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Items: 1 to 50 of 77

1.

Considerations for refining the risk assessment process for formaldehyde: Results from an interdisciplinary workshop.

Andersen ME, Gentry PR, Swenberg JA, Mundt KA, White KW, Thompson C, Bus J, Sherman JH, Greim H, Bolt H, Marsh GM, Checkoway H, Coggon D, Clewell HJ 3rd.

Regul Toxicol Pharmacol. 2019 May 3;106:210-223. doi: 10.1016/j.yrtph.2019.04.015. [Epub ahead of print]

2.

Updating physiologically based pharmacokinetic models for manganese by incorporating rapid association/dissociation processes in tissues.

Yoon M, Efremenko A, Van Landingham C, Gentry PR, Keene AM, Taylor MD, Clewell HJ, Andersen ME.

Toxicol Appl Pharmacol. 2019 Jun 1;372:1-10. doi: 10.1016/j.taap.2019.04.006. Epub 2019 Apr 9.

3.

Dose-response for assessing the cancer risk of inorganic arsenic in drinking water: the scientific basis for use of a threshold approach.

Tsuji JS, Chang ET, Gentry PR, Clewell HJ, Boffetta P, Cohen SM.

Crit Rev Toxicol. 2019 Apr 1:1-49. doi: 10.1080/10408444.2019.1573804. [Epub ahead of print]

PMID:
30932726
4.

Peak Exposures in Epidemiologic Studies and Cancer Risks: Considerations for Regulatory Risk Assessment.

Checkoway H, Lees PSJ, Dell LD, Gentry PR, Mundt KA.

Risk Anal. 2019 Mar 29. doi: 10.1111/risa.13294. [Epub ahead of print]

PMID:
30925210
5.

Identification of a novel scaffold for a small molecule GPR139 receptor agonist.

Nøhr AC, Shehata MA, Palmer D, Pokhrel R, Vallianou M, Foster SR, Gentry PR, Gloriam DE, Bräuner-Osborne H.

Sci Rep. 2019 Mar 7;9(1):3802. doi: 10.1038/s41598-019-40085-9.

6.

An evaluation of the USEPA Proposed Approaches for applying a biologically based dose-response model in a risk assessment for perchlorate in drinking water.

Clewell HJ 3rd, Gentry PR, Hack CE, Greene T, Clewell RA.

Regul Toxicol Pharmacol. 2019 Apr;103:237-252. doi: 10.1016/j.yrtph.2019.01.028. Epub 2019 Jan 29. Review.

7.

Physiologically-based pharmacokinetic modeling suggests similar bioavailability of Mn from diet and drinking water.

Song G, Van Landingham CB, Gentry PR, Taylor MD, Keene AM, Andersen ME, Clewell HJ, Yoon M.

Toxicol Appl Pharmacol. 2018 Nov 15;359:70-81. doi: 10.1016/j.taap.2018.09.023. Epub 2018 Sep 20.

8.

Application of the adverse outcome pathway (AOP) approach to inform mode of action (MOA): A case study with inorganic arsenic.

Clewell HJ, Yager JW, Greene TB, Gentry PR.

J Toxicol Environ Health A. 2018;81(18):893-912. doi: 10.1080/15287394.2018.1500326. Epub 2018 Sep 19.

PMID:
30230972
9.

Discovery and Optimization of Potent and CNS Penetrant M5-Preferring Positive Allosteric Modulators Derived from a Novel, Chiral N-(Indanyl)piperidine Amide Scaffold.

Bender AM, Cho HP, Nance KD, Lingenfelter KS, Luscombe VB, Gentry PR, Voigtritter K, Berizzi AE, Sexton PM, Langmead CJ, Christopoulos A, Locuson CW, Bridges TM, Chang S, O'Neill JC, Zhan X, Niswender CM, Jones CK, Conn PJ, Lindsley CW.

ACS Chem Neurosci. 2018 Jul 18;9(7):1572-1581. doi: 10.1021/acschemneuro.8b00126. Epub 2018 Apr 26.

