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Items: 1 to 50 of 121

1.

Potent and selective inhibitors of receptor-interacting protein kinase 1 that lack an aromatic back pocket group.

Hamilton GL, Chen H, Deshmukh G, Eigenbrot C, Fong R, Johnson A, Kohli PB, Lupardus PJ, Liederer BM, Ramaswamy S, Wang H, Wang J, Xu Z, Zhu Y, Vucic D, Patel S.

Bioorg Med Chem Lett. 2019 Jun 15;29(12):1497-1501. doi: 10.1016/j.bmcl.2019.04.014. Epub 2019 Apr 11.

PMID:
31000154
2.

Water molecules in protein-ligand interfaces. Evaluation of software tools and SAR comparison.

Nittinger E, Gibbons P, Eigenbrot C, Davies DR, Maurer B, Yu CL, Kiefer JR, Kuglstatter A, Murray J, Ortwine DF, Tang Y, Tsui V.

J Comput Aided Mol Des. 2019 Mar;33(3):307-330. doi: 10.1007/s10822-019-00187-y. Epub 2019 Feb 12.

PMID:
30756207
3.

Identification of a Helical Segment within the Intrinsically Disordered Region of the PCSK9 Prodomain.

Ultsch M, Li W, Eigenbrot C, Di Lello P, Lipari MT, Gerhardy S, AhYoung AP, Quinn J, Franke Y, Chen Y, Kong Beltran M, Peterson A, Kirchhofer D.

J Mol Biol. 2019 Mar 1;431(5):885-903. doi: 10.1016/j.jmb.2018.11.025. Epub 2019 Jan 15.

PMID:
30653992
4.

Dual functionality of β-tryptase protomers as both proteases and cofactors in the active tetramer.

Maun HR, Liu PS, Franke Y, Eigenbrot C, Forrest WF, Schwartz LB, Lazarus RA.

J Biol Chem. 2018 Jun 22;293(25):9614-9628. doi: 10.1074/jbc.M117.812016. Epub 2018 Apr 16.

5.

Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development.

Crawford JJ, Johnson AR, Misner DL, Belmont LD, Castanedo G, Choy R, Coraggio M, Dong L, Eigenbrot C, Erickson R, Ghilardi N, Hau J, Katewa A, Kohli PB, Lee W, Lubach JW, McKenzie BS, Ortwine DF, Schutt L, Tay S, Wei B, Reif K, Liu L, Wong H, Young WB.

J Med Chem. 2018 Mar 22;61(6):2227-2245. doi: 10.1021/acs.jmedchem.7b01712. Epub 2018 Feb 23.

PMID:
29457982
6.

Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity.

Wei B, Gunzner-Toste J, Yao H, Wang T, Wang J, Xu Z, Chen J, Wai J, Nonomiya J, Tsai SP, Chuh J, Kozak KR, Liu Y, Yu SF, Lau J, Li G, Phillips GD, Leipold D, Kamath A, Su D, Xu K, Eigenbrot C, Steinbacher S, Ohri R, Raab H, Staben LR, Zhao G, Flygare JA, Pillow TH, Verma V, Masterson LA, Howard PW, Safina B.

J Med Chem. 2018 Feb 8;61(3):989-1000. doi: 10.1021/acs.jmedchem.7b01430. Epub 2017 Dec 21.

PMID:
29227683
7.

Identification of an imidazopyridine scaffold to generate potent and selective TYK2 inhibitors that demonstrate activity in an in vivo psoriasis model.

Liang J, Van Abbema A, Balazs M, Barrett K, Berezhkovsky L, Blair WS, Chang C, Delarosa D, DeVoss J, Driscoll J, Eigenbrot C, Goodacre S, Ghilardi N, MacLeod C, Johnson A, Bir Kohli P, Lai Y, Lin Z, Mantik P, Menghrajani K, Nguyen H, Peng I, Sambrone A, Shia S, Smith J, Sohn S, Tsui V, Ultsch M, Williams K, Wu LC, Yang W, Zhang B, Magnuson S.

