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Items: 29


Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.

Zhou H, McGowan MA, Lipford K, Christopher M, Fradera X, Witter D, Lesburg CA, Li C, Methot JL, Lampe J, Achab A, Shaffer L, Goldenblatt P, Shah S, Bass A, Schroeder G, Chen D, Zeng H, Augustin MA, Katz JD.

Bioorg Med Chem Lett. 2020 Jan 1;30(1):126715. doi: 10.1016/j.bmcl.2019.126715. Epub 2019 Oct 18.


Discovery of Amino-cyclobutarene-derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors for Cancer Immunotherapy.

Zhang H, Liu K, Pu Q, Achab A, Ardolino MJ, Cheng M, Deng Y, Doty AC, Ferguson H, Fradera X, Knemeyer I, Kurukulasuriya R, Lam YH, Lesburg CA, Martinot TA, McGowan MA, Miller JR, Otte K, Biju PJ, Sciammetta N, Solban N, Yu W, Zhou H, Wang X, Bennett DJ, Han Y.

ACS Med Chem Lett. 2019 Sep 18;10(11):1530-1536. doi: 10.1021/acsmedchemlett.9b00344. eCollection 2019 Nov 14.


Design of selective PI3Kδ inhibitors using an iterative scaffold-hopping workflow.

Fradera X, Methot JL, Achab A, Christopher M, Altman MD, Zhou H, McGowan MA, Kattar SD, Wilson K, Garcia Y, Augustin MA, Lesburg CA, Shah S, Goldenblatt P, Katz JD.

Bioorg Med Chem Lett. 2019 Sep 15;29(18):2575-2580. doi: 10.1016/j.bmcl.2019.08.004. Epub 2019 Aug 5.


Discovery of a Novel cGAMP Competitive Ligand of the Inactive Form of STING.

Siu T, Altman MD, Baltus GA, Childers M, Ellis JM, Gunaydin H, Hatch H, Ho T, Jewell J, Lacey BM, Lesburg CA, Pan BS, Sauvagnat B, Schroeder GK, Xu S.

ACS Med Chem Lett. 2018 Dec 6;10(1):92-97. doi: 10.1021/acsmedchemlett.8b00466. eCollection 2019 Jan 10.



Lesburg CA.

Methods Enzymol. 2018;610:xiii-xiv. doi: 10.1016/S0076-6879(18)30454-3. No abstract available.


The Discovery of 3-((4-Chloro-3-methoxyphenyl)amino)-1-((3R,4S)-4-cyanotetrahydro-2H-pyran-3-yl)-1H-pyrazole-4-carboxamide, a Highly Ligand Efficient and Efficacious Janus Kinase 1 Selective Inhibitor with Favorable Pharmacokinetic Properties.

Siu T, Brubaker J, Fuller P, Torres L, Zeng H, Close J, Mampreian DM, Shi F, Liu D, Fradera X, Johnson K, Bays N, Kadic E, He F, Goldenblatt P, Shaffer L, Patel SB, Lesburg CA, Alpert C, Dorosh L, Deshmukh SV, Yu H, Klappenbach J, Elwood F, Dinsmore CJ, Fernandez R, Moy L, Young JR.

J Med Chem. 2017 Dec 14;60(23):9676-9690. doi: 10.1021/acs.jmedchem.7b01135. Epub 2017 Dec 4.


Development of a New Structural Class of Broadly Acting HCV Non-Nucleoside Inhibitors Leading to the Discovery of MK-8876.

McComas CC, Palani A, Chang W, Holloway MK, Lesburg CA, Li P, Liverton N, Meinke PT, Olsen DB, Peng X, Soll RM, Ummat A, Wu J, Wu J, Zorn N, Ludmerer SW.

ChemMedChem. 2017 Sep 7;12(17):1436-1448. doi: 10.1002/cmdc.201700228. Epub 2017 Jul 25.


Discovery of SCH 900188: A Potent Hepatitis C Virus NS5B Polymerase Inhibitor Prodrug As a Development Candidate.

Chen KX, Venkatraman S, Anilkumar GN, Zeng Q, Lesburg CA, Vibulbhan B, Velazquez F, Chan TY, Bennet F, Jiang Y, Pinto P, Huang Y, Selyutin O, Agrawal S, Huang HC, Li C, Cheng KC, Shih NY, Kozlowski JA, Rosenblum SB, Njoroge FG.

