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Items: 1 to 50 of 105

1.

Optimization of a Series of Mu Opioid Receptor (MOR) Agonists with High G Protein Signaling Bias.

Kennedy NM, Schmid CL, Ross NC, Lovell KM, Yue Z, Chen YT, Cameron MD, Bohn LM, Bannister TD.

J Med Chem. 2018 Sep 10. doi: 10.1021/acs.jmedchem.8b01136. [Epub ahead of print]

PMID:
30199635
2.

Development of novel NEMO-binding domain mimetics for inhibiting IKK/NF-κB activation.

Zhao J, Zhang L, Mu X, Doebelin C, Nguyen W, Wallace C, Reay DP, McGowan SJ, Corbo L, Clemens PR, Wilson GM, Watkins SC, Solt LA, Cameron MD, Huard J, Niedernhofer LJ, Kamenecka TM, Robbins PD.

PLoS Biol. 2018 Jun 11;16(6):e2004663. doi: 10.1371/journal.pbio.2004663. eCollection 2018 Jun.

3.

Design, synthesis, and evaluation of simple phenol amides as ERRγ agonists.

Lin H, Doebelin C, Patouret R, Garcia-Ordonez RD, Chang MR, Dharmarajan V, Bayona CR, Cameron MD, Griffin PR, Kamenecka TM.

Bioorg Med Chem Lett. 2018 May 1;28(8):1313-1319. doi: 10.1016/j.bmcl.2018.03.019. Epub 2018 Mar 8.

PMID:
29548571
4.

Identification of an aminothiazole series of RORβ modulators.

Patouret R, Doebelin C, Garcia-Ordonez RD, Chang MR, Ruiz C, Cameron MD, Griffin PR, Kamenecka TM.

Bioorg Med Chem Lett. 2018 Apr 15;28(7):1178-1181. doi: 10.1016/j.bmcl.2018.03.001. Epub 2018 Mar 3.

PMID:
29534930
5.

Discovery of Hydrolysis-Resistant Isoindoline N-Acyl Amino Acid Analogues that Stimulate Mitochondrial Respiration.

Lin H, Long JZ, Roche AM, Svensson KJ, Dou FY, Chang MR, Strutzenberg T, Ruiz C, Cameron MD, Novick SJ, Berdan CA, Louie SM, Nomura DK, Spiegelman BM, Griffin PR, Kamenecka TM.

J Med Chem. 2018 Apr 12;61(7):3224-3230. doi: 10.1021/acs.jmedchem.8b00029. Epub 2018 Mar 22.

PMID:
29533650
6.

Fentanyl-related designer drugs W-18 and W-15 lack appreciable opioid activity in vitro and in vivo.

Huang XP, Che T, Mangano TJ, Le Rouzic V, Pan YX, Majumdar S, Cameron MD, Baumann MH, Pasternak GW, Roth BL.

JCI Insight. 2017 Nov 16;2(22). pii: 97222. doi: 10.1172/jci.insight.97222. [Epub ahead of print]

7.

Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics.

Schmid CL, Kennedy NM, Ross NC, Lovell KM, Yue Z, Morgenweck J, Cameron MD, Bannister TD, Bohn LM.

Cell. 2017 Nov 16;171(5):1165-1175.e13. doi: 10.1016/j.cell.2017.10.035.

PMID:
29149605
8.

M344 promotes nonamyloidogenic amyloid precursor protein processing while normalizing Alzheimer's disease genes and improving memory.

Volmar CH, Salah-Uddin H, Janczura KJ, Halley P, Lambert G, Wodrich A, Manoah S, Patel NH, Sartor GC, Mehta N, Miles NTH, Desse S, Dorcius D, Cameron MD, Brothers SP, Wahlestedt C.

Proc Natl Acad Sci U S A. 2017 Oct 24;114(43):E9135-E9144. doi: 10.1073/pnas.1707544114. Epub 2017 Oct 9.

9.

Rational design of peptide derivatives for inhibition of MyD88-mediated toll-like receptor signaling in human peripheral blood mononuclear cells and epithelial cells exposed to Francisella tularensis.

Ryan DA, Degardin M, Alam S, Kissner TL, Hale M, Cameron MD, Rebek M, Ajami D, Saikh KU, Rebek J Jr.

Chem Biol Drug Des. 2017 Dec;90(6):1190-1205. doi: 10.1111/cbdd.13039. Epub 2017 Jul 17.

PMID:
28599094
10.

In vivo instability of platensimycin and platencin: Synthesis and biological evaluation of urea- and carbamate-platensimycin.