Bioorg Med Chem Lett. 2017 Sep 15;27(18):4370-4376. doi: 10.1016/j.bmcl.2017.08.022. Epub 2017 Aug 12.

PMID:
28830649
8.

Discovery of a cryptic peptide-binding site on PCSK9 and design of antagonists.

Zhang Y, Ultsch M, Skelton NJ, Burdick DJ, Beresini MH, Li W, Kong-Beltran M, Peterson A, Quinn J, Chiu C, Wu Y, Shia S, Moran P, Di Lello P, Eigenbrot C, Kirchhofer D.

Nat Struct Mol Biol. 2017 Oct;24(10):848-856. doi: 10.1038/nsmb.3453. Epub 2017 Aug 21.

PMID:
28825733
9.

Discovery of Potent and Selective Tricyclic Inhibitors of Bruton's Tyrosine Kinase with Improved Druglike Properties.

Wang X, Barbosa J, Blomgren P, Bremer MC, Chen J, Crawford JJ, Deng W, Dong L, Eigenbrot C, Gallion S, Hau J, Hu H, Johnson AR, Katewa A, Kropf JE, Lee SH, Liu L, Lubach JW, Macaluso J, Maciejewski P, Mitchell SA, Ortwine DF, DiPaolo J, Reif K, Scheerens H, Schmitt A, Wong H, Xiong JM, Xu J, Zhao Z, Zhou F, Currie KS, Young WB.

ACS Med Chem Lett. 2017 May 3;8(6):608-613. doi: 10.1021/acsmedchemlett.7b00103. eCollection 2017 Jun 8.

10.

3-2-1: Structural insights from stepwise shrinkage of a three-helix Fc-binding domain to a single helix.

Ultsch M, Braisted A, Maun HR, Eigenbrot C.

Protein Eng Des Sel. 2017 Sep 1;30(9):619-625. doi: 10.1093/protein/gzx029.

11.

Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K).

Castanedo GM, Blaquiere N, Beresini M, Bravo B, Brightbill H, Chen J, Cui HF, Eigenbrot C, Everett C, Feng J, Godemann R, Gogol E, Hymowitz S, Johnson A, Kayagaki N, Kohli PB, Knüppel K, Kraemer J, Krüger S, Loke P, McEwan P, Montalbetti C, Roberts DA, Smith M, Steinbacher S, Sujatha-Bhaskar S, Takahashi R, Wang X, Wu LC, Zhang Y, Staben ST.

J Med Chem. 2017 Jan 26;60(2):627-640. doi: 10.1021/acs.jmedchem.6b01363. Epub 2017 Jan 12.

PMID:
28005357
12.

Structure of Crenezumab Complex with Aβ Shows Loss of β-Hairpin.

Ultsch M, Li B, Maurer T, Mathieu M, Adolfsson O, Muhs A, Pfeifer A, Pihlgren M, Bainbridge TW, Reichelt M, Ernst JA, Eigenbrot C, Fuh G, Atwal JK, Watts RJ, Wang W.

Sci Rep. 2016 Dec 20;6:39374. doi: 10.1038/srep39374.

13.

Resolving TYK2 locus genotype-to-phenotype differences in autoimmunity.

Dendrou CA, Cortes A, Shipman L, Evans HG, Attfield KE, Jostins L, Barber T, Kaur G, Kuttikkatte SB, Leach OA, Desel C, Faergeman SL, Cheeseman J, Neville MJ, Sawcer S, Compston A, Johnson AR, Everett C, Bell JI, Karpe F, Ultsch M, Eigenbrot C, McVean G, Fugger L.

Sci Transl Med. 2016 Nov 2;8(363):363ra149.

14.

Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.