PMID:
29678111
10.

Quantitative risk assessment of tobacco products: A potentially useful component of substantial equivalence evaluations.

Marano KM, Liu C, Fuller W, Gentry PR.

Regul Toxicol Pharmacol. 2018 Jun;95:371-384. doi: 10.1016/j.yrtph.2018.03.026. Epub 2018 Mar 31.

11.

Response to Dr. Bernard D. Goldstein's Letter to the Editor.

Mundt KA, Gallagher AE, Dell LD, Natelson EA, Boffetta P, Gentry PR.

Crit Rev Toxicol. 2018 May;48(5):341-343. doi: 10.1080/10408444.2018.1431765. Epub 2018 Feb 20. No abstract available.

PMID:
29460663
12.

Formaldehyde, Hematotoxicity, and Chromosomal Changes-Letter.

Mundt KA, Gallagher AE, Dell LD, Natelson E, Boffetta P, Gentry PR.

Cancer Epidemiol Biomarkers Prev. 2018 Jan;27(1):119. doi: 10.1158/1055-9965.EPI-17-0306. No abstract available.

13.

Six years after the NRC review of EPA's Draft IRIS Toxicological Review of Formaldehyde: Regulatory implications of new science in evaluating formaldehyde leukemogenicity.

Mundt KA, Gentry PR, Dell LD, Rodricks JV, Boffetta P.

Regul Toxicol Pharmacol. 2018 Feb;92:472-490. doi: 10.1016/j.yrtph.2017.11.006. Epub 2017 Nov 20.

14.

Evaluation of triclosan in Minnesota lakes and rivers: Part II - human health risk assessment.

Yost LJ, Barber TR, Gentry PR, Bock MJ, Lyndall JL, Capdevielle MC, Slezak BP.

Ecotoxicol Environ Saf. 2017 Aug;142:588-596. doi: 10.1016/j.ecoenv.2017.04.048. Epub 2017 May 5.

PMID:
28483548
15.

Does occupational exposure to formaldehyde cause hematotoxicity and leukemia-specific chromosome changes in cultured myeloid progenitor cells?

Mundt KA, Gallagher AE, Dell LD, Natelson EA, Boffetta P, Gentry PR.

Crit Rev Toxicol. 2017 Aug;47(7):592-602. doi: 10.1080/10408444.2017.1301878. Epub 2017 May 2. Review. Erratum in: Crit Rev Toxicol. 2017 Aug;47(7):i.

PMID:
28462599
16.

A tissue dose-based comparative exposure assessment of manganese using physiologically based pharmacokinetic modeling-The importance of homeostatic control for an essential metal.

Gentry PR, Van Landingham C, Fuller WG, Sulsky SI, Greene TB, Clewell HJ 3rd, Andersen ME, Roels HA, Taylor MD, Keene AM.

Toxicol Appl Pharmacol. 2017 May 1;322:27-40. doi: 10.1016/j.taap.2017.02.015. Epub 2017 Feb 22.

17.

The need for transparency and reproducibility in documenting values for regulatory decision making and evaluating causality: The example of formaldehyde.

Van Landingham C, Mundt KA, Allen BC, Gentry PR.

Regul Toxicol Pharmacol. 2016 Nov;81:512-521. doi: 10.1016/j.yrtph.2016.10.011. Epub 2016 Oct 19.

18.

Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators.

Berizzi AE, Gentry PR, Rueda P, Den Hoedt S, Sexton PM, Langmead CJ, Christopoulos A.

Mol Pharmacol. 2016 Oct;90(4):427-36. doi: 10.1124/mol.116.104182. Epub 2016 Jul 26.

PMID:
27461343
19.

Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy.

Gogliotti RD, Engers DW, Garcia-Barrantes PM, Panarese JD, Gentry PR, Blobaum AL, Morrison RD, Daniels JS, Thompson AD, Jones CK, Conn PJ, Niswender CM, Lindsley CW, Hopkins CR.

Bioorg Med Chem Lett. 2016 Jun 15;26(12):2915-2919. doi: 10.1016/j.bmcl.2016.04.041. Epub 2016 Apr 19.

