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Items: 30

1.

Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signaling.

Zak M, Hanan EJ, Lupardus P, Brown DG, Robinson C, Siu M, Lyssikatos JP, Romero FA, Zhao G, Kellar T, Mendonca R, Ray NC, Goodacre SC, Crackett PH, McLean N, Hurley CA, Yuen PW, Cheng YX, Liu X, Liimatta M, Kohli PB, Nonomiya J, Salmon G, Buckley G, Lloyd J, Gibbons P, Ghilardi N, Kenny JR, Johnson A.

Bioorg Med Chem Lett. 2019 Jun 15;29(12):1522-1531. doi: 10.1016/j.bmcl.2019.04.008. Epub 2019 Apr 4.

PMID:
30981576
2.

Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.

Wang X, Blackaby W, Allen V, Chan GKY, Chang JH, Chiang PC, Diène C, Drummond J, Do S, Fan E, Harstad EB, Hodges A, Hu H, Jia W, Kofie W, Kolesnikov A, Lyssikatos JP, Ly J, Matteucci M, Moffat JG, Munugalavadla V, Murray J, Nash D, Noland CL, Del Rosario G, Ross L, Rouse C, Sharpe A, Slaga D, Sun M, Tsui V, Wallweber H, Yu SF, Ebens AJ.

J Med Chem. 2019 Feb 28;62(4):2140-2153. doi: 10.1021/acs.jmedchem.8b01857. Epub 2019 Feb 20.

PMID:
30715878
3.

Discovery of a Potent (4 R,5 S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling.

Chen H, Volgraf M, Do S, Kolesnikov A, Shore DG, Verma VA, Villemure E, Wang L, Chen Y, Hu B, Lu AJ, Wu G, Xu X, Yuen PW, Zhang Y, Erickson SD, Dahl M, Brotherton-Pleiss C, Tay S, Ly JQ, Murray LJ, Chen J, Amm D, Lange W, Hackos DH, Reese RM, Shields SD, Lyssikatos JP, Safina BS, Estrada AA.

J Med Chem. 2018 Apr 26;61(8):3641-3659. doi: 10.1021/acs.jmedchem.8b00117. Epub 2018 Apr 12.

PMID:
29590749
4.

Selective Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12) with Activity in a Model of Alzheimer's Disease.

Patel S, Meilandt WJ, Erickson RI, Chen J, Deshmukh G, Estrada AA, Fuji RN, Gibbons P, Gustafson A, Harris SF, Imperio J, Liu W, Liu X, Liu Y, Lyssikatos JP, Ma C, Yin J, Lewcock JW, Siu M.

J Med Chem. 2017 Oct 12;60(19):8083-8102. doi: 10.1021/acs.jmedchem.7b00843. Epub 2017 Sep 20.

PMID:
28929759
5.

Germinal-center kinase-like kinase co-crystal structure reveals a swapped activation loop and C-terminal extension.

Marcotte D, Rushe M, M Arduini R, Lukacs C, Atkins K, Sun X, Little K, Cullivan M, Paramasivam M, Patterson TA, Hesson T, D McKee T, May-Dracka TL, Xin Z, Bertolotti-Ciarlet A, Bhisetti GR, Lyssikatos JP, Silvian LF.

Protein Sci. 2017 Feb;26(2):152-162. doi: 10.1002/pro.3062. Epub 2016 Oct 21.

6.

Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.

Ndubaku CO, Crawford JJ, Drobnick J, Aliagas I, Campbell D, Dong P, Dornan LM, Duron S, Epler J, Gazzard L, Heise CE, Hoeflich KP, Jakubiak D, La H, Lee W, Lin B, Lyssikatos JP, Maksimoska J, Marmorstein R, Murray LJ, O'Brien T, Oh A, Ramaswamy S, Wang W, Zhao X, Zhong Y, Blackwood E, Rudolph J.

ACS Med Chem Lett. 2015 Oct 31;6(12):1241-6. doi: 10.1021/acsmedchemlett.5b00398. eCollection 2015 Dec 10.

7.

α-Aryl pyrrolidine sulfonamides as TRPA1 antagonists.

Verma VA, Shore DGM, Chen H, Chen J, Do S, Hackos DH, Kolesnikov A, Lyssikatos JP, Tay S, Wang L, Estrada AA.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):495-498. doi: 10.1016/j.bmcl.2015.11.088. Epub 2015 Nov 25.

PMID:
26706172
8.

