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Items: 29

1.

6-Chloro-5-[4-(1-Hydroxycyclobutyl)Phenyl]-1H-Indole-3-Carboxylic Acid is a Highly Selective Substrate for Glucuronidation by UGT1A1, Relative to β-Estradiol.

Lapham K, Lin J, Novak J, Orozco C, Niosi M, Di L, Goosen TC, Ryu S, Riccardi K, Eng H, Cameron KO, Kalgutkar AS.

Drug Metab Dispos. 2018 Dec;46(12):1836-1846. doi: 10.1124/dmd.118.083709. Epub 2018 Sep 7.

PMID:
30194276
2.

Acyl Glucuronide Metabolites of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1 H-indole-3-carboxylic Acid (PF-06409577) and Related Indole-3-carboxylic Acid Derivatives are Direct Activators of Adenosine Monophosphate-Activated Protein Kinase (AMPK).

Ryder TF, Calabrese MF, Walker GS, Cameron KO, Reyes AR, Borzilleri KA, Delmore J, Miller R, Kurumbail RG, Ward J, Kung DW, Brown JA, Edmonds DJ, Eng H, Wolford AC, Kalgutkar AS.

J Med Chem. 2018 Aug 23;61(16):7273-7288. doi: 10.1021/acs.jmedchem.8b00807. Epub 2018 Aug 2.

PMID:
30036059
3.

Activation of Liver AMPK with PF-06409577 Corrects NAFLD and Lowers Cholesterol in Rodent and Primate Preclinical Models.

Esquejo RM, Salatto CT, Delmore J, Albuquerque B, Reyes A, Shi Y, Moccia R, Cokorinos E, Peloquin M, Monetti M, Barricklow J, Bollinger E, Smith BK, Day EA, Nguyen C, Geoghegan KF, Kreeger JM, Opsahl A, Ward J, Kalgutkar AS, Tess D, Butler L, Shirai N, Osborne TF, Steinberg GR, Birnbaum MJ, Cameron KO, Miller RA.

EBioMedicine. 2018 May;31:122-132. doi: 10.1016/j.ebiom.2018.04.009. Epub 2018 Apr 8.

4.

Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).

Edmonds DJ, Kung DW, Kalgutkar AS, Filipski KJ, Ebner DC, Cabral S, Smith AC, Aspnes GE, Bhattacharya SK, Borzilleri KA, Brown JA, Calabrese MF, Caspers NL, Cokorinos EC, Conn EL, Dowling MS, Eng H, Feng B, Fernando DP, Genung NE, Herr M, Kurumbail RG, Lavergne SY, Lee EC, Li Q, Mathialagan S, Miller RA, Panteleev J, Polivkova J, Rajamohan F, Reyes AR, Salatto CT, Shavnya A, Thuma BA, Tu M, Ward J, Withka JM, Xiao J, Cameron KO.

J Med Chem. 2018 Mar 22;61(6):2372-2383. doi: 10.1021/acs.jmedchem.7b01641. Epub 2018 Feb 28.

PMID:
29466005
5.

Activation of Skeletal Muscle AMPK Promotes Glucose Disposal and Glucose Lowering in Non-human Primates and Mice.

Cokorinos EC, Delmore J, Reyes AR, Albuquerque B, Kjøbsted R, Jørgensen NO, Tran JL, Jatkar A, Cialdea K, Esquejo RM, Meissen J, Calabrese MF, Cordes J, Moccia R, Tess D, Salatto CT, Coskran TM, Opsahl AC, Flynn D, Blatnik M, Li W, Kindt E, Foretz M, Viollet B, Ward J, Kurumbail RG, Kalgutkar AS, Wojtaszewski JFP, Cameron KO, Miller RA.

Cell Metab. 2017 May 2;25(5):1147-1159.e10. doi: 10.1016/j.cmet.2017.04.010.

6.

Selective Activation of AMPK β1-Containing Isoforms Improves Kidney Function in a Rat Model of Diabetic Nephropathy.