20.

Novel Allosteric Modulators of G Protein-coupled Receptors.

Gentry PR, Sexton PM, Christopoulos A.

J Biol Chem. 2015 Aug 7;290(32):19478-88. doi: 10.1074/jbc.R115.662759. Epub 2015 Jun 22. Review.

21.

Risk assessments for chronic exposure of children and prospective parents to ethylbenzene (CAS No. 100-41-4).

Sweeney LM, Kester JE, Kirman CR, Gentry PR, Banton MI, Bus JS, Gargas ML.

Crit Rev Toxicol. 2015;45(8):662-726. doi: 10.3109/10408444.2015.1046157. Epub 2015 Sep 25. Review.

PMID:
25997510
22.

Evaluation of gene expression changes in human primary lung epithelial cells following 24-hr exposures to inorganic arsenic and its methylated metabolites and to arsenic trioxide.

Efremenko AY, Seagrave J, Clewell HJ, Van Landingham C, Gentry PR, Yager JW.

Environ Mol Mutagen. 2015 Jun;56(5):477-90. doi: 10.1002/em.21937. Epub 2015 Apr 14.

PMID:
25873331
23.

Development of a Novel, Orthosteric M5 Antagonist Possessing a High Degree of Muscarinic Subtype Selectivity.

Gentry PR, Kokubo M, Bridges TM, Daniels JS, Niswender CM, Smith E, Chase P, Hodder PS, Rosen H, Conn PJ, Engers J, Brewer KA, Wood MR, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Dec 15 [updated 2015 Feb 11].

24.

Development of the First CNS penetrant M5 Positive Allosteric Modulator (PAM) Based on a Novel, non-Isatin Core.

Gentry PR, Kokubo M, Bridges TM, Daniels JS, Niswender CM, Smith E, Chase P, Hodder PS, Rosen H, Conn PJ, Engers J, Brewer KA, Lindsley CW, Wood MR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Dec 15 [updated 2015 Feb 11].

25.

Further optimization of the M5 NAM MLPCN probe ML375: tactics and challenges.

Kurata H, Gentry PR, Kokubo M, Cho HP, Bridges TM, Niswender CM, Byers FW, Wood MR, Daniels JS, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2015 Feb 1;25(3):690-4. doi: 10.1016/j.bmcl.2014.11.082. Epub 2014 Dec 13.

26.

Development of the First Potent, Selective and CNS penetrant M5 Negative Allosteric Modulator (NAM).

Gentry PR, Kokubo M, Bridges TM, Daniels JS, Niswender CM, Smith E, Chase P, Hodder PS, Rosen H, Conn PJ, Engers J, Brewer KA, Wood MR, Lindsley CW.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2013 Dec 9 [updated 2014 Sep 18].

27.

Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM).

Morris LC, Nance KD, Gentry PR, Days EL, Weaver CD, Niswender CM, Thompson AD, Jones CK, Locuson CW, Morrison RD, Daniels JS, Niswender KD, Lindsley CW.

J Med Chem. 2014 Dec 11;57(23):10192-7. doi: 10.1021/jm501375c. Epub 2014 Dec 2.

28.

Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380).

Gentry PR, Kokubo M, Bridges TM, Noetzel MJ, Cho HP, Lamsal A, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Lindsley CW, Wood MR.

J Med Chem. 2014 Sep 25;57(18):7804-10. doi: 10.1021/jm500995y. Epub 2014 Sep 3.

29.

A constrained maximum likelihood approach to evaluate the impact of dose metric on cancer risk assessment: application to β-chloroprene.

Allen BC, Van Landingham C, Yang Y, Youk AO, Marsh GM, Esmen N, Gentry PR, Clewell HJ 3rd, Himmelstein MW.

Regul Toxicol Pharmacol. 2014 Oct;70(1):203-13. doi: 10.1016/j.yrtph.2014.07.001. Epub 2014 Jul 7.

PMID:
25010378
30.