Novel antibody-antibiotic conjugate eliminates intracellular S. aureus.

Lehar SM, Pillow T, Xu M, Staben L, Kajihara KK, Vandlen R, DePalatis L, Raab H, Hazenbos WL, Morisaki JH, Kim J, Park S, Darwish M, Lee BC, Hernandez H, Loyet KM, Lupardus P, Fong R, Yan D, Chalouni C, Luis E, Khalfin Y, Plise E, Cheong J, Lyssikatos JP, Strandh M, Koefoed K, Andersen PS, Flygare JA, Wah Tan M, Brown EJ, Mariathasan S.

Nature. 2015 Nov 19;527(7578):323-8. doi: 10.1038/nature16057. Epub 2015 Nov 4.

PMID:
26536114
9.

Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors.

Hu H, Wang X, Chan GK, Chang JH, Do S, Drummond J, Ebens A, Lee W, Ly J, Lyssikatos JP, Murray J, Moffat JG, Chao Q, Tsui V, Wallweber H, Kolesnikov A.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5258-64. doi: 10.1016/j.bmcl.2015.09.052. Epub 2015 Sep 30.

PMID:
26459208
10.

Probing Mechanisms of CYP3A Time-Dependent Inhibition Using a Truncated Model System.

Wang X, Sun M, New C, Nam S, Blackaby WP, Hodges AJ, Nash D, Matteucci M, Lyssikatos JP, Fan PW, Tay S, Chang JH.

ACS Med Chem Lett. 2015 Jul 12;6(8):925-9. doi: 10.1021/acsmedchemlett.5b00191. eCollection 2015 Aug 13.

11.

Effect of selective LRRK2 kinase inhibition on nonhuman primate lung.

Fuji RN, Flagella M, Baca M, Baptista MA, Brodbeck J, Chan BK, Fiske BK, Honigberg L, Jubb AM, Katavolos P, Lee DW, Lewin-Koh SC, Lin T, Liu X, Liu S, Lyssikatos JP, O'Mahony J, Reichelt M, Roose-Girma M, Sheng Z, Sherer T, Smith A, Solon M, Sweeney ZK, Tarrant J, Urkowitz A, Warming S, Yaylaoglu M, Zhang S, Zhu H, Estrada AA, Watts RJ.

Sci Transl Med. 2015 Feb 4;7(273):273ra15. doi: 10.1126/scitranslmed.aaa3634.

PMID:
25653221
12.

8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.

Thomas AA, Hunt KW, Newhouse B, Watts RJ, Liu X, Vigers G, Smith D, Rhodes SP, Brown KD, Otten JN, Burkard M, Cox AA, Geck Do MK, Dutcher D, Rana S, DeLisle RK, Regal K, Wright AD, Groneberg R, Liao J, Scearce-Levie K, Siu M, Purkey HE, Lyssikatos JP.

J Med Chem. 2014 Dec 11;57(23):10112-29. doi: 10.1021/jm5015132. Epub 2014 Nov 26.

PMID:
25411915
13.

Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.

Patel S, Cohen F, Dean BJ, De La Torre K, Deshmukh G, Estrada AA, Ghosh AS, Gibbons P, Gustafson A, Huestis MP, Le Pichon CE, Lin H, Liu W, Liu X, Liu Y, Ly CQ, Lyssikatos JP, Ma C, Scearce-Levie K, Shin YG, Solanoy H, Stark KL, Wang J, Wang B, Zhao X, Lewcock JW, Siu M.

J Med Chem. 2015 Jan 8;58(1):401-18. doi: 10.1021/jm5013984. Epub 2014 Oct 23.

PMID:
25341110
14.

Discovery of a Novel Class of Imidazo[1,2-a]Pyridines with Potent PDGFR Activity and Oral Bioavailability.

Hicken EJ, Marmsater FP, Munson MC, Schlachter ST, Robinson JE, Allen S, Burgess LE, DeLisle RK, Rizzi JP, Topalov GT, Zhao Q, Hicks JM, Kallan NC, Tarlton E, Allen A, Callejo M, Cox A, Rana S, Klopfenstein N, Woessner R, Lyssikatos JP.

ACS Med Chem Lett. 2013 Nov 12;5(1):78-83. doi: 10.1021/ml4003953. eCollection 2014 Jan 9.

15.

Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors.

Volgraf M, Chan L, Huestis MP, Purkey HE, Burkard M, Geck Do M, Harris J, Hunt KW, Liu X, Lyssikatos JP, Rana S, Thomas AA, Vigers GP, Siu M.