Purkey HE, Robarge K, Chen J, Chen Z, Corson LB, Ding CZ, DiPasquale AG, Dragovich PS, Eigenbrot C, Evangelista M, Fauber BP, Gao Z, Ge H, Hitz A, Ho Q, Labadie SS, Lai KW, Liu W, Liu Y, Li C, Ma S, Malek S, O'Brien T, Pang J, Peterson D, Salphati L, Sideris S, Ultsch M, Wei B, Yen I, Yue Q, Zhang H, Zhou A.

ACS Med Chem Lett. 2016 Aug 26;7(10):896-901. eCollection 2016 Oct 13.

15.

Battling Btk Mutants With Noncovalent Inhibitors That Overcome Cys481 and Thr474 Mutations.

Johnson AR, Kohli PB, Katewa A, Gogol E, Belmont LD, Choy R, Penuel E, Burton L, Eigenbrot C, Yu C, Ortwine DF, Bowman K, Franke Y, Tam C, Estevez A, Mortara K, Wu J, Li H, Lin M, Bergeron P, Crawford JJ, Young WB.

ACS Chem Biol. 2016 Oct 21;11(10):2897-2907. Epub 2016 Sep 7.

PMID:
27571029
16.

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor.

Chan BK, Hanan EJ, Bowman KK, Bryan MC, Burdick D, Chan E, Chen Y, Clausen S, Dela Vega T, Dotson J, Eigenbrot C, Elliott RL, Heald RA, Jackson PS, Knight JD, La H, Lainchbury MD, Malek S, Purkey HE, Schaefer G, Schmidt S, Seward EM, Sideris S, Shao L, Wang S, Yeap SK, Yen I, Yu C, Heffron TP.

J Med Chem. 2016 Oct 13;59(19):9080-9093. Epub 2016 Sep 12.

PMID:
27564586
17.

Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition.

Boudreau A, Purkey HE, Hitz A, Robarge K, Peterson D, Labadie S, Kwong M, Hong R, Gao M, Del Nagro C, Pusapati R, Ma S, Salphati L, Pang J, Zhou A, Lai T, Li Y, Chen Z, Wei B, Yen I, Sideris S, McCleland M, Firestein R, Corson L, Vanderbilt A, Williams S, Daemen A, Belvin M, Eigenbrot C, Jackson PK, Malek S, Hatzivassiliou G, Sampath D, Evangelista M, O'Brien T.

Nat Chem Biol. 2016 Oct;12(10):779-86. doi: 10.1038/nchembio.2143. Epub 2016 Aug 1.

PMID:
27479743
18.

Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2.

Foster SA, Whalen DM, Özen A, Wongchenko MJ, Yin J, Yen I, Schaefer G, Mayfield JD, Chmielecki J, Stephens PJ, Albacker LA, Yan Y, Song K, Hatzivassiliou G, Eigenbrot C, Yu C, Shaw AS, Manning G, Skelton NJ, Hymowitz SG, Malek S.

Cancer Cell. 2016 Apr 11;29(4):477-493. doi: 10.1016/j.ccell.2016.02.010. Epub 2016 Mar 17.

19.

Correction to Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.

Heald R, Bowman KK, Bryan MC, Burdick D, Chan B, Chan E, Chen Y, Clausen S, Dominguez-Fernandez B, Eigenbrot C, Elliott R, Hanan EJ, Jackson P, Knight J, La H, Lainchbury M, Malek S, Mann S, Merchant M, Mortara K, Purkey H, Schaefer G, Schmidt S, Seward E, Sideris S, Shao L, Wang S, Yeap K, Yen I, Yu C, Heffron TP.

J Med Chem. 2016 Mar 24;59(6):2848. doi: 10.1021/acs.jmedchem.6b00301. Epub 2016 Mar 11. No abstract available.

PMID:
26967667
20.

