, Zhang L, Mente S, Subramanyam C, Liu S, Doran AC, Chang C, Fisher K, Grimwood S, Hedde JR, Marconi M, Schildknegt K.

ACS Chem Neurosci. 2017 Sep 20;8(9):1995-2004. doi: 10.1021/acschemneuro.7b00155. Epub 2017 Jun 30.

PMID:
28609096
6.

Dopamine D3/D2 Receptor Antagonist PF-4363467 Attenuates Opioid Drug-Seeking Behavior without Concomitant D2 Side Effects.

Wager TT, Chappie T, Horton D, Chandrasekaran RY, Samas B, Dunn-Sims ER, Hsu C, Nawreen N, Vanase-Frawley MA, O'Connor RE, Schmidt CJ, Dlugolenski K, Stratman NC, Majchrzak MJ, Kormos BL, Nguyen DP, Sawant-Basak A, Mead AN.

ACS Chem Neurosci. 2017 Jan 18;8(1):165-177. doi: 10.1021/acschemneuro.6b00297. Epub 2016 Oct 21.

PMID:
27715007
7.

Targeting of the circadian clock via CK1δ/ε to improve glucose homeostasis in obesity.

Cunningham PS, Ahern SA, Smith LC, da Silva Santos CS, Wager TT, Bechtold DA.

Sci Rep. 2016 Jul 21;6:29983. doi: 10.1038/srep29983.

8.

Quantitative Assessment of the Impact of Fluorine Substitution on P-Glycoprotein (P-gp) Mediated Efflux, Permeability, Lipophilicity, and Metabolic Stability.

Pettersson M, Hou X, Kuhn M, Wager TT, Kauffman GW, Verhoest PR.

J Med Chem. 2016 Jun 9;59(11):5284-96. doi: 10.1021/acs.jmedchem.6b00027. Epub 2016 May 26.

PMID:
27228214
9.

Central Nervous System Multiparameter Optimization Desirability: Application in Drug Discovery.

Wager TT, Hou X, Verhoest PR, Villalobos A.

ACS Chem Neurosci. 2016 Jun 15;7(6):767-75. doi: 10.1021/acschemneuro.6b00029. Epub 2016 Apr 4.

PMID:
26991242
10.

Discovery and preclinical profiling of 3-[4-(morpholin-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl]benzonitrile (PF-06447475), a highly potent, selective, brain penetrant, and in vivo active LRRK2 kinase inhibitor.

Henderson JL, Kormos BL, Hayward MM, Coffman KJ, Jasti J, Kurumbail RG, Wager TT, Verhoest PR, Noell GS, Chen Y, Needle E, Berger Z, Steyn SJ, Houle C, Hirst WD, Galatsis P.

J Med Chem. 2015 Jan 8;58(1):419-32. doi: 10.1021/jm5014055. Epub 2014 Nov 17.

PMID:
25353650
11.

Casein kinase 1δ/ε inhibitor PF-5006739 attenuates opioid drug-seeking behavior.

Wager TT, Chandrasekaran RY, Bradley J, Rubitski D, Berke H, Mente S, Butler T, Doran A, Chang C, Fisher K, Knafels J, Liu S, Ohren J, Marconi M, DeMarco G, Sneed B, Walton K, Horton D, Rosado A, Mead A.

ACS Chem Neurosci. 2014 Dec 17;5(12):1253-65. doi: 10.1021/cn500201x. Epub 2014 Oct 28.

PMID:
25299732
12.

Kinase domain inhibition of leucine rich repeat kinase 2 (LRRK2) using a [1,2,4]triazolo[4,3-b]pyridazine scaffold.

Galatsis P, Henderson JL, Kormos BL, Han S, Kurumbail RG, Wager TT, Verhoest PR, Noell GS, Chen Y, Needle E, Berger Z, Steyn SJ, Houle C, Hirst WD.

Bioorg Med Chem Lett. 2014 Sep 1;24(17):4132-40. doi: 10.1016/j.bmcl.2014.07.052. Epub 2014 Jul 30.

PMID:
25113930
13.

A novel mechanism controlling resetting speed of the circadian clock to environmental stimuli.

Pilorz V, Cunningham PS, Jackson A, West AC, Wager TT, Loudon AS, Bechtold DA.

Curr Biol. 2014 Mar 31;24(7):766-73. doi: 10.1016/j.cub.2014.02.027. Epub 2014 Mar 20.

14.

Improving the odds of success in drug discovery: choosing the best compounds for in vivo toxicology studies.

Wager TT, Kormos BL, Brady JT, Will Y, Aleo MD, Stedman DB, Kuhn M, Chandrasekaran RY.

J Med Chem. 2013 Dec 12;56(23):9771-9. doi: 10.1021/jm401485p. Epub 2013 Nov 22.

PMID:
24219752
15.

Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development of a novel phosphodiesterase 2A PET ligand.

Zhang L, Villalobos A, Beck EM, Bocan T, Chappie TA, Chen L, Grimwood S, Heck SD, Helal CJ, Hou X, Humphrey JM, Lu J, Skaddan MB, McCarthy TJ, Verhoest PR, Wager TT, Zasadny K.