Bioorg Med Chem Lett. 2014 Jun 1;24(11):2477-80. doi: 10.1016/j.bmcl.2014.04.012. Epub 2014 Apr 13.

PMID:
24780121
16.

Dose-dependent exposure and metabolism of GNE-892, a β-secretase inhibitor, in monkeys: contributions by P450, AO, and P-gp.

Takahashi R, Ma S, Yue Q, Kim-Kang H, Yi Y, Lyssikatos JP, Regal K, Hunt KW, Kallan NC, Siu M, Hop CE, Liu X, Khojasteh SC.

Eur J Drug Metab Pharmacokinet. 2015 Jun;40(2):171-85. doi: 10.1007/s13318-014-0198-5. Epub 2014 Apr 3.

PMID:
24696325
17.

Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system.

Thomas AA, Hunt KW, Volgraf M, Watts RJ, Liu X, Vigers G, Smith D, Sammond D, Tang TP, Rhodes SP, Metcalf AT, Brown KD, Otten JN, Burkard M, Cox AA, Do MK, Dutcher D, Rana S, DeLisle RK, Regal K, Wright AD, Groneberg R, Scearce-Levie K, Siu M, Purkey HE, Lyssikatos JP, Gunawardana IW.

J Med Chem. 2014 Feb 13;57(3):878-902. doi: 10.1021/jm401635n. Epub 2014 Jan 22.

PMID:
24397738
18.

Discovery of highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

Estrada AA, Chan BK, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chen H, Dominguez SL, Dotson J, Drummond J, Flagella M, Fuji R, Gill A, Halladay J, Harris SF, Heffron TP, Kleinheinz T, Lee DW, Le Pichon CE, Liu X, Lyssikatos JP, Medhurst AD, Moffat JG, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Wong S, Zhang S, Zhang X, Zhu H, Sweeney ZK.

J Med Chem. 2014 Feb 13;57(3):921-36. doi: 10.1021/jm401654j. Epub 2014 Jan 15.

PMID:
24354345
19.

A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.

Lee W, Ortwine DF, Bergeron P, Lau K, Lin L, Malek S, Nonomiya J, Pei Z, Robarge KD, Schmidt S, Sideris S, Lyssikatos JP.

Bioorg Med Chem Lett. 2013 Sep 15;23(18):5097-104. doi: 10.1016/j.bmcl.2013.07.027. Epub 2013 Jul 23.

PMID:
23932790
20.

2-Amino-[1,2,4]triazolo[1,5-a]pyridines as JAK2 inhibitors.

Siu M, Pastor R, Liu W, Barrett K, Berry M, Blair WS, Chang C, Chen JZ, Eigenbrot C, Ghilardi N, Gibbons P, He H, Hurley CA, Kenny JR, Cyrus Khojasteh S, Le H, Lee L, Lyssikatos JP, Magnuson S, Pulk R, Tsui V, Ultsch M, Xiao Y, Zhu BY, Sampath D.

Bioorg Med Chem Lett. 2013 Sep 1;23(17):5014-21. doi: 10.1016/j.bmcl.2013.06.008. Epub 2013 Jun 15.

PMID:
23870430
21.

Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species.

Hunt KW, Cook AW, Watts RJ, Clark CT, Vigers G, Smith D, Metcalf AT, Gunawardana IW, Burkard M, Cox AA, Geck Do MK, Dutcher D, Thomas AA, Rana S, Kallan NC, DeLisle RK, Rizzi JP, Regal K, Sammond D, Groneberg R, Siu M, Purkey H, Lyssikatos JP, Marlow A, Liu X, Tang TP.

J Med Chem. 2013 Apr 25;56(8):3379-403. doi: 10.1021/jm4002154. Epub 2013 Apr 16.

PMID:
23537249
22.

Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).

Estrada AA, Shore DG, Blackwood E, Chen YH, Deshmukh G, Ding X, Dipasquale AG, Epler JA, Friedman LS, Koehler MF, Liu L, Malek S, Nonomiya J, Ortwine DF, Pei Z, Sideris S, St-Jean F, Trinh L, Truong T, Lyssikatos JP.

J Med Chem. 2013 Apr 11;56(7):3090-101. doi: 10.1021/jm400194n. Epub 2013 Mar 29.

PMID:
23473235
23.