Dong LB, Rudolf JD, Lin L, Ruiz C, Cameron MD, Shen B.

Bioorg Med Chem. 2017 Mar 15;25(6):1990-1996. doi: 10.1016/j.bmc.2017.02.028. Epub 2017 Feb 16.

11.

Precise small-molecule recognition of a toxic CUG RNA repeat expansion.

Rzuczek SG, Colgan LA, Nakai Y, Cameron MD, Furling D, Yasuda R, Disney MD.

Nat Chem Biol. 2017 Feb;13(2):188-193. doi: 10.1038/nchembio.2251. Epub 2016 Dec 12.

12.

Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria.

Brust TF, Morgenweck J, Kim SA, Rose JH, Locke JL, Schmid CL, Zhou L, Stahl EL, Cameron MD, Scarry SM, Aubé J, Jones SR, Martin TJ, Bohn LM.

Sci Signal. 2016 Nov 29;9(456):ra117.

13.

N-Arylsulfonyl Indolines as Retinoic Acid Receptor-Related Orphan Receptor γ (RORγ) Agonists.

Doebelin C, Patouret R, Garcia-Ordonez RD, Chang MR, Dharmarajan V, Kuruvilla DS, Novick SJ, Lin L, Cameron MD, Griffin PR, Kamenecka TM.

ChemMedChem. 2016 Dec 6;11(23):2607-2620. doi: 10.1002/cmdc.201600491. Epub 2016 Nov 23.

14.

Probing the Complex Binding Modes of the PPARγ Partial Agonist 2-Chloro-N-(3-chloro-4-((5-chlorobenzo[d]thiazol-2-yl)thio)phenyl)-4-(trifluoromethyl)benzenesulfonamide (T2384) to Orthosteric and Allosteric Sites with NMR Spectroscopy.

Hughes TS, Shang J, Brust R, de Vera IMS, Fuhrmann J, Ruiz C, Cameron MD, Kamenecka TM, Kojetin DJ.

J Med Chem. 2016 Nov 23;59(22):10335-10341. doi: 10.1021/acs.jmedchem.6b01340. Epub 2016 Nov 4.

15.

TNP [N2-(m-Trifluorobenzyl), N6-(p-nitrobenzyl)purine] ameliorates diet induced obesity and insulin resistance via inhibition of the IP6K1 pathway.

Ghoshal S, Zhu Q, Asteian A, Lin H, Xu H, Ernst G, Barrow JC, Xu B, Cameron MD, Kamenecka TM, Chakraborty A.

Mol Metab. 2016 Aug 21;5(10):903-917. doi: 10.1016/j.molmet.2016.08.008. eCollection 2016 Oct.

16.

Albumin-Oxanorbornadiene Conjugates Formed ex Vivo for the Extended Circulation of Hydrophilic Cargo.

Higginson CJ, Eno MR, Khan S, Cameron MD, Finn MG.

ACS Chem Biol. 2016 Aug 19;11(8):2320-7. doi: 10.1021/acschembio.6b00444. Epub 2016 Jun 27.

17.

Design of a small molecule against an oncogenic noncoding RNA.

Velagapudi SP, Cameron MD, Haga CL, Rosenberg LH, Lafitte M, Duckett DR, Phinney DG, Disney MD.

Proc Natl Acad Sci U S A. 2016 May 24;113(21):5898-903. doi: 10.1073/pnas.1523975113. Epub 2016 May 11.

18.

P450 3A-Catalyzed O-Dealkylation of Lapatinib Induces Mitochondrial Stress and Activates Nrf2.

Eno MR, El-Gendy Bel-D, Cameron MD.

Chem Res Toxicol. 2016 May 16;29(5):784-96. doi: 10.1021/acs.chemrestox.5b00524. Epub 2016 Apr 8.

PMID:
26958860
19.

Synthesis and Evaluation of Oxyguanidine Analogues of the Cysteine Protease Inhibitor WRR-483 against Cruzain.

Jones BD, Tochowicz A, Tang Y, Cameron MD, McCall LI, Hirata K, Siqueira-Neto JL, Reed SL, McKerrow JH, Roush WR.

ACS Med Chem Lett. 2015 Dec 15;7(1):77-82. doi: 10.1021/acsmedchemlett.5b00336. eCollection 2016 Jan 14.

20.

Selective Targeting of Extracellular Insulin-Degrading Enzyme by Quasi-Irreversible Thiol-Modifying Inhibitors.