Use of mode of action data to inform a dose-response assessment for bladder cancer following exposure to inorganic arsenic.

Gentry PR, Yager JW, Clewell RA, Clewell HJ 3rd.

Toxicol In Vitro. 2014 Oct;28(7):1196-205. doi: 10.1016/j.tiv.2014.05.011. Epub 2014 Jun 14.

PMID:
24937311
31.

Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe.

Gentry PR, Kokubo M, Bridges TM, Cho HP, Smith E, Chase P, Hodder PS, Utley TJ, Rajapakse A, Byers F, Niswender CM, Morrison RD, Daniels JS, Wood MR, Conn PJ, Lindsley CW.

ChemMedChem. 2014 Aug;9(8):1677-82. doi: 10.1002/cmdc.201402051. Epub 2014 Apr 1.

32.

M5 receptor activation produces opposing physiological outcomes in dopamine neurons depending on the receptor's location.

Foster DJ, Gentry PR, Lizardi-Ortiz JE, Bridges TM, Wood MR, Niswender CM, Sulzer D, Lindsley CW, Xiang Z, Conn PJ.

J Neurosci. 2014 Feb 26;34(9):3253-62. doi: 10.1523/JNEUROSCI.4896-13.2014.

33.

The impact of recent advances in research on arsenic cancer risk assessment.

Gentry PR, Clewell HJ 3rd, Greene TB, Franzen AC, Yager JW.

Regul Toxicol Pharmacol. 2014 Jun;69(1):91-104. doi: 10.1016/j.yrtph.2014.02.006. Epub 2014 Feb 15.

PMID:
24534001
34.

Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375).

Gentry PR, Kokubo M, Bridges TM, Kett NR, Harp JM, Cho HP, Smith E, Chase P, Hodder PS, Niswender CM, Daniels JS, Conn PJ, Wood MR, Lindsley CW.

J Med Chem. 2013 Nov 27;56(22):9351-5. doi: 10.1021/jm4013246. Epub 2013 Nov 13.

35.

Drugs for allosteric sites on receptors.

Wenthur CJ, Gentry PR, Mathews TP, Lindsley CW.

Annu Rev Pharmacol Toxicol. 2014;54:165-84. doi: 10.1146/annurev-pharmtox-010611-134525. Epub 2013 Oct 2. Review.

36.

Potential occupational risk of amines in carbon capture for power generation.

Gentry PR, House-Knight T, Harris A, Greene T, Campleman S.

Int Arch Occup Environ Health. 2014 Aug;87(6):591-606. doi: 10.1007/s00420-013-0900-y. Epub 2013 Sep 3. Review.

PMID:
23999744
37.

Formaldehyde exposure and leukemia: critical review and reevaluation of the results from a study that is the focus for evidence of biological plausibility.

Gentry PR, Rodricks JV, Turnbull D, Bachand A, Van Landingham C, Shipp AM, Albertini RJ, Irons R.

Crit Rev Toxicol. 2013 Sep;43(8):661-70. doi: 10.3109/10408444.2013.818618. Epub 2013 Jul 31. Review.

PMID:
23902349
38.

Development and characterization of a highly selective M5 PAM probe molecule with improved potency.

Gentry PR, Bridges TM, Daniels JS, Lamsal A, Vinson PN, Niswender CM, Hodder PS, Rosen H, Conn PJ, Engers J, Lindsley CW, Wood MR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2012 Dec 13 [updated 2013 Mar 22].

39.

Discovery of ML326: The first sub-micromolar, selective M5 PAM.

Gentry PR, Bridges TM, Lamsal A, Vinson PN, Smith E, Chase P, Hodder PS, Engers JL, Niswender CM, Daniels JS, Conn PJ, Wood MR, Lindsley CW.

Bioorg Med Chem Lett. 2013 May 15;23(10):2996-3000. doi: 10.1016/j.bmcl.2013.03.032. Epub 2013 Mar 16.

40.

Spirocyclic replacements for the isatin in the highly selective, muscarinic M1 PAM ML137: the continued optimization of an MLPCN probe molecule.