ACS Med Chem Lett. 2013 Aug 12;5(3):244-8. doi: 10.1021/ml400192w. eCollection 2014 Mar 13.


Discovery of an irreversible HCV NS5B polymerase inhibitor.

Zeng Q, Nair AG, Rosenblum SB, Huang HC, Lesburg CA, Jiang Y, Selyutin O, Chan TY, Bennett F, Chen KX, Venkatraman S, Sannigrahi M, Velazquez F, Duca JS, Gavalas S, Huang Y, Pu H, Wang L, Pinto P, Vibulbhan B, Agrawal S, Ferrari E, Jiang CK, Li C, Hesk D, Gesell J, Sorota S, Shih NY, Njoroge FG, Kozlowski JA.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6585-7. doi: 10.1016/j.bmcl.2013.10.060. Epub 2013 Nov 6.


A novel class of highly potent irreversible hepatitis C virus NS5B polymerase inhibitors.

Chen KX, Lesburg CA, Vibulbhan B, Yang W, Chan TY, Venkatraman S, Velazquez F, Zeng Q, Bennett F, Anilkumar GN, Duca J, Jiang Y, Pinto P, Wang L, Huang Y, Selyutin O, Gavalas S, Pu H, Agrawal S, Feld B, Huang HC, Li C, Cheng KC, Shih NY, Kozlowski JA, Rosenblum SB, Njoroge FG.

J Med Chem. 2012 Mar 8;55(5):2089-101. doi: 10.1021/jm201322r. Epub 2012 Feb 22.


Synthesis of new 4,5-dihydrofuranoindoles and their evaluation as HCV NS5B polymerase inhibitors.

Velázquez F, Venkatraman S, Lesburg CA, Duca J, Rosenblum SB, Kozlowski JA, Njoroge FG.

Org Lett. 2012 Jan 20;14(2):556-9. doi: 10.1021/ol203177g. Epub 2012 Jan 5.


Structure-activity relationship (SAR) development and discovery of potent indole-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase.

Chen KX, Vibulbhan B, Yang W, Sannigrahi M, Velazquez F, Chan TY, Venkatraman S, Anilkumar GN, Zeng Q, Bennet F, Jiang Y, Lesburg CA, Duca J, Pinto P, Gavalas S, Huang Y, Wu W, Selyutin O, Agrawal S, Feld B, Huang HC, Li C, Cheng KC, Shih NY, Kozlowski JA, Rosenblum SB, Njoroge FG.

J Med Chem. 2012 Jan 26;55(2):754-65. doi: 10.1021/jm201258k. Epub 2012 Jan 6.


II. Novel HCV NS5B polymerase inhibitors: discovery of indole C2 acyl sulfonamides.

Anilkumar GN, Selyutin O, Rosenblum SB, Zeng Q, Jiang Y, Chan TY, Pu H, Wang L, Bennett F, Chen KX, Lesburg CA, Duca J, Gavalas S, Huang Y, Pinto P, Sannigrahi M, Velazquez F, Venkatraman S, Vibulbhan B, Agrawal S, Ferrari E, Jiang CK, Huang HC, Shih NY, George Njoroge F, Kozlowski JA.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):713-7. doi: 10.1016/j.bmcl.2011.10.041. Epub 2011 Oct 20.


I. Novel HCV NS5B polymerase inhibitors: discovery of indole 2-carboxylic acids with C3-heterocycles.

Anilkumar GN, Lesburg CA, Selyutin O, Rosenblum SB, Zeng Q, Jiang Y, Chan TY, Pu H, Vaccaro H, Wang L, Bennett F, Chen KX, Duca J, Gavalas S, Huang Y, Pinto P, Sannigrahi M, Velazquez F, Venkatraman S, Vibulbhan B, Agrawal S, Butkiewicz N, Feld B, Ferrari E, He Z, Jiang CK, Palermo RE, McMonagle P, Huang HC, Shih NY, Njoroge G, Kozlowski JA.

Bioorg Med Chem Lett. 2011 Sep 15;21(18):5336-41. doi: 10.1016/j.bmcl.2011.07.021. Epub 2011 Jul 19.