Abdul-Hay SO, Bannister TD, Wang H, Cameron MD, Caulfield TR, Masson A, Bertrand J, Howard EA, McGuire MP, Crisafulli U, Rosenberry TR, Topper CL, Thompson CR, Schürer SC, Madoux F, Hodder P, Leissring MA.

ACS Chem Biol. 2015 Dec 18;10(12):2716-24. doi: 10.1021/acschembio.5b00334. Epub 2015 Sep 30.

PMID:
26398879
21.

Design, Synthesis, and Biological Evaluation of Indole Biphenylcarboxylic Acids as PPARγ Antagonists.

Asteian A, Blayo AL, He Y, Koenig M, Shin Y, Kuruvilla DS, Corzo CA, Cameron MD, Lin L, Ruiz C, Khan S, Kumar N, Busby S, Marciano DP, Garcia-Ordonez RD, Griffin PR, Kamenecka TM.

ACS Med Chem Lett. 2015 Aug 4;6(9):998-1003. doi: 10.1021/acsmedchemlett.5b00218. eCollection 2015 Sep 10.

22.

Nonmuscle myosin IIB as a therapeutic target for the prevention of relapse to methamphetamine use.

Young EJ, Blouin AM, Briggs SB, Sillivan SE, Lin L, Cameron MD, Rumbaugh G, Miller CA.

Mol Psychiatry. 2016 May;21(5):615-23. doi: 10.1038/mp.2015.103. Epub 2015 Aug 4.

23.

Antiobesity Effect of a Small Molecule Repressor of RORγ.

Chang MR, He Y, Khan TM, Kuruvilla DS, Garcia-Ordonez R, Corzo CA, Unger TJ, White DW, Khan S, Lin L, Cameron MD, Kamenecka TM, Griffin PR.

Mol Pharmacol. 2015 Jul;88(1):48-56. doi: 10.1124/mol.114.097485. Epub 2015 Apr 22.

24.

Selective inhibitor of platelet-activating factor acetylhydrolases 1b2 and 1b3 that impairs cancer cell survival.

Chang JW, Zuhl AM, Speers AE, Niessen S, Brown SJ, Mulvihill MM, Fan YC, Spicer TP, Southern M, Scampavia L, Fernandez-Vega V, Dix MM, Cameron MD, Hodder PS, Rosen H, Nomura DK, Kwon O, Hsu KL, Cravatt BF.

ACS Chem Biol. 2015 Apr 17;10(4):925-32. doi: 10.1021/cb500893q. Epub 2015 Jan 20.

25.

Binding mode and potency of N-indolyloxopyridinyl-4-aminopropanyl-based inhibitors targeting Trypanosoma cruzi CYP51.

Vieira DF, Choi JY, Calvet CM, Siqueira-Neto JL, Johnston JB, Kellar D, Gut J, Cameron MD, McKerrow JH, Roush WR, Podust LM.

J Med Chem. 2014 Dec 11;57(23):10162-75. doi: 10.1021/jm501568b. Epub 2014 Nov 25.

26.

Gauging reactive metabolites in drug-induced toxicity.

Eno MR, Cameron MD.

Curr Med Chem. 2015;22(4):465-89. Review.

PMID:
25174933
27.

4-Aminopyridyl-based CYP51 inhibitors as anti-Trypanosoma cruzi drug leads with improved pharmacokinetic profile and in vivo potency.

Calvet CM, Vieira DF, Choi JY, Kellar D, Cameron MD, Siqueira-Neto JL, Gut J, Johnston JB, Lin L, Khan S, McKerrow JH, Roush WR, Podust LM.

J Med Chem. 2014 Aug 28;57(16):6989-7005. doi: 10.1021/jm500448u. Epub 2014 Aug 19.

28.

R-Configuration of 4-Aminopyridyl-Based Inhibitors of CYP51 Confers Superior Efficacy Against Trypanosoma cruzi.

Choi JY, Calvet CM, Vieira DF, Gunatilleke SS, Cameron MD, McKerrow JH, Podust LM, Roush WR.

ACS Med Chem Lett. 2014 Jan 22;5(4):434-9. doi: 10.1021/ml500010m. eCollection 2014 Apr 10.

29.

Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for α4β2α5 nicotinic acetylcholine receptors.

Jin Z, Khan P, Shin Y, Wang J, Lin L, Cameron MD, Lindstrom JM, Kenny PJ, Kamenecka TM.

Bioorg Med Chem Lett. 2014 Jan 15;24(2):674-8. doi: 10.1016/j.bmcl.2013.11.049. Epub 2013 Nov 28.

30.

Characterization of T-5 N-oxide formation as the first highly selective measure of CYP3A5 activity.