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

Bryan MC, Burdick DJ, Chan BK, Chen Y, Clausen S, Dotson J, Eigenbrot C, Elliott R, Hanan EJ, Heald R, Jackson P, La H, Lainchbury M, Malek S, Mann SE, Purkey HE, Schaefer G, Schmidt S, Seward E, Sideris S, Wang S, Yen I, Yu C, Heffron TP.

ACS Med Chem Lett. 2015 Dec 17;7(1):100-4. doi: 10.1021/acsmedchemlett.5b00428. eCollection 2016 Jan 14.

21.

The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).

Heffron TP, Heald RA, Ndubaku C, Wei B, Augistin M, Do S, Edgar K, Eigenbrot C, Friedman L, Gancia E, Jackson PS, Jones G, Kolesnikov A, Lee LB, Lesnick JD, Lewis C, McLean N, Mörtl M, Nonomiya J, Pang J, Price S, Prior WW, Salphati L, Sideris S, Staben ST, Steinbacher S, Tsui V, Wallin J, Sampath D, Olivero AG.

J Med Chem. 2016 Feb 11;59(3):985-1002. doi: 10.1021/acs.jmedchem.5b01483. Epub 2016 Jan 20.

PMID:
26741947
22.

Discovery of highly potent and selective Bruton's tyrosine kinase inhibitors: Pyridazinone analogs with improved metabolic stability.

Young WB, Barbosa J, Blomgren P, Bremer MC, Crawford JJ, Dambach D, Eigenbrot C, Gallion S, Johnson AR, Kropf JE, Lee SH, Liu L, Lubach JW, Macaluso J, Maciejewski P, Mitchell SA, Ortwine DF, Di Paolo J, Reif K, Scheerens H, Schmitt A, Wang X, Wong H, Xiong JM, Xu J, Yu C, Zhao Z, Currie KS.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):575-579. doi: 10.1016/j.bmcl.2015.11.076. Epub 2015 Nov 24.

PMID:
26675441
23.

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.

Hanan EJ, Baumgardner M, Bryan MC, Chen Y, Eigenbrot C, Fan P, Gu XH, La H, Malek S, Purkey HE, Schaefer G, Schmidt S, Sideris S, Yen I, Yu C, Heffron TP.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):534-539. doi: 10.1016/j.bmcl.2015.11.078. Epub 2015 Nov 22.

PMID:
26639762
24.

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.

Heald R, Bowman KK, Bryan MC, Burdick D, Chan B, Chan E, Chen Y, Clausen S, Dominguez-Fernandez B, Eigenbrot C, Elliott R, Hanan EJ, Jackson P, Knight J, La H, Lainchbury M, Malek S, Mann S, Merchant M, Mortara K, Purkey H, Schaefer G, Schmidt S, Seward E, Sideris S, Shao L, Wang S, Yeap K, Yen I, Yu C, Heffron TP.

J Med Chem. 2015 Nov 25;58(22):8877-95. doi: 10.1021/acs.jmedchem.5b01412. Epub 2015 Nov 12. Erratum in: J Med Chem. 2016 Mar 24;59(6):2848.

PMID:
26455919
25.

The trimeric serine protease HtrA1 forms a cage-like inhibition complex with an anti-HtrA1 antibody.

Ciferri C, Lipari MT, Liang WC, Estevez A, Hang J, Stawicki S, Wu Y, Moran P, Elliott M, Eigenbrot C, Katschke KJ, van Lookeren Campagne M, Kirchhofer D.

Biochem J. 2015 Dec 1;472(2):169-81. doi: 10.1042/BJ20150601. Epub 2015 Sep 18.

PMID:
26385991
26.

Structural basis of the broadly neutralizing anti-interferon-α antibody rontalizumab.

Maurer B, Bosanac I, Shia S, Kwong M, Corpuz R, Vandlen R, Schmidt K, Eigenbrot C.

Protein Sci. 2015 Sep;24(9):1440-50. doi: 10.1002/pro.2729. Epub 2015 Aug 18.

27.

Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo.

