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Items: 40

1.

PF-06651600, a Dual JAK3/TEC Family Kinase Inhibitor.

Xu H, Jesson MI, Seneviratne UI, Lin TH, Sharif MN, Xue L, Nguyen C, Everley RA, Trujillo JI, Johnson DS, Point GR, Thorarensen A, Kilty I, Telliez JB.

ACS Chem Biol. 2019 May 22. doi: 10.1021/acschembio.9b00188. [Epub ahead of print]

PMID:
31082193
2.

Identification of Cyanamide-Based Janus Kinase 3 (JAK3) Covalent Inhibitors.

Casimiro-Garcia A, Trujillo JI, Vajdos F, Juba B, Banker ME, Aulabaugh A, Balbo P, Bauman J, Chrencik J, Coe JW, Czerwinski R, Dowty M, Knafels JD, Kwon S, Leung L, Liang S, Robinson RP, Telliez JB, Unwalla R, Yang X, Thorarensen A.

J Med Chem. 2018 Dec 13;61(23):10665-10699. doi: 10.1021/acs.jmedchem.8b01308. Epub 2018 Nov 30.

PMID:
30423248
3.

Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.

Schnute ME, Wennerstål M, Alley J, Bengtsson M, Blinn JR, Bolten CW, Braden T, Bonn T, Carlsson B, Caspers N, Chen M, Choi C, Collis LP, Crouse K, Färnegårdh M, Fennell KF, Fish S, Flick AC, Goos-Nilsson A, Gullberg H, Harris PK, Heasley SE, Hegen M, Hromockyj AE, Hu X, Husman B, Janosik T, Jones P, Kaila N, Kallin E, Kauppi B, Kiefer JR, Knafels J, Koehler K, Kruger L, Kurumbail RG, Kyne RE Jr, Li W, Löfstedt J, Long SA, Menard CA, Mente S, Messing D, Meyers MJ, Napierata L, Nöteberg D, Nuhant P, Pelc MJ, Prinsen MJ, Rhönnstad P, Backström-Rydin E, Sandberg J, Sandström M, Shah F, Sjöberg M, Sundell A, Taylor AP, Thorarensen A, Trujillo JI, Trzupek JD, Unwalla R, Vajdos FF, Weinberg RA, Wood DC, Xing L, Zamaratski E, Zapf CW, Zhao Y, Wilhelmsson A, Berstein G.

J Med Chem. 2018 Dec 13;61(23):10415-10439. doi: 10.1021/acs.jmedchem.8b00392. Epub 2018 Sep 9.

PMID:
30130103
4.

Microfluidic-Enabled Intracellular Delivery of Membrane Impermeable Inhibitors to Study Target Engagement in Human Primary Cells.

Li J, Wang B, Juba BM, Vazquez M, Kortum SW, Pierce BS, Pacheco M, Roberts L, Strohbach JW, Jones LH, Hett E, Thorarensen A, Telliez JB, Sharei A, Bunnage M, Gilbert JB.

ACS Chem Biol. 2017 Dec 15;12(12):2970-2974. doi: 10.1021/acschembio.7b00683. Epub 2017 Nov 13.

PMID:
29088528
5.

Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-((2S,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans.

Thorarensen A, Dowty ME, Banker ME, Juba B, Jussif J, Lin T, Vincent F, Czerwinski RM, Casimiro-Garcia A, Unwalla R, Trujillo JI, Liang S, Balbo P, Che Y, Gilbert AM, Brown MF, Hayward M, Montgomery J, Leung L, Yang X, Soucy S, Hegen M, Coe J, Langille J, Vajdos F, Chrencik J, Telliez JB.

J Med Chem. 2017 Mar 9;60(5):1971-1993. doi: 10.1021/acs.jmedchem.6b01694. Epub 2017 Feb 16.

PMID:
28139931
6.

Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition.

Telliez JB, Dowty ME, Wang L, Jussif J, Lin T, Li L, Moy E, Balbo P, Li W, Zhao Y, Crouse K, Dickinson C, Symanowicz P, Hegen M, Banker ME, Vincent F, Unwalla R, Liang S, Gilbert AM, Brown MF, Hayward M, Montgomery J, Yang X, Bauman J, Trujillo JI, Casimiro-Garcia A, Vajdos FF, Leung L, Geoghegan KF, Quazi A, Xuan D, Jones L, Hett E, Wright K, Clark JD, Thorarensen A.

ACS Chem Biol. 2016 Dec 16;11(12):3442-3451. Epub 2016 Nov 10.

PMID:
27791347
7.

Clearance Prediction of Targeted Covalent Inhibitors by In Vitro-In Vivo Extrapolation of Hepatic and Extrahepatic Clearance Mechanisms.