Li X, Jeso V, Heyward S, Walker GS, Sharma R, Micalizio GC, Cameron MD.

Drug Metab Dispos. 2014 Mar;42(3):334-42. doi: 10.1124/dmd.113.054726. Epub 2013 Dec 11.

31.

Synthesis and SAR of novel isoxazoles as potent c-jun N-terminal kinase (JNK) inhibitors.

He Y, Duckett D, Chen W, Ling YY, Cameron MD, Lin L, Ruiz CH, Lograsso PV, Kamenecka TM, Koenig M.

Bioorg Med Chem Lett. 2014 Jan 1;24(1):161-4. doi: 10.1016/j.bmcl.2013.11.052. Epub 2013 Dec 4.

32.

Blocking lactate export by inhibiting the Myc target MCT1 Disables glycolysis and glutathione synthesis.

Doherty JR, Yang C, Scott KE, Cameron MD, Fallahi M, Li W, Hall MA, Amelio AL, Mishra JK, Li F, Tortosa M, Genau HM, Rounbehler RJ, Lu Y, Dang CV, Kumar KG, Butler AA, Bannister TD, Hooper AT, Unsal-Kacmaz K, Roush WR, Cleveland JL.

Cancer Res. 2014 Feb 1;74(3):908-20. doi: 10.1158/0008-5472.CAN-13-2034. Epub 2013 Nov 27.

33.

Development of functionally selective, small molecule agonists at kappa opioid receptors.

Zhou L, Lovell KM, Frankowski KJ, Slauson SR, Phillips AM, Streicher JM, Stahl E, Schmid CL, Hodder P, Madoux F, Cameron MD, Prisinzano TE, Aubé J, Bohn LM.

J Biol Chem. 2013 Dec 20;288(51):36703-16. doi: 10.1074/jbc.M113.504381. Epub 2013 Nov 1.

34.

Rational development of 4-aminopyridyl-based inhibitors targeting Trypanosoma cruzi CYP51 as anti-chagas agents.

Choi JY, Calvet CM, Gunatilleke SS, Ruiz C, Cameron MD, McKerrow JH, Podust LM, Roush WR.

J Med Chem. 2013 Oct 10;56(19):7651-68. doi: 10.1021/jm401067s. Epub 2013 Sep 30.

35.

Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties.

Bibian M, Rahaim RJ, Choi JY, Noguchi Y, Schürer S, Chen W, Nakanishi S, Licht K, Rosenberg LH, Li L, Feng Y, Cameron MD, Duckett DR, Cleveland JL, Roush WR.

Bioorg Med Chem Lett. 2013 Aug 1;23(15):4374-80. doi: 10.1016/j.bmcl.2013.05.075. Epub 2013 May 31.

36.

Potent Anti-Diabetic Actions of a Novel Non-Agonist PPARγ Ligand that Blocks Cdk5-Mediated Phosphorylation.

Kamenecka TM, Busby SA, Kumar N, Choi JH, Banks AS, Vidovic D, Cameron MD, Schurer SC, Mercer BA, Hodder P, Spiegelman BM, Griffin PR.

Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-.
2011 Jul 5 [updated 2013 Mar 7].

37.

Synthesis and biological evaluation of urea derivatives as highly potent and selective rho kinase inhibitors.

Yin Y, Lin L, Ruiz C, Khan S, Cameron MD, Grant W, Pocas J, Eid N, Park H, Schröter T, Lograsso PV, Feng Y.

J Med Chem. 2013 May 9;56(9):3568-81. doi: 10.1021/jm400062r. Epub 2013 Apr 25.

PMID:
23570561
38.

Synthesis of benzoquinone ansamycin-inspired macrocyclic lactams from shikimic acid.

Jeso V, Iqbal S, Hernandez P, Cameron MD, Park H, LoGrasso PV, Micalizio GC.

Angew Chem Int Ed Engl. 2013 Apr 26;52(18):4800-4. doi: 10.1002/anie.201301323. Epub 2013 Apr 2. No abstract available.

PMID:
23554224
39.

Synthesis and SAR of Lehualide B: a marine-derived natural product with potent anti-multiple myeloma activity.

Jeso V, Yang C, Cameron MD, Cleveland JL, Micalizio GC.

ACS Chem Biol. 2013;8(6):1241-52. doi: 10.1021/cb300582s. Epub 2013 Apr 2.

40.

Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors.

Jiang R, Frackowiak B, Shin Y, Song X, Chen W, Lin L, Cameron MD, Duckett DR, Kamenecka TM.