Burch JD, Barrett K, Chen Y, DeVoss J, Eigenbrot C, Goldsmith R, Ismaili MH, Lau K, Lin Z, Ortwine DF, Zarrin AA, McEwan PA, Barker JJ, Ellebrandt C, Kordt D, Stein DB, Wang X, Chen Y, Hu B, Xu X, Yuen PW, Zhang Y, Pei Z.

J Med Chem. 2015 May 14;58(9):3806-16. doi: 10.1021/jm501998m. Epub 2015 Apr 16.

PMID:
25844760
28.

Framework selection can influence pharmacokinetics of a humanized therapeutic antibody through differences in molecule charge.

Li B, Tesar D, Boswell CA, Cahaya HS, Wong A, Zhang J, Meng YG, Eigenbrot C, Pantua H, Diao J, Kapadia SB, Deng R, Kelley RF.

MAbs. 2014;6(5):1255-64. doi: 10.4161/mabs.29809. Epub 2014 Oct 30.

29.

Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase.

Fauber BP, Dragovich PS, Chen J, Corson LB, Ding CZ, Eigenbrot C, Labadie S, Malek S, Peterson D, Purkey HE, Robarge K, Sideris S, Ultsch M, Wei B, Yen I, Yue Q, Zhou A.

Bioorg Med Chem Lett. 2014 Dec 15;24(24):5683-5687. doi: 10.1016/j.bmcl.2014.10.067. Epub 2014 Oct 27.

PMID:
25467161
30.

Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.

Labadie S, Dragovich PS, Chen J, Fauber BP, Boggs J, Corson LB, Ding CZ, Eigenbrot C, Ge H, Ho Q, Lai KW, Ma S, Malek S, Peterson D, Purkey HE, Robarge K, Salphati L, Sideris S, Ultsch M, VanderPorten E, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X, Zhou A.

Bioorg Med Chem Lett. 2015 Jan 1;25(1):75-82. Epub 2014 Nov 10.

PMID:
25466195
31.

Design, synthesis and structure-activity relationships of a novel class of sulfonylpyridine inhibitors of Interleukin-2 inducible T-cell kinase (ITK).

Trani G, Barker JJ, Bromidge SM, Brookfield FA, Burch JD, Chen Y, Eigenbrot C, Heifetz A, Ismaili MHA, Johnson A, Krülle TM, MacKinnon CH, Maghames R, McEwan PA, Montalbetti CAGN, Ortwine DF, Pérez-Fuertes Y, Vaidya DG, Wang X, Zarrin AA, Pei Z.

Bioorg Med Chem Lett. 2014 Dec 15;24(24):5818-5823. doi: 10.1016/j.bmcl.2014.10.020. Epub 2014 Oct 12.

PMID:
25455497
32.

Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.

Hanan EJ, Eigenbrot C, Bryan MC, Burdick DJ, Chan BK, Chen Y, Dotson J, Heald RA, Jackson PS, La H, Lainchbury MD, Malek S, Purkey HE, Schaefer G, Schmidt S, Seward EM, Sideris S, Tam C, Wang S, Yeap SK, Yen I, Yin J, Yu C, Zilberleyb I, Heffron TP.

J Med Chem. 2014 Dec 11;57(23):10176-91. doi: 10.1021/jm501578n. Epub 2014 Nov 20.

33.

Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.

Robarge KD, Lee W, Eigenbrot C, Ultsch M, Wiesmann C, Heald R, Price S, Hewitt J, Jackson P, Savy P, Burton B, Choo EF, Pang J, Boggs J, Yang A, Yang X, Baumgardner M.

Bioorg Med Chem Lett. 2014 Oct 1;24(19):4714-4723. doi: 10.1016/j.bmcl.2014.08.008. Epub 2014 Aug 15.

PMID:
25193232
34.

Structures of neutrophil serine protease 4 reveal an unusual mechanism of substrate recognition by a trypsin-fold protease.