Leung L, Yang X, Strelevitz TJ, Montgomery J, Brown MF, Zientek MA, Banfield C, Gilbert AM, Thorarensen A, Dowty ME.

Drug Metab Dispos. 2017 Jan;45(1):1-7. Epub 2016 Oct 26.

PMID:
27784718
8.

Binding site elucidation and structure guided design of macrocyclic IL-17A antagonists.

Liu S, Dakin LA, Xing L, Withka JM, Sahasrabudhe PV, Li W, Banker ME, Balbo P, Shanker S, Chrunyk BA, Guo Z, Chen JM, Young JA, Bai G, Starr JT, Wright SW, Bussenius J, Tan S, Gopalsamy A, Lefker BA, Vincent F, Jones LH, Xu H, Hoth LR, Geoghegan KF, Qiu X, Bunnage ME, Thorarensen A.

Sci Rep. 2016 Aug 16;6:30859. doi: 10.1038/srep30859.

9.

Inhibiting complex IL-17A and IL-17RA interactions with a linear peptide.

Liu S, Desharnais J, Sahasrabudhe PV, Jin P, Li W, Oates BD, Shanker S, Banker ME, Chrunyk BA, Song X, Feng X, Griffor M, Jimenez J, Chen G, Tumelty D, Bhat A, Bradshaw CW, Woodnutt G, Lappe RW, Thorarensen A, Qiu X, Withka JM, Wood LD.

Sci Rep. 2016 May 17;6:26071. doi: 10.1038/srep26071.

10.

Target the More Druggable Protein States in a Highly Dynamic Protein--Protein Interaction System.

Guo Z, Thorarensen A, Che J, Xing L.

J Chem Inf Model. 2016 Jan 25;56(1):35-45. doi: 10.1021/acs.jcim.5b00503. Epub 2015 Dec 23.

PMID:
26650754
11.

Imidazotriazines: Spleen Tyrosine Kinase (Syk) Inhibitors Identified by Free-Energy Perturbation (FEP).

Lovering F, Aevazelis C, Chang J, Dehnhardt C, Fitz L, Han S, Janz K, Lee J, Kaila N, McDonald J, Moore W, Moretto A, Papaioannou N, Richard D, Ryan MS, Wan ZK, Thorarensen A.

ChemMedChem. 2016 Jan 19;11(2):217-33. doi: 10.1002/cmdc.201500333. Epub 2015 Sep 18.

PMID:
26381330
12.

New spleen tyrosine kinase inhibitors: patent applications published during 2011-2013.

Thorarensen A, Kaila N.

Pharm Pat Anal. 2014 Sep;3(5):523-41. doi: 10.4155/ppa.14.34. Review.

PMID:
25374321
13.

ATP-mediated kinome selectivity: the missing link in understanding the contribution of individual JAK Kinase isoforms to cellular signaling.

Thorarensen A, Banker ME, Fensome A, Telliez JB, Juba B, Vincent F, Czerwinski RM, Casimiro-Garcia A.

ACS Chem Biol. 2014 Jul 18;9(7):1552-8. doi: 10.1021/cb5002125. Epub 2014 May 28.

PMID:
24814050
14.

Identification of type-II inhibitors using kinase structures.

Lovering F, McDonald J, Whitlock GA, Glossop PA, Phillips C, Bent A, Sabnis Y, Ryan M, Fitz L, Lee J, Chang JS, Han S, Kurumbail R, Thorarensen A.

Chem Biol Drug Des. 2012 Nov;80(5):657-64. doi: 10.1111/j.1747-0285.2012.01443.x. Epub 2012 Sep 3.

PMID:
22759374
15.

Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): a tale of two waters.

Trujillo JI, Kiefer JR, Huang W, Day JE, Moon J, Jerome GM, Bono CP, Kornmeier CM, Williams ML, Kuhn C, Rennie GR, Wynn TA, Carron CP, Thorarensen A.

Bioorg Med Chem Lett. 2012 Jun 1;22(11):3795-9. doi: 10.1016/j.bmcl.2012.04.004. Epub 2012 Apr 13.

PMID:
22546671
16.

The 2010 patent landscape for spleen tyrosine kinase inhibitors.

Moretto AF, Dehnhardt C, Kaila N, Papaioannou N, Thorarensen A.

Recent Pat Inflamm Allergy Drug Discov. 2012 May;6(2):97-120. Review.

PMID:
22292554
17.

Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 1: identification of 7-azaspiro[3.5]nonane and 1-oxa-8-azaspiro[4.5]decane as lead scaffolds.

Meyers MJ, Long SA, Pelc MJ, Wang JL, Bowen SJ, Walker MC, Schweitzer BA, Madsen HM, Tenbrink RE, McDonald J, Smith SE, Foltin S, Beidler D, Thorarensen A.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6538-44. doi: 10.1016/j.bmcl.2011.08.055. Epub 2011 Aug 22.

