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Items: 9


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.


Engineering Antibody Reactivity for Efficient Derivatization to Generate NaV1.7 Inhibitory GpTx-1 Peptide-Antibody Conjugates.

Biswas K, Nixey TE, Murray JK, Falsey JR, Yin L, Liu H, Gingras J, Hall BE, Herberich B, Holder JR, Li H, Ligutti J, Lin MJ, Liu D, Soriano BD, Soto M, Tran L, Tegley CM, Zou A, Gunasekaran K, Moyer BD, Doherty L, Miranda LP.

ACS Chem Biol. 2017 Sep 15;12(9):2427-2435. doi: 10.1021/acschembio.7b00542. Epub 2017 Aug 28.


N-substituted azaindoles as potent inhibitors of Cdc7 kinase.

Bryan MC, Falsey JR, Frohn M, Reichelt A, Yao G, Bartberger MD, Bailis JM, Zalameda L, Miguel TS, Doherty EM, Allen JG.

Bioorg Med Chem Lett. 2013 Apr 1;23(7):2056-60. doi: 10.1016/j.bmcl.2013.02.007. Epub 2013 Feb 13.


Discovery of selective biaryl ethers as PDE10A inhibitors: improvement in potency and mitigation of Pgp-mediated efflux.

Rzasa RM, Hu E, Rumfelt S, Chen N, Andrews KL, Chmait S, Falsey JR, Zhong W, Jones AD, Porter A, Louie SW, Zhao X, Treanor JJ, Allen JR.

Bioorg Med Chem Lett. 2012 Dec 15;22(24):7371-5. doi: 10.1016/j.bmcl.2012.10.078. Epub 2012 Oct 22.


Rapid development of piperidine carboxamides as potent and selective anaplastic lymphoma kinase inhibitors.

Bryan MC, Whittington DA, Doherty EM, Falsey JR, Cheng AC, Emkey R, Brake RL, Lewis RT.

J Med Chem. 2012 Feb 23;55(4):1698-705. doi: 10.1021/jm201565s. Epub 2012 Feb 9.


Palladium-catalyzed chemoselective monoarylation of hydrazides for the synthesis of [1,2,4]triazolo[4,3-a]pyridines.

Reichelt A, Falsey JR, Rzasa RM, Thiel OR, Achmatowicz MM, Larsen RD, Zhang D.

Org Lett. 2010 Feb 19;12(4):792-5. doi: 10.1021/ol902868q.


Discovery of highly selective and potent p38 inhibitors based on a phthalazine scaffold.

Herberich B, Cao GQ, Chakrabarti PP, Falsey JR, Pettus L, Rzasa RM, Reed AB, Reichelt A, Sham K, Thaman M, Wurz RP, Xu S, Zhang D, Hsieh F, Lee MR, Syed R, Li V, Grosfeld D, Plant MH, Henkle B, Sherman L, Middleton S, Wong LM, Tasker AS.

J Med Chem. 2008 Oct 23;51(20):6271-9. doi: 10.1021/jm8005417. Epub 2008 Sep 26.


Peptide and small molecule microarray for high throughput cell adhesion and functional assays.

Falsey JR, Renil M, Park S, Li S, Lam KS.

Bioconjug Chem. 2001 May-Jun;12(3):346-53.


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