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Items: 15


Use of Cryopreserved Hepatocytes as Part of an Integrated Strategy to Characterize In Vivo Clearance for Peptide-Antibody Conjugate Inhibitors of Nav1.7 in Preclinical Species.

Foti RS, Biswas K, Aral J, Be X, Berry L, Cheng Y, Conner K, Falsey JR, Glaus C, Herberich B, Hickman D, Ikotun T, Li H, Long J, Huang L, Miranda LP, Murray J, Moyer B, Netirojjanakul C, Nixey TE, Sham K, Soto M, Tegley CM, Tran L, Wu B, Yin L, Rock DA.

Drug Metab Dispos. 2019 Aug 6. pii: dmd.119.087742. doi: 10.1124/dmd.119.087742. [Epub ahead of print]


Engineering NaV1.7 Inhibitory JzTx-V Peptides with a Potency and Basicity Profile Suitable for Antibody Conjugation To Enhance Pharmacokinetics.

Murray JK, Wu B, Tegley CM, Nixey TE, Falsey JR, Herberich B, Yin L, Sham K, Long J, Aral J, Cheng Y, Netirojjanakul C, Doherty L, Glaus C, Ikotun T, Li H, Tran L, Soto M, Salimi-Moosavi H, Ligutti J, Amagasu S, Andrews KL, Be X, Lin MJ, Foti RS, Ilch CP, Youngblood B, Kornecook TJ, Karow M, Walker KW, Moyer BD, Biswas K, Miranda LP.

ACS Chem Biol. 2019 Apr 19;14(4):806-818. doi: 10.1021/acschembio.9b00183. Epub 2019 Mar 27.


Discovery of Tarantula Venom-Derived NaV1.7-Inhibitory JzTx-V Peptide 5-Br-Trp24 Analogue AM-6120 with Systemic Block of Histamine-Induced Pruritis.

Wu B, Murray JK, Andrews KL, Sham K, Long J, Aral J, Ligutti J, Amagasu S, Liu D, Zou A, Min X, Wang Z, Ilch CP, Kornecook TJ, Lin MJ, Be X, Miranda LP, Moyer BD, Biswas K.

J Med Chem. 2018 Nov 8;61(21):9500-9512. doi: 10.1021/acs.jmedchem.8b00736. Epub 2018 Oct 22.


Pharmacologic Characterization of AMG8379, a Potent and Selective Small Molecule Sulfonamide Antagonist of the Voltage-Gated Sodium Channel NaV1.7.

Kornecook TJ, Yin R, Altmann S, Be X, Berry V, Ilch CP, Jarosh M, Johnson D, Lee JH, Lehto SG, Ligutti J, Liu D, Luther J, Matson D, Ortuno D, Roberts J, Taborn K, Wang J, Weiss MM, Yu V, Zhu DXD, Fremeau RT Jr, Moyer BD.

J Pharmacol Exp Ther. 2017 Jul;362(1):146-160. doi: 10.1124/jpet.116.239590. Epub 2017 May 4.


Discovery of N-(4-(3-(2-aminopyrimidin-4-yl)pyridin-2-yloxy)phenyl)-4-(4-methylthiophen-2-yl)phthalazin-1-amine (AMG 900), a highly selective, orally bioavailable inhibitor of aurora kinases with activity against multidrug-resistant cancer cell lines.

Geuns-Meyer S, Cee VJ, Deak HL, Du B, Hodous BL, Nguyen HN, Olivieri PR, Schenkel LB, Vaida KR, Andrews P, Bak A, Be X, Beltran PJ, Bush TL, Chaves MK, Chung G, Dai Y, Eden P, Hanestad K, Huang L, Lin MH, Tang J, Ziegler B, Radinsky R, Kendall R, Patel VF, Payton M.

J Med Chem. 2015 Jul 9;58(13):5189-207. doi: 10.1021/acs.jmedchem.5b00183. Epub 2015 May 31.


LC-MS/MS bioanalytical method development for AMG 900: resolution of an isobaric interference in rodent in vivo studies.

Be X, Moore ES, Zhao Z, Wells MC.

J Pharm Biomed Anal. 2013 Feb 23;74:171-7. doi: 10.1016/j.jpba.2012.10.026. Epub 2012 Nov 2.


Deletion of Abcg2 has differential effects on excretion and pharmacokinetics of probe substrates in rats.

Huang L, Be X, Tchaparian EH, Colletti AE, Roberts J, Langley M, Ling Y, Wong BK, Jin L.

J Pharmacol Exp Ther. 2012 Nov;343(2):316-24. doi: 10.1124/jpet.112.197046. Epub 2012 Aug 6.


Use of uptake intrinsic clearance from attached rat hepatocytes to predict hepatic clearance for poorly permeable compounds.

Huang L, Chen A, Roberts J, Janosky B, Be X, Berry L, Lin MH.

Xenobiotica. 2012 Sep;42(9):830-40. doi: 10.3109/00498254.2012.667847. Epub 2012 Mar 22.


Discovery of triazine-benzimidazoles as selective inhibitors of mTOR.

Peterson EA, Andrews PS, Be X, Boezio AA, Bush TL, Cheng AC, Coats JR, Colletti AE, Copeland KW, DuPont M, Graceffa R, Grubinska B, Harmange JC, Kim JL, Mullady EL, Olivieri P, Schenkel LB, Stanton MK, Teffera Y, Whittington DA, Cai T, La DS.

Bioorg Med Chem Lett. 2011 Apr 1;21(7):2064-70. doi: 10.1016/j.bmcl.2011.02.007. Epub 2011 Feb 12.


In vitro and in vivo pharmacokinetic characterizations of AMG 900, an orally bioavailable small molecule inhibitor of aurora kinases.

Huang L, Be X, Berry L, Moore E, Janosky B, Wells M, Pan WJ, Zhao Z, Lin MH.

Xenobiotica. 2011 May;41(5):400-8. doi: 10.3109/00498254.2010.548534. Epub 2011 Feb 4.


Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.

Cee VJ, Schenkel LB, Hodous BL, Deak HL, Nguyen HN, Olivieri PR, Romero K, Bak A, Be X, Bellon S, Bush TL, Cheng AC, Chung G, Coats S, Eden PM, Hanestad K, Gallant PL, Gu Y, Huang X, Kendall RL, Lin MH, Morrison MJ, Patel VF, Radinsky R, Rose PE, Ross S, Sun JR, Tang J, Zhao H, Payton M, Geuns-Meyer SD.

J Med Chem. 2010 Sep 9;53(17):6368-77. doi: 10.1021/jm100394y.


Prediction of V(ss) from in vitro tissue-binding studies.

Berry LM, Roberts J, Be X, Zhao Z, Lin MH.

Drug Metab Dispos. 2010 Jan;38(1):115-21. doi: 10.1124/dmd.109.029629.


Detecting and profiling tissue-selective genes.

Liang S, Li Y, Be X, Howes S, Liu W.

Physiol Genomics. 2006 Jul 12;26(2):158-62. Epub 2006 May 9.


Solution structure determination and mutational analysis of the papillomavirus E6 interacting peptide of E6AP.

Be X, Hong Y, Wei J, Androphy EJ, Chen JJ, Baleja JD.

Biochemistry. 2001 Feb 6;40(5):1293-9.


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