PMID:
21924614
18.

Discovery of novel spirocyclic inhibitors of fatty acid amide hydrolase (FAAH). Part 2. Discovery of 7-azaspiro[3.5]nonane urea PF-04862853, an orally efficacious inhibitor of fatty acid amide hydrolase (FAAH) for pain.

Meyers MJ, Long SA, Pelc MJ, Wang JL, Bowen SJ, Schweitzer BA, Wilcox MV, McDonald J, Smith SE, Foltin S, Rumsey J, Yang YS, Walker MC, Kamtekar S, Beidler D, Thorarensen A.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6545-53. doi: 10.1016/j.bmcl.2011.08.048. Epub 2011 Aug 19.

PMID:
21924613
19.

An analysis of the diaminopyrimidine patent estates describing spleen tyrosine kinase inhibitors by Rigel and Portola.

Moore WJ, Richard D, Thorarensen A.

Expert Opin Ther Pat. 2010 Dec;20(12):1703-22. doi: 10.1517/13543776.2010.534459. Epub 2010 Nov 14. Review.

PMID:
21073366
20.

Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS).

Carron CP, Trujillo JI, Olson KL, Huang W, Hamper BC, Dice T, Neal BE, Pelc MJ, Day JE, Rohrer DC, Kiefer JR, Moon JB, Schweitzer BA, Blake TD, Turner SR, Woerndle R, Case BL, Bono CP, Dilworth VM, Funckes-Shippy CL, Hood BL, Jerome GM, Kornmeier CM, Radabaugh MR, Williams ML, Davies MS, Wegner CD, Welsch DJ, Abraham WM, Warren CJ, Dowty ME, Hua F, Zutshi A, Yang JZ, Thorarensen A.

ACS Med Chem Lett. 2010 Feb 2;1(2):59-63. doi: 10.1021/ml900025z. eCollection 2010 May 13.

21.

A novel autotaxin inhibitor reduces lysophosphatidic acid levels in plasma and the site of inflammation.

Gierse J, Thorarensen A, Beltey K, Bradshaw-Pierce E, Cortes-Burgos L, Hall T, Johnston A, Murphy M, Nemirovskiy O, Ogawa S, Pegg L, Pelc M, Prinsen M, Schnute M, Wendling J, Wene S, Weinberg R, Wittwer A, Zweifel B, Masferrer J.

J Pharmacol Exp Ther. 2010 Jul;334(1):310-7. doi: 10.1124/jpet.110.165845. Epub 2010 Apr 14.

PMID:
20392816
22.

Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode.

Meyers MJ, Pelc M, Kamtekar S, Day J, Poda GI, Hall MK, Michener ML, Reitz BA, Mathis KJ, Pierce BS, Parikh MD, Mischke DA, Long SA, Parlow JJ, Anderson DR, Thorarensen A.

Bioorg Med Chem Lett. 2010 Mar 1;20(5):1543-7. doi: 10.1016/j.bmcl.2010.01.078. Epub 2010 Jan 21.

PMID:
20137931
23.

Structure based design of novel irreversible FAAH inhibitors.

Wang JL, Bowen SJ, Schweitzer BA, Madsen HM, McDonald J, Pelc MJ, Tenbrink RE, Beidler D, Thorarensen A.

Bioorg Med Chem Lett. 2009 Oct 15;19(20):5970-4. doi: 10.1016/j.bmcl.2009.07.101. Epub 2009 Jul 25.

PMID:
19765986
24.

Synthesis of tert-butyl 6-oxo-2-azaspiro[3.3]heptane-2-carboxylate.

Meyers MJ, Muizebelt I, van Wiltenburg J, Brown DL, Thorarensen A.

Org Lett. 2009 Aug 20;11(16):3523-5. doi: 10.1021/ol901325s.

PMID:
19637855
25.

2-(6-Phenyl-1H-indazol-3-yl)-1H-benzo[d]imidazoles: design and synthesis of a potent and isoform selective PKC-zeta inhibitor.

Trujillo JI, Kiefer JR, Huang W, Thorarensen A, Xing L, Caspers NL, Day JE, Mathis KJ, Kretzmer KK, Reitz BA, Weinberg RA, Stegeman RA, Wrightstone A, Christine L, Compton R, Li X.

Bioorg Med Chem Lett. 2009 Feb 1;19(3):908-11. doi: 10.1016/j.bmcl.2008.11.105. Epub 2008 Dec 6.

PMID:
19097791
26.

Bacterial translation inhibitors, 1-acylindazol-3-ols as anthranilic acid mimics.

Stiff C, Graber DR, Thorarensen A, Wakefield BD, Marotti KR, Melchior EP, Sweeney MT, Han F, Rohrer DC, Zurenko GE, Romero DL.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6293-7. doi: 10.1016/j.bmcl.2007.08.041. Epub 2007 Aug 25.