Lin SJ, Dong KC, Eigenbrot C, van Lookeren Campagne M, Kirchhofer D.

Structure. 2014 Sep 2;22(9):1333-1340. doi: 10.1016/j.str.2014.07.008. Epub 2014 Aug 21.

35.

Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.

Dragovich PS, Fauber BP, Boggs J, Chen J, Corson LB, Ding CZ, Eigenbrot C, Ge H, Giannetti AM, Hunsaker T, Labadie S, Li C, Liu Y, Liu Y, Ma S, Malek S, Peterson D, Pitts KE, Purkey HE, Robarge K, Salphati L, Sideris S, Ultsch M, VanderPorten E, Wang J, Wei B, Xu Q, Yen I, Yue Q, Zhang H, Zhang X, Zhou A.

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3764-71. doi: 10.1016/j.bmcl.2014.06.076. Epub 2014 Jul 1.

PMID:
25037916
36.

Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors.

Burch JD, Lau K, Barker JJ, Brookfield F, Chen Y, Chen Y, Eigenbrot C, Ellebrandt C, Ismaili MH, Johnson A, Kordt D, MacKinnon CH, McEwan PA, Ortwine DF, Stein DB, Wang X, Winkler D, Yuen PW, Zhang Y, Zarrin AA, Pei Z.

J Med Chem. 2014 Jul 10;57(13):5714-27. doi: 10.1021/jm500550e. Epub 2014 Jun 27.

PMID:
24918870
37.

An allosteric switch for pro-HGF/Met signaling using zymogen activator peptides.

Landgraf KE, Steffek M, Quan C, Tom J, Yu C, Santell L, Maun HR, Eigenbrot C, Lazarus RA.

Nat Chem Biol. 2014 Jul;10(7):567-73. doi: 10.1038/nchembio.1533. Epub 2014 May 25.

PMID:
24859116
38.

Structure of the pseudokinase-kinase domains from protein kinase TYK2 reveals a mechanism for Janus kinase (JAK) autoinhibition.

Lupardus PJ, Ultsch M, Wallweber H, Bir Kohli P, Johnson AR, Eigenbrot C.

Proc Natl Acad Sci U S A. 2014 Jun 3;111(22):8025-30. doi: 10.1073/pnas.1401180111. Epub 2014 May 19.

39.

Generation of a high-fidelity antibody against nerve growth factor using library scanning mutagenesis and validation with structures of the initial and optimized Fab-antigen complexes.

La Porte SL, Eigenbrot C, Ultsch M, Ho WH, Foletti D, Forgie A, Lindquist KC, Shelton DL, Pons J.

MAbs. 2014 Jul-Aug;6(4):1059-68.

40.

Discovery and optimization of indazoles as potent and selective interleukin-2 inducible T cell kinase (ITK) inhibitors.

Pastor RM, Burch JD, Magnuson S, Ortwine DF, Chen Y, De La Torre K, Ding X, Eigenbrot C, Johnson A, Liimatta M, Liu Y, Shia S, Wang X, Wu LC, Pei Z.

Bioorg Med Chem Lett. 2014 Jun 1;24(11):2448-52. doi: 10.1016/j.bmcl.2014.04.023. Epub 2014 Apr 16.

PMID:
24767842
41.

Antiparallel conformation of knob and hole aglycosylated half-antibody homodimers is mediated by a CH2-CH3 hydrophobic interaction.

Elliott JM, Ultsch M, Lee J, Tong R, Takeda K, Spiess C, Eigenbrot C, Scheer JM.

J Mol Biol. 2014 May 1;426(9):1947-57. doi: 10.1016/j.jmb.2014.02.015. Epub 2014 Feb 24.

PMID:
24576605
42.

Identification of a small peptide that inhibits PCSK9 protein binding to the low density lipoprotein receptor.

Zhang Y, Eigenbrot C, Zhou L, Shia S, Li W, Quan C, Tom J, Moran P, Di Lello P, Skelton NJ, Kong-Beltran M, Peterson A, Kirchhofer D.

