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Items: 16

1.

Global Portrait of Protein Targets of Metabolites of the Neurotoxic Compound BIA 10-2474.

Huang Z, Ogasawara D, Seneviratne UI, Cognetta AB 3rd, Am Ende CW, Nason DM, Lapham K, Litchfield J, Johnson DS, Cravatt BF.

ACS Chem Biol. 2019 Feb 15;14(2):192-197. doi: 10.1021/acschembio.8b01097. Epub 2019 Jan 31.

PMID:
30702848
2.

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
3.

Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.

O'Neill BT, Beck EM, Butler CR, Nolan CE, Gonzales C, Zhang L, Doran SD, Lapham K, Buzon LM, Dutra JK, Barreiro G, Hou X, Martinez-Alsina LA, Rogers BN, Villalobos A, Murray JC, Ogilvie K, LaChapelle EA, Chang C, Lanyon LF, Steppan CM, Robshaw A, Hales K, Boucher GG, Pandher K, Houle C, Ambroise CW, Karanian D, Riddell D, Bales KR, Brodney MA.

J Med Chem. 2018 May 24;61(10):4476-4504. doi: 10.1021/acs.jmedchem.8b00246. Epub 2018 Apr 17.

PMID:
29613789
4.

Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.

Butler CR, Ogilvie K, Martinez-Alsina L, Barreiro G, Beck EM, Nolan CE, Atchison K, Benvenuti E, Buzon L, Doran S, Gonzales C, Helal CJ, Hou X, Hsu MH, Johnson EF, Lapham K, Lanyon L, Parris K, O'Neill BT, Riddell D, Robshaw A, Vajdos F, Brodney MA.

J Med Chem. 2017 Jan 12;60(1):386-402. doi: 10.1021/acs.jmedchem.6b01451. Epub 2016 Dec 20.

5.

Inhibition of Hepatobiliary Transport Activity by the Antibacterial Agent Fusidic Acid: Insights into Factors Contributing to Conjugated Hyperbilirubinemia/Cholestasis.

Lapham K, Novak J, Marroquin LD, Swiss R, Qin S, Strock CJ, Scialis R, Aleo MD, Schroeter T, Eng H, Rodrigues AD, Kalgutkar AS.

Chem Res Toxicol. 2016 Oct 17;29(10):1778-1788. doi: 10.1021/acs.chemrestox.6b00262. Epub 2016 Oct 4.

PMID:
27676153
6.

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.

7.

Automated Assay of Telomere Length Measurement and Informatics for 100,000 Subjects in the Genetic Epidemiology Research on Adult Health and Aging (GERA) Cohort.

Lapham K, Kvale MN, Lin J, Connell S, Croen LA, Dispensa BP, Fang L, Hesselson S, Hoffmann TJ, Iribarren C, Jorgenson E, Kushi LH, Ludwig D, Matsuguchi T, McGuire WB, Miles S, Quesenberry CP Jr, Rowell S, Sadler M, Sakoda LC, Smethurst D, Somkin CP, Van Den Eeden SK, Walter L, Whitmer RA, Kwok PY, Risch N, Schaefer C, Blackburn EH.

Genetics. 2015 Aug;200(4):1061-72. doi: 10.1534/genetics.115.178624. Epub 2015 Jun 19.

8.

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.

9.

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.

10.

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
11.

Reactive metabolite trapping studies on imidazo- and 2-methylimidazo[2,1-b]thiazole-based inverse agonists of the ghrelin receptor.

Kalgutkar AS, Ryder TF, Walker GS, Orr ST, Cabral S, Goosen TC, Lapham K, Eng H.

Drug Metab Dispos. 2013 Jul;41(7):1375-88. doi: 10.1124/dmd.113.051839. Epub 2013 Apr 22.

PMID:
23610086
12.

Insights into the novel hydrolytic mechanism of a diethyl 2-phenyl-2-(2-arylacetoxy)methyl malonate ester-based microsomal triglyceride transfer protein (MTP) inhibitor.

Ryder T, Walker GS, Goosen TC, Ruggeri RB, Conn EL, Rocke BN, Lapham K, Steppan CM, Hepworth D, Kalgutkar AS.

Chem Res Toxicol. 2012 Oct 15;25(10):2138-52. doi: 10.1021/tx300243v. Epub 2012 Sep 27.

PMID:
22989032
13.

Optimized assays for human UDP-glucuronosyltransferase (UGT) activities: altered alamethicin concentration and utility to screen for UGT inhibitors.

Walsky RL, Bauman JN, Bourcier K, Giddens G, Lapham K, Negahban A, Ryder TF, Obach RS, Hyland R, Goosen TC.

Drug Metab Dispos. 2012 May;40(5):1051-65. doi: 10.1124/dmd.111.043117. Epub 2012 Feb 22.

PMID:
22357286
14.

Telomere length trajectory and its determinants in persons with coronary artery disease: longitudinal findings from the heart and soul study.

Farzaneh-Far R, Lin J, Epel E, Lapham K, Blackburn E, Whooley MA.

PLoS One. 2010 Jan 8;5(1):e8612. doi: 10.1371/journal.pone.0008612.

15.

(1R,2S)-4-(2-cyano-cyclohexyl-oxy)-2-trifluoromethyl-benzonitrile, a potent androgen receptor antagonist for stimulating hair growth and reducing sebum production.

Hu LY, Du D, Hoffman J, Smith Y, Fedij V, Kostlan C, Johnson TR, Huang Y, Kesten S, Harter W, Yue WS, Li JJ, Barvian N, Mitchell L, Lei HJ, Lefker B, Carroll M, Dettling D, Krieger-Burke T, Samas B, Yalamanchili R, Lapham K, Pocalyko D, Sliskovic D, Ciotti S, Stoller B, Hena MA, Ding Q, Maiti SN, Stier M, Welgus H.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5983-8. Epub 2007 Aug 21.

PMID:
17827000
16.

Synthesis and biological evaluation of amino-pyridines as androgen receptor antagonists for stimulating hair growth and reducing sebum production.

Hu LY, Lei HJ, Du D, Johnson TR, Fedij V, Kostlan C, Yue WS, Lovdahl M, Li JJ, Carroll M, Dettling D, Asbill J, Fan C, Wade K, Pocalyko D, Lapham K, Yalamanchili R, Samas B, Vrieze D, Ciotti S, Krieger-Burke T, Sliskovic D, Welgus H.

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5693-7. Epub 2007 Aug 19.

PMID:
17766112

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