J Med Chem. 2013 Jun 13;56(11):4568-79. doi: 10.1021/jm400312y. Epub 2013 May 28.

PMID:
23651455
16.

Getting the MAX out of Computational Models: The Prediction of Unbound-Brain and Unbound-Plasma Maximum Concentrations.

Mente S, Doran A, Wager TT.

ACS Med Chem Lett. 2012 May 16;3(6):515-9. doi: 10.1021/ml300029a. eCollection 2012 Jun 14.

17.

Strategies to minimize CNS toxicity: in vitro high-throughput assays and computational modeling.

Wager TT, Liras JL, Mente S, Trapa P.

Expert Opin Drug Metab Toxicol. 2012 May;8(5):531-42. doi: 10.1517/17425255.2012.677028. Epub 2012 Mar 29. Review.

PMID:
22458547
18.

Csnk1e is a genetic regulator of sensitivity to psychostimulants and opioids.

Bryant CD, Parker CC, Zhou L, Olker C, Chandrasekaran RY, Wager TT, Bolivar VJ, Loudon AS, Vitaterna MH, Turek FW, Palmer AA.

Neuropsychopharmacology. 2012 Mar;37(4):1026-35. doi: 10.1038/npp.2011.287. Epub 2011 Nov 16.

19.

Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764).

Wager TT, Pettersen BA, Schmidt AW, Spracklin DK, Mente S, Butler TW, Howard H, Lettiere DJ, Rubitski DM, Wong DF, Nedza FM, Nelson FR, Rollema H, Raggon JW, Aubrecht J, Freeman JK, Marcek JM, Cianfrogna J, Cook KW, James LC, Chatman LA, Iredale PA, Banker MJ, Homiski ML, Munzner JB, Chandrasekaran RY.

J Med Chem. 2011 Nov 10;54(21):7602-20. doi: 10.1021/jm200939b. Epub 2011 Oct 7.

PMID:
21928839
20.

Strategies to optimize the brain availability of central nervous system drug candidates.

Wager TT, Villalobos A, Verhoest PR, Hou X, Shaffer CL.

Expert Opin Drug Discov. 2011 Apr;6(4):371-81. doi: 10.1517/17460441.2011.564158. Epub 2011 Mar 22.

PMID:
22646015
21.

Entrainment of disrupted circadian behavior through inhibition of casein kinase 1 (CK1) enzymes.

Meng QJ, Maywood ES, Bechtold DA, Lu WQ, Li J, Gibbs JE, Dupré SM, Chesham JE, Rajamohan F, Knafels J, Sneed B, Zawadzke LE, Ohren JF, Walton KM, Wager TT, Hastings MH, Loudon AS.

Proc Natl Acad Sci U S A. 2010 Aug 24;107(34):15240-5. doi: 10.1073/pnas.1005101107. Epub 2010 Aug 9.

22.

Moving beyond rules: the development of a central nervous system multiparameter optimization (CNS MPO) approach to enable alignment of druglike properties.

Wager TT, Hou X, Verhoest PR, Villalobos A.

ACS Chem Neurosci. 2010 Jun 16;1(6):435-49. doi: 10.1021/cn100008c. Epub 2010 Mar 25.

23.

Defining desirable central nervous system drug space through the alignment of molecular properties, in vitro ADME, and safety attributes.

Wager TT, Chandrasekaran RY, Hou X, Troutman MD, Verhoest PR, Villalobos A, Will Y.

ACS Chem Neurosci. 2010 Jun 16;1(6):420-34. doi: 10.1021/cn100007x. Epub 2010 Mar 25.

24.

Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period.

Walton KM, Fisher K, Rubitski D, Marconi M, Meng QJ, Sládek M, Adams J, Bass M, Chandrasekaran R, Butler T, Griffor M, Rajamohan F, Serpa M, Chen Y, Claffey M, Hastings M, Loudon A, Maywood E, Ohren J, Doran A, Wager TT.

J Pharmacol Exp Ther. 2009 Aug;330(2):430-9. doi: 10.1124/jpet.109.151415. Epub 2009 May 19.

PMID:
19458106
25.

Asymmetric Total Synthesis of Rhizoxin D Financial support has been provided by the National Institutes of Health (through grant GM-28961) and by Pfizer, Inc.

Keck GE, Wager CA, Wager TT, Savin KA, Covel JA, McLaws MD, Krishnamurthy D, Cee VJ.

Angew Chem Int Ed Engl. 2001 Jan 5;40(1):231-234. No abstract available.

PMID:
11169722
26.

Asymmetric Total Synthesis of Rhizoxin D.

Keck GE, Wager CA, Wager TT, Savin KA, Covel JA, McLaws MD, Krishnamurthy D, Cee VJ.

Angew Chem Int Ed Engl. 2001 Jan 5;40(1):231-234. doi: 10.1002/1521-3773(20010105)40:1<231::AID-ANIE231>3.0.CO;2-W. No abstract available.

PMID:
29711955

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