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

Pei Z, Blackwood E, Liu L, Malek S, Belvin M, Koehler MF, Ortwine DF, Chen H, Cohen F, Kenny JR, Bergeron P, Lau K, Ly C, Zhao X, Estrada AA, Truong T, Epler JA, Nonomiya J, Trinh L, Sideris S, Lesnick J, Bao L, Vijapurkar U, Mukadam S, Tay S, Deshmukh G, Chen YH, Ding X, Friedman LS, Lyssikatos JP.

ACS Med Chem Lett. 2012 Nov 29;4(1):103-7. doi: 10.1021/ml3003132. eCollection 2013 Jan 10.

24.

Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.

Koehler MF, Bergeron P, Blackwood E, Bowman KK, Chen YH, Deshmukh G, Ding X, Epler J, Lau K, Lee L, Liu L, Ly C, Malek S, Nonomiya J, Oeh J, Ortwine DF, Sampath D, Sideris S, Trinh L, Truong T, Wu J, Pei Z, Lyssikatos JP.

J Med Chem. 2012 Dec 27;55(24):10958-71. doi: 10.1021/jm301389h. Epub 2012 Dec 12.

PMID:
23199076
25.

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.

Hanan EJ, van Abbema A, Barrett K, Blair WS, Blaney J, Chang C, Eigenbrot C, Flynn S, Gibbons P, Hurley CA, Kenny JR, Kulagowski J, Lee L, Magnuson SR, Morris C, Murray J, Pastor RM, Rawson T, Siu M, Ultsch M, Zhou A, Sampath D, Lyssikatos JP.

J Med Chem. 2012 Nov 26;55(22):10090-107. doi: 10.1021/jm3012239. Epub 2012 Oct 24.

PMID:
23061660
26.

Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors.

Estrada AA, Liu X, Baker-Glenn C, Beresford A, Burdick DJ, Chambers M, Chan BK, Chen H, Ding X, DiPasquale AG, Dominguez SL, Dotson J, Drummond J, Flagella M, Flynn S, Fuji R, Gill A, Gunzner-Toste J, Harris SF, Heffron TP, Kleinheinz T, Lee DW, Le Pichon CE, Lyssikatos JP, Medhurst AD, Moffat JG, Mukund S, Nash K, Scearce-Levie K, Sheng Z, Shore DG, Tran T, Trivedi N, Wang S, Zhang S, Zhang X, Zhao G, Zhu H, Sweeney ZK.

J Med Chem. 2012 Nov 26;55(22):9416-33. doi: 10.1021/jm301020q. Epub 2012 Oct 15.

PMID:
22985112
27.

Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.

Cohen F, Bergeron P, Blackwood E, Bowman KK, Chen H, Dipasquale AG, Epler JA, Koehler MF, Lau K, Lewis C, Liu L, Ly CQ, Malek S, Nonomiya J, Ortwine DF, Pei Z, Robarge KD, Sideris S, Trinh L, Truong T, Wu J, Zhao X, Lyssikatos JP.

J Med Chem. 2011 May 12;54(9):3426-35. doi: 10.1021/jm200215y. Epub 2011 Apr 15.

PMID:
21495671
28.

Non-charged thiamine analogs as inhibitors of enzyme transketolase.

Thomas AA, De Meese J, Le Huerou Y, Boyd SA, Romoff TT, Gonzales SS, Gunawardana I, Kaplan T, Sullivan F, Condroski K, Lyssikatos JP, Aicher TD, Ballard J, Bernat B, DeWolf W, Han M, Lemieux C, Smith D, Weiler S, Wright SK, Vigers G, Brandhuber B.

Bioorg Med Chem Lett. 2008 Jan 15;18(2):509-12. doi: 10.1016/j.bmcl.2007.11.098. Epub 2007 Dec 3.

PMID:
18182286
29.

Progress towards therapeutic small molecule MEK inhibitors for use in cancer therapy.

Wallace EM, Lyssikatos JP, Yeh T, Winkler JD, Koch K.

Curr Top Med Chem. 2005;5(2):215-29. Review.

PMID:
15853648
30.

Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451.

Roberts WG, Whalen PM, Soderstrom E, Moraski G, Lyssikatos JP, Wang HF, Cooper B, Baker DA, Savage D, Dalvie D, Atherton JA, Ralston S, Szewc R, Kath JC, Lin J, Soderstrom C, Tkalcevic G, Cohen BD, Pollack V, Barth W, Hungerford W, Ung E.

Cancer Res. 2005 Feb 1;65(3):957-66.

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