Bioorg Med Chem Lett. 2013 May 1;23(9):2683-7. doi: 10.1016/j.bmcl.2013.02.082. Epub 2013 Feb 27.

PMID:
23518277
41.

D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy.

Bicker KL, Anguish L, Chumanevich AA, Cameron MD, Cui X, Witalison E, Subramanian V, Zhang X, Chumanevich AP, Hofseth LJ, Coonrod SA, Thompson PR.

ACS Med Chem Lett. 2012 Oct 26;3(12):1081-1085.

42.

Amino acid derived quinazolines as Rock/PKA inhibitors.

Chowdhury S, Chen YT, Fang X, Grant W, Pocas J, Cameron MD, Ruiz C, Lin L, Park H, Schröter T, Bannister TD, Lograsso PV, Feng Y.

Bioorg Med Chem Lett. 2013 Mar 15;23(6):1592-9. doi: 10.1016/j.bmcl.2013.01.109. Epub 2013 Jan 31.

PMID:
23416002
43.

Small molecule amides as potent ROR-γ selective modulators.

Khan PM, El-Gendy Bel-D, Kumar N, Garcia-Ordonez R, Lin L, Ruiz CH, Cameron MD, Griffin PR, Kamenecka TM.

Bioorg Med Chem Lett. 2013 Jan 15;23(2):532-6. doi: 10.1016/j.bmcl.2012.11.025. Epub 2012 Nov 22.

44.

Discovery of a highly selective CYP3A4 inhibitor suitable for reaction phenotyping studies and differentiation of CYP3A4 and CYP3A5.

Li X, Song X, Kamenecka TM, Cameron MD.

Drug Metab Dispos. 2012 Sep;40(9):1803-9. doi: 10.1124/dmd.112.046144. Epub 2012 Jun 13.

45.

Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα.

Shin Y, Noel R, Banerjee S, Kojetin D, Song X, He Y, Lin L, Cameron MD, Burris TP, Kamenecka TM.

Bioorg Med Chem Lett. 2012 Jul 1;22(13):4413-7. doi: 10.1016/j.bmcl.2012.04.126. Epub 2012 May 8.

46.

Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists.

Jiang R, Song X, Bali P, Smith A, Bayona CR, Lin L, Cameron MD, McDonald PH, Kenny PJ, Kamenecka TM.

Bioorg Med Chem Lett. 2012 Jun 15;22(12):3890-4. doi: 10.1016/j.bmcl.2012.04.122. Epub 2012 May 4.

47.

Synthesis and SAR of tetrahydroisoquinolines as Rev-erbα agonists.

Noel R, Song X, Shin Y, Banerjee S, Kojetin D, Lin L, Ruiz CH, Cameron MD, Burris TP, Kamenecka TM.

Bioorg Med Chem Lett. 2012 Jun 1;22(11):3739-42. doi: 10.1016/j.bmcl.2012.04.023. Epub 2012 Apr 13.

48.

Potential role of a quetiapine metabolite in quetiapine-induced neutropenia and agranulocytosis.

Li X, Cameron MD.

Chem Res Toxicol. 2012 May 21;25(5):1004-11. doi: 10.1021/tx2005635. Epub 2012 Apr 25.

PMID:
22506851
49.

Regulation of circadian behaviour and metabolism by synthetic REV-ERB agonists.

Solt LA, Wang Y, Banerjee S, Hughes T, Kojetin DJ, Lundasen T, Shin Y, Liu J, Cameron MD, Noel R, Yoo SH, Takahashi JS, Butler AA, Kamenecka TM, Burris TP.

Nature. 2012 Mar 29;485(7396):62-8. doi: 10.1038/nature11030.

50.

A murine lung cancer co-clinical trial identifies genetic modifiers of therapeutic response.

Chen Z, Cheng K, Walton Z, Wang Y, Ebi H, Shimamura T, Liu Y, Tupper T, Ouyang J, Li J, Gao P, Woo MS, Xu C, Yanagita M, Altabef A, Wang S, Lee C, Nakada Y, Peña CG, Sun Y, Franchetti Y, Yao C, Saur A, Cameron MD, Nishino M, Hayes DN, Wilkerson MD, Roberts PJ, Lee CB, Bardeesy N, Butaney M, Chirieac LR, Costa DB, Jackman D, Sharpless NE, Castrillon DH, Demetri GD, Jänne PA, Pandolfi PP, Cantley LC, Kung AL, Engelman JA, Wong KK.

Nature. 2012 Mar 18;483(7391):613-7. doi: 10.1038/nature10937.

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