Salatto CT, Miller RA, Cameron KO, Cokorinos E, Reyes A, Ward J, Calabrese MF, Kurumbail RG, Rajamohan F, Kalgutkar AS, Tess DA, Shavnya A, Genung NE, Edmonds DJ, Jatkar A, Maciejewski BS, Amaro M, Gandhok H, Monetti M, Cialdea K, Bollinger E, Kreeger JM, Coskran TM, Opsahl AC, Boucher GG, Birnbaum MJ, DaSilva-Jardine P, Rolph T.

J Pharmacol Exp Ther. 2017 May;361(2):303-311. doi: 10.1124/jpet.116.237925. Epub 2017 Mar 13.

PMID:
28289077
7.

Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators.

Cameron KO, Kurumbail RG.

Bioorg Med Chem Lett. 2016 Nov 1;26(21):5139-5148. doi: 10.1016/j.bmcl.2016.09.065. Epub 2016 Sep 28. Review.

PMID:
27727125
8.

Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy.

Cameron KO, Kung DW, Kalgutkar AS, Kurumbail RG, Miller R, Salatto CT, Ward J, Withka JM, Bhattacharya SK, Boehm M, Borzilleri KA, Brown JA, Calabrese M, Caspers NL, Cokorinos E, Conn EL, Dowling MS, Edmonds DJ, Eng H, Fernando DP, Frisbie R, Hepworth D, Landro J, Mao Y, Rajamohan F, Reyes AR, Rose CR, Ryder T, Shavnya A, Smith AC, Tu M, Wolford AC, Xiao J.

J Med Chem. 2016 Sep 8;59(17):8068-81. doi: 10.1021/acs.jmedchem.6b00866. Epub 2016 Aug 20.

PMID:
27490827
9.

Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent insulin secretion ex vivo.

Kong J, Chuddy J, Stock IA, Loria PM, Straub SV, Vage C, Cameron KO, Bhattacharya SK, Lapham K, McClure KF, Zhang Y, Jackson VM.

Br J Pharmacol. 2016 May;173(9):1452-64. doi: 10.1111/bph.13439. Epub 2016 Mar 17.

10.

Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.

Orr ST, Beveridge R, Bhattacharya SK, Cameron KO, Coffey S, Fernando D, Hepworth D, Jackson MV, Khot V, Kosa R, Lapham K, Loria PM, McClure KF, Patel J, Rose C, Saenz J, Stock IA, Storer G, von Volkenburg M, Vrieze D, Wang G, Xiao J, Zhang Y.

ACS Med Chem Lett. 2014 Dec 14;6(2):156-61. doi: 10.1021/ml500414n. eCollection 2015 Feb 12.

11.

Structural basis for AMPK activation: natural and synthetic ligands regulate kinase activity from opposite poles by different molecular mechanisms.

Calabrese MF, Rajamohan F, Harris MS, Caspers NL, Magyar R, Withka JM, Wang H, Borzilleri KA, Sahasrabudhe PV, Hoth LR, Geoghegan KF, Han S, Brown J, Subashi TA, Reyes AR, Frisbie RK, Ward J, Miller RA, Landro JA, Londregan AT, Carpino PA, Cabral S, Smith AC, Conn EL, Cameron KO, Qiu X, Kurumbail RG.

Structure. 2014 Aug 5;22(8):1161-1172. doi: 10.1016/j.str.2014.06.009. Epub 2014 Jul 24.

12.

Small molecule ghrelin receptor inverse agonists and antagonists.

Cameron KO, Bhattacharya SK, Loomis AK.

J Med Chem. 2014 Nov 13;57(21):8671-91. doi: 10.1021/jm5003183. Epub 2014 Aug 6. Review.

PMID:
25036503
13.

Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate.

Bhattacharya SK, Andrews K, Beveridge R, Cameron KO, Chen C, Dunn M, Fernando D, Gao H, Hepworth D, Jackson VM, Khot V, Kong J, Kosa RE, Lapham K, Loria PM, Londregan AT, McClure KF, Orr ST, Patel J, Rose C, Saenz J, Stock IA, Storer G, VanVolkenburg M, Vrieze D, Wang G, Xiao J, Zhang Y.

ACS Med Chem Lett. 2014 Feb 24;5(5):474-9. doi: 10.1021/ml400473x. eCollection 2014 May 8.

14.