J Biol Chem. 2014 Jan 10;289(2):942-55. doi: 10.1074/jbc.M113.514067. Epub 2013 Nov 13.

43.

Structure-based design and synthesis of potent benzothiazole inhibitors of interleukin-2 inducible T cell kinase (ITK).

MacKinnon CH, Lau K, Burch JD, Chen Y, Dines J, Ding X, Eigenbrot C, Heifetz A, Jaochico A, Johnson A, Kraemer J, Kruger S, Krülle TM, Liimatta M, Ly J, Maghames R, Montalbetti CA, Ortwine DF, Pérez-Fuertes Y, Shia S, Stein DB, Trani G, Vaidya DG, Wang X, Bromidge SM, Wu LC, Pei Z.

Bioorg Med Chem Lett. 2013 Dec 1;23(23):6331-5. doi: 10.1016/j.bmcl.2013.09.069. Epub 2013 Oct 1.

PMID:
24138940
44.

Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors.

Labadie S, Barrett K, Blair WS, Chang C, Deshmukh G, Eigenbrot C, Gibbons P, Johnson A, Kenny JR, Kohli PB, Liimatta M, Lupardus PJ, Shia S, Steffek M, Ubhayakar S, van Abbema A, Zak M.

Bioorg Med Chem Lett. 2013 Nov 1;23(21):5923-30. doi: 10.1016/j.bmcl.2013.08.082. Epub 2013 Aug 27.

PMID:
24042009
45.

Identification of 2-amino-5-aryl-pyrazines as inhibitors of human lactate dehydrogenase.

Fauber BP, Dragovich PS, Chen J, Corson LB, Ding CZ, Eigenbrot C, Giannetti AM, Hunsaker T, Labadie S, Liu Y, Liu Y, Malek S, Peterson D, Pitts K, Sideris S, Ultsch M, VanderPorten E, Wang J, Wei B, Yen I, Yue Q.

Bioorg Med Chem Lett. 2013 Oct 15;23(20):5533-9. doi: 10.1016/j.bmcl.2013.08.060. Epub 2013 Aug 22.

PMID:
24012183
46.

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
47.

Lead identification of novel and selective TYK2 inhibitors.

Liang J, Tsui V, Van Abbema A, Bao L, Barrett K, Beresini M, Berezhkovskiy L, Blair WS, Chang C, Driscoll J, Eigenbrot C, Ghilardi N, Gibbons P, Halladay J, Johnson A, Kohli PB, Lai Y, Liimatta M, Mantik P, Menghrajani K, Murray J, Sambrone A, Xiao Y, Shia S, Shin Y, Smith J, Sohn S, Stanley M, Ultsch M, Zhang B, Wu LC, Magnuson S.

Eur J Med Chem. 2013 Sep;67:175-87. doi: 10.1016/j.ejmech.2013.03.070. Epub 2013 May 14.

PMID:
23867602
48.

Generation and characterization of a unique reagent that recognizes a panel of recombinant human monoclonal antibody therapeutics in the presence of endogenous human IgG.

Wang X, Quarmby V, Ng C, Chuntharapai A, Shek T, Eigenbrot C, Kelley RF, Shia S, McCutcheon K, Lowe J, Leddy C, Coachman K, Cain G, Chu F, Hotzel I, Maia M, Wakshull E, Yang J.

MAbs. 2013 Jul-Aug;5(4):540-54. doi: 10.4161/mabs.24822. Epub 2013 Apr 29.

49.

Two-in-One antibodies with dual action Fabs.

Eigenbrot C, Fuh G.

Curr Opin Chem Biol. 2013 Jun;17(3):400-5. doi: 10.1016/j.cbpa.2013.04.015. Epub 2013 May 14. Review.

PMID:
23683347
50.

Oncogenic ERBB3 mutations in human cancers.

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