PMID:
18951783
27.

Human serum albumin binding assay based on displacement of a non selective fluorescent inhibitor.

Thorarensen A, Sarver RW, Tian F, Ho A, Romero DL, Marotti KR.

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4646-9. Epub 2007 May 27.

PMID:
17560104
28.

Preparation of novel anthranilic acids as antibacterial agents: extensive evaluation of structural and physical properties on antibacterial activity and human serum albumin affinity.

Thorarensen A, Li J, Wakefield BD, Romero DL, Marotti KR, Sweeney MT, Zurenko GE, Sarver RW.

Bioorg Med Chem Lett. 2007 Jun 1;17(11):3113-6. Epub 2007 Mar 15.

PMID:
17400450
29.

Preparation of novel anthranilic acids as antibacterial agents. Extensive evaluation of alternative amide bioisosteres connecting the A- and the B-rings.

Thorarensen A, Wakefield BD, Romero DL, Marotti KR, Sweeney MT, Zurenko GE, Rohrer DC, Han F, Bryant GL Jr.

Bioorg Med Chem Lett. 2007 May 15;17(10):2823-7. Epub 2007 Feb 25.

PMID:
17368020
30.

Preparation of novel antibacterial agents. Replacement of the central aromatic ring with heterocycles.

Li J, Wakefield BD, Ruble JC, Stiff CM, Romero DL, Marotti KR, Sweeney MT, Zurenko GE, Rohrer DC, Thorarensen A.

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2347-50. Epub 2006 Dec 21.

PMID:
17350254
31.

Advances in the discovery of novel antibacterial agents during the year 2002.

Harris CR, Thorarensen A.

Curr Med Chem. 2004 Aug;11(16):2213-43. Review.

PMID:
15279560
32.

Immobilization of a novel antibacterial agent on solid phase and subsequent isolation of EF-Tu.

Deibel MR Jr, Bodnar AL, Yem AW, Wolfe CL, Heckaman CL, Bohanon MJ, Mathews WR, Sweeney MT, Zurenko GE, Marotti KR, Boyle TP, Thorarensen A.

Bioconjug Chem. 2004 Mar-Apr;15(2):333-43.

PMID:
15025529
33.

Enols as potent antibacterial agents.

Thorarensen A, Zurenko GE, Sweeney MT, Marotti KR, Boyle TP.

Bioorg Med Chem Lett. 2001 Nov 19;11(22):2931-4.

PMID:
11677129
34.

A Versatile Route to 2-Substituted Cyclic 1,3-dienes via a Copper(I)-Catalyzed Cross-Coupling Reaction of Dienyl Triflates with Grignard Reagents.

Karlström AS, Rönn M, Thorarensen A, Bäckvall JE.

J Org Chem. 1998 Apr 17;63(8):2784. No abstract available.

PMID:
11672159
35.

A Versatile Route to 2-Substituted Cyclic 1,3-Dienes via a Copper(I)-Catalyzed Cross-Coupling Reaction of Dienyl Triflates with Grignard Reagents.

Karlström AS, Rönn M, Thorarensen A, Bäckvall JE.

J Org Chem. 1998 Apr 17;63(8):2517-2522.

PMID:
11672113
36.

3-Arylpiperidines as potentiators of existing antibacterial agents.

Thorarensen A, Presley-Bodnar AL, Marotti KR, Boyle TP, Heckaman CL, Bohanon MJ, Tomich PK, Zurenko GE, Sweeney MT, Yagi BH.

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1903-6.

PMID:
11459657
37.

Identification of novel potent hydroxamic acid inhibitors of peptidyl deformylase and the importance of the hydroxamic acid functionality on inhibition.

Thorarensen A, Deibel MR Jr, Rohrer DC, Vosters AF, Yem AW, Marshall VD, Lynn JC, Bohanon MJ, Tomich PK, Zurenko GE, Sweeney MT, Jensen RM, Nielsen JW, Seest EP, Dolak LA.

Bioorg Med Chem Lett. 2001 Jun 4;11(11):1355-8. Erratum in: Bioorg Med Chem Lett 2001 Aug 6;11(15):2053.

PMID:
11378353
39.

Tandem [4 + 2]/[3 + 2] Cycloadditions of Nitroalkenes. 10. trans-2-(1-Methyl-1-phenylethyl)cyclohexanol as a New Auxiliary.

Denmark SE, Thorarensen A.

J Org Chem. 1996 Sep 20;61(19):6727-6729. No abstract available.

PMID:
11667549
40.

Tandem [4+2]/[3+2] Cycloadditions of Nitroalkenes.

Denmark SE, Thorarensen A.

Chem Rev. 1996 Feb 1;96(1):137-166. No abstract available.

PMID:
11848747

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