Chemical Probe Identification Platform for Orphan GPCRs Using Focused Compound Screening: GPR39 as a Case Example.

Boehm M, Hepworth D, Loria PM, Norquay LD, Filipski KJ, Chin JE, Cameron KO, Brenner M, Bonnette P, Cabral S, Conn E, Ebner DC, Gautreau D, Hadcock J, Lee EC, Mathiowetz AM, Morin M, Rogers L, Smith A, VanVolkenburg M, Carpino PA.

ACS Med Chem Lett. 2013 Sep 16;4(11):1079-84. doi: 10.1021/ml400275z. eCollection 2013 Nov 14.

15.

Identification of potent, selective, CNS-targeted inverse agonists of the ghrelin receptor.

McClure KF, Jackson M, Cameron KO, Kung DW, Perry DA, Orr ST, Zhang Y, Kohrt J, Tu M, Gao H, Fernando D, Jones R, Erasga N, Wang G, Polivkova J, Jiao W, Swartz R, Ueno H, Bhattacharya SK, Stock IA, Varma S, Bagdasarian V, Perez S, Kelly-Sullivan D, Wang R, Kong J, Cornelius P, Michael L, Lee E, Janssen A, Steyn SJ, Lapham K, Goosen T.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5410-4. doi: 10.1016/j.bmcl.2013.07.044. Epub 2013 Jul 30.

PMID:
23953189
16.

Medicinal chemistry design principles for liver targeting through OATP transporters.

Tu M, Mathiowetz AM, Pfefferkorn JA, Cameron KO, Dow RL, Litchfield J, Di L, Feng B, Liras S.

Curr Top Med Chem. 2013;13(7):857-66. Review.

PMID:
23578029
17.

Intestinal targeting of drugs: rational design approaches and challenges.

Filipski KJ, Varma MV, El-Kattan AF, Ambler CM, Ruggeri RB, Goosen TC, Cameron KO.

Curr Top Med Chem. 2013;13(7):776-802. Review.

PMID:
23578023
18.

Effects of pressure and electrical charge on macromolecular transport across bovine lens basement membrane.

Ferrell N, Cameron KO, Groszek JJ, Hofmann CL, Li L, Smith RA, Bian A, Shintani A, Zydney AL, Fissell WH.

Biophys J. 2013 Apr 2;104(7):1476-84. doi: 10.1016/j.bpj.2013.01.062.

19.

Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists.

Cameron KO, Beretta EE, Chen Y, Chu-Moyer M, Fernando D, Gao H, Kohrt J, Lavergne S, Jardine Pda S, Guzman-Perez A, Hoth C, Perry DA, Hadcock JR, Gautreau D, Makowski M, Perez S, Polivkova J, Rogers L, Scott DO, Swick AG, Thiede L, Trebino CE, Trilles RV, Wilmowski J, Zhang Y.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2943-7. doi: 10.1016/j.bmcl.2012.02.049. Epub 2012 Feb 23.

PMID:
22424974
20.

Discovery of N-benzyl-2-[(4S)-4-(1H-indol-3-ylmethyl)-5-oxo-1-phenyl-4,5-dihydro-6H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepin-6-yl]-N-isopropylacetamide, an orally active, gut-selective CCK1 receptor agonist for the potential treatment of obesity.

Elliott RL, Cameron KO, Chin JE, Bartlett JA, Beretta EE, Chen Y, Jardine Pda S, Dubins JS, Gillaspy ML, Hargrove DM, Kalgutkar AS, LaFlamme JA, Lame ME, Martin KA, Maurer TS, Nardone NA, Oliver RM, Scott DO, Sun D, Swick AG, Trebino CE, Zhang Y.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6797-801. doi: 10.1016/j.bmcl.2010.08.115. Epub 2010 Sep 28.

PMID:
20851601
21.

Discovery of CP-533536: an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation.

Cameron KO, Lefker BA, Ke HZ, Li M, Zawistoski MP, Tjoa CM, Wright AS, DeNinno SL, Paralkar VM, Owen TA, Yu L, Thompson DD.

Bioorg Med Chem Lett. 2009 Apr 1;19(7):2075-8. doi: 10.1016/j.bmcl.2009.01.059. Epub 2009 Jan 23.