Crystallization of an apo form of human arginase: using all the tools in the toolbox simultaneously.

Newman J, Pearce L, Lesburg CA, Strickland C, Peat TS.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2011 Jan 1;67(Pt 1):90-3. doi: 10.1107/S1744309110046208. Epub 2010 Dec 23.


Evaluation of in vitro PXR-based assays and in silico modeling approaches for understanding the binding of a structurally diverse set of drugs to PXR.

Xiao L, Nickbarg E, Wang W, Thomas A, Ziebell M, Prosise WW, Lesburg CA, Taremi SS, Gerlach VL, Le HV, Cheng KC.

Biochem Pharmacol. 2011 Mar 1;81(5):669-79. doi: 10.1016/j.bcp.2010.12.003. Epub 2010 Dec 9.


Inhibitors of hepatitis C virus polymerase: synthesis and characterization of novel 2-oxy-6-fluoro-N-((S)-1-hydroxy-3-phenylpropan-2-yl)-benzamides.

Cheng CC, Shipps GW Jr, Yang Z, Kawahata N, Lesburg CA, Duca JS, Bandouveres J, Bracken JD, Jiang CK, Agrawal S, Ferrari E, Huang HC.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2119-24. doi: 10.1016/j.bmcl.2010.02.054. Epub 2010 Feb 18.


Thermodynamics of nucleotide and inhibitor binding to wild-type and ispinesib-resistant forms of human kinesin spindle protein.

Sheth PR, Basso A, Duca JS, Lesburg CA, Ogas P, Gray K, Nale L, Mannarino AF, Prongay AJ, Le HV.

Biochemistry. 2009 Nov 24;48(46):11045-55. doi: 10.1021/bi900946r.


soaPDB: a web application for searching the Protein Data Bank, organizing results, and receiving automatic email alerts.

Lesburg CA, Duca JS.

Nucleic Acids Res. 2008 Jul 1;36(Web Server issue):W252-4. doi: 10.1093/nar/gkn270. Epub 2008 May 16.


Construction and characterization of a fully active PXR/SRC-1 tethered protein with increased stability.

Wang W, Prosise WW, Chen J, Taremi SS, Le HV, Madison V, Cui X, Thomas A, Cheng KC, Lesburg CA.

Protein Eng Des Sel. 2008 Jul;21(7):425-33. doi: 10.1093/protein/gzn017. Epub 2008 May 2.


Active-site engineering of carbonic anhydrase and its application to biosensors.

Hunt JA, Lesburg CA, Christianson DW, Thompson RB, Fierke CA.

EXS. 2000;(90):221-40. Review. No abstract available.


Recent advances in the analysis of HCV NS5B RNA-dependent RNA polymerase.

Lesburg CA, Radfar R, Weber PC.

Curr Opin Investig Drugs. 2000 Nov;1(3):289-96. Review.


Template/primer requirements and single nucleotide incorporation by hepatitis C virus nonstructural protein 5B polymerase.

Zhong W, Ferrari E, Lesburg CA, Maag D, Ghosh SK, Cameron CE, Lau JY, Hong Z.

J Virol. 2000 Oct;74(19):9134-43.


Crystal structure of the RNA-dependent RNA polymerase from hepatitis C virus reveals a fully encircled active site.

Lesburg CA, Cable MB, Ferrari E, Hong Z, Mannarino AF, Weber PC.

Nat Struct Biol. 1999 Oct;6(10):937-43.


Managing and manipulating carbocations in biology: terpenoid cyclase structure and mechanism.

Lesburg CA, Caruthers JM, Paschall CM, Christianson DW.

Curr Opin Struct Biol. 1998 Dec;8(6):695-703. Review.


Crystal structure of pentalenene synthase: mechanistic insights on terpenoid cyclization reactions in biology.

Lesburg CA, Zhai G, Cane DE, Christianson DW.

Science. 1997 Sep 19;277(5333):1820-4.


Crystallization and preliminary X-ray diffraction analysis of recombinant pentalenene synthase.

Lesburg CA, Lloyd MD, Cane DE, Christianson DW.

Protein Sci. 1995 Nov;4(11):2436-8.

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