Poslusney MS, Melancon BJ, Gentry PR, Sheffler DJ, Bridges TM, Utley TJ, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Wood MR.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1860-4. doi: 10.1016/j.bmcl.2013.01.017. Epub 2013 Jan 11.

41.

Isatin replacements applied to the highly selective, muscarinic M1 PAM ML137: continued optimization of an MLPCN probe molecule.

Melancon BJ, Poslusney MS, Gentry PR, Tarr JC, Sheffler DJ, Mattmann ME, Bridges TM, Utley TJ, Daniels JS, Niswender CM, Conn PJ, Lindsley CW, Wood MR.

Bioorg Med Chem Lett. 2013 Jan 15;23(2):412-6. doi: 10.1016/j.bmcl.2012.11.092. Epub 2012 Dec 1.

42.

Evaluation of gene expression changes in human primary uroepithelial cells following 24-hr exposures to inorganic arsenic and its methylated metabolites.

Yager JW, Gentry PR, Thomas RS, Pluta L, Efremenko A, Black M, Arnold LL, McKim JM, Wilga P, Gill G, Choe KY, Clewell HJ.

Environ Mol Mutagen. 2013 Mar;54(2):82-98. doi: 10.1002/em.21749. Epub 2012 Nov 29.

PMID:
23192986
43.

Physiologically based pharmacokinetic/toxicokinetic modeling.

Campbell JL Jr, Clewell RA, Gentry PR, Andersen ME, Clewell HJ 3rd.

Methods Mol Biol. 2012;929:439-99.

PMID:
23007440
44.

Challenges in the application of quantitative approaches in risk assessment: a case study with di-(2-ethylhexyl)phthalate.

Gentry PR, Clewell HJ 3rd, Clewell R, Campbell J, Van Landingham C, Shipp AM.

Crit Rev Toxicol. 2011 Aug;41 Suppl 2:1-72. doi: 10.3109/10408444.2011.599366. Review.

PMID:
21838516
45.

Concentration- and time-dependent genomic changes in the mouse urinary bladder following exposure to arsenate in drinking water for up to 12 weeks.

Clewell HJ, Thomas RS, Kenyon EM, Hughes MF, Adair BM, Gentry PR, Yager JW.

Toxicol Sci. 2011 Oct;123(2):421-32. doi: 10.1093/toxsci/kfr199. Epub 2011 Jul 27.

PMID:
21795629
46.

Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).

Engers DW, Gentry PR, Williams R, Bolinger JD, Weaver CD, Menon UN, Conn PJ, Lindsley CW, Niswender CM, Hopkins CR.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5175-8. doi: 10.1016/j.bmcl.2010.07.007. Epub 2010 Jul 8.

47.

Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.

Bridges TM, Phillip Kennedy J, Noetzel MJ, Breininger ML, Gentry PR, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2010 Mar 15;20(6):1972-5. doi: 10.1016/j.bmcl.2010.01.109. Epub 2010 Feb 1.

48.

In vivo structure-activity relationship study of dorsomorphin analogues identifies selective VEGF and BMP inhibitors.

Hao J, Ho JN, Lewis JA, Karim KA, Daniels RN, Gentry PR, Hopkins CR, Lindsley CW, Hong CC.

ACS Chem Biol. 2010 Feb 19;5(2):245-53. doi: 10.1021/cb9002865.

49.

Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.

Bridges TM, Kennedy JP, Cho HP, Breininger ML, Gentry PR, Hopkins CR, Conn PJ, Lindsley CW.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):558-62. doi: 10.1016/j.bmcl.2009.11.089. Epub 2009 Nov 22.

50.

Synthesis and structure-activity relationships of allosteric potentiators of the m(4) muscarinic acetylcholine receptor.

Kennedy JP, Bridges TM, Gentry PR, Brogan JT, Kane AS, Jones CK, Brady AE, Shirey JK, Conn PJ, Lindsley CW.

ChemMedChem. 2009 Oct;4(10):1600-7. doi: 10.1002/cmdc.200900231. No abstract available.

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