PMID:
19250823
22.

A nonprostanoid EP4 receptor selective prostaglandin E2 agonist restores bone mass and strength in aged, ovariectomized rats.

Ke HZ, Crawford DT, Qi H, Simmons HA, Owen TA, Paralkar VM, Li M, Lu B, Grasser WA, Cameron KO, Lefker BA, DaSilva-Jardine P, Scott DO, Zhang Q, Tian XY, Jee WS, Brown TA, Thompson DD.

J Bone Miner Res. 2006 Apr;21(4):565-75. Epub 2006 Apr 5.

23.

Discovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized rats.

Cameron KO, Lefker BA, Chu-Moyer MY, Crawford DT, Jardine PD, DeNinno SL, Gilbert S, Grasser WA, Ke H, Lu B, Owen TA, Paralkar VM, Qi H, Scott DO, Thompson DD, Tjoa CM, Zawistoski MP.

Bioorg Med Chem Lett. 2006 Apr 1;16(7):1799-802. Epub 2006 Jan 26.

PMID:
16442794
24.

Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.

Chesworth R, Wessel MD, Heyden L, Mangano FM, Zawistoski M, Gegnas L, Galluzzo D, Lefker B, Cameron KO, Tickner J, Lu B, Castleberry TA, Petersen DN, Brault A, Perry P, Ng O, Owen TA, Pan L, Ke HZ, Brown TA, Thompson DD, DaSilva-Jardine P.

Bioorg Med Chem Lett. 2005 Dec 15;15(24):5562-6. Epub 2005 Oct 10.

PMID:
16219463
25.

Tetrahydroisoquinolines as subtype selective estrogen agonists/antagonists.

Chesworth R, Zawistoski MP, Lefker BA, Cameron KO, Day RF, Mangano FM, Rosati RL, Colella S, Petersen DN, Brault A, Lu B, Pan LC, Perry P, Ng O, Castleberry TA, Owen TA, Brown TA, Thompson DD, DaSilva-Jardine P.

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2729-33.

PMID:
15125923
26.

A novel, non-prostanoid EP2 receptor-selective prostaglandin E2 agonist stimulates local bone formation and enhances fracture healing.

Li M, Ke HZ, Qi H, Healy DR, Li Y, Crawford DT, Paralkar VM, Owen TA, Cameron KO, Lefker BA, Brown TA, Thompson DD.

J Bone Miner Res. 2003 Nov;18(11):2033-42.

27.

An EP2 receptor-selective prostaglandin E2 agonist induces bone healing.

Paralkar VM, Borovecki F, Ke HZ, Cameron KO, Lefker B, Grasser WA, Owen TA, Li M, DaSilva-Jardine P, Zhou M, Dunn RL, Dumont F, Korsmeyer R, Krasney P, Brown TA, Plowchalk D, Vukicevic S, Thompson DD.

Proc Natl Acad Sci U S A. 2003 May 27;100(11):6736-40. Epub 2003 May 14.

28.

Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene.

Rosati RL, Da Silva Jardine P, Cameron KO, Thompson DD, Ke HZ, Toler SM, Brown TA, Pan LC, Ebbinghaus CF, Reinhold AR, Elliott NC, Newhouse BN, Tjoa CM, Sweetnam PM, Cole MJ, Arriola MW, Gauthier JW, Crawford DT, Nickerson DF, Pirie CM, Qi H, Simmons HA, Tkalcevic GT.

J Med Chem. 1998 Jul 30;41(16):2928-31. No abstract available.

PMID:
9685230
29.

Effects of CP-336,156, a new, nonsteroidal estrogen agonist/antagonist, on bone, serum cholesterol, uterus and body composition in rat models.

Ke HZ, Paralkar VM, Grasser WA, Crawford DT, Qi H, Simmons HA, Pirie CM, Chidsey-Frink KL, Owen TA, Smock SL, Chen HK, Jee WS, Cameron KO, Rosati RL, Brown TA, Dasilva-Jardine P, Thompson DD.

Endocrinology. 1998 Apr;139(4):2068-76.

PMID:
9528995

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