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Items: 41

1.

Discovery of Novel Dual Mechanism of Action Src Signaling and Tubulin Polymerization Inhibitors (KX2-391 and KX2-361).

Smolinski MP, Bu Y, Clements J, Gelman IH, Hegab T, Cutler DL, Fang JWS, Fetterly G, Kwan R, Barnett A, Lau JYN, Hangauer DG.

J Med Chem. 2018 Jun 14;61(11):4704-4719. doi: 10.1021/acs.jmedchem.8b00164. Epub 2018 Apr 17.

PMID:
29617135
2.

Dual Src Kinase/Pretubulin Inhibitor KX-01, Sensitizes ERα-negative Breast Cancers to Tamoxifen through ERα Reexpression.

Anbalagan M, Sheng M, Fleischer B, Zhang Y, Gao Y, Hoang V, Matossian M, Burks HE, Burow ME, Collins-Burow BM, Hangauer D, Rowan BG.

Mol Cancer Res. 2017 Nov;15(11):1491-1502. doi: 10.1158/1541-7786.MCR-16-0297-T. Epub 2017 Jul 27.

PMID:
28751463
3.

Modulating hydrogen-bond basicity within the context of protein-ligand binding: A case study with thrombin inhibitors that reveals a dominating role for desolvation.

Nasief NN, Said AM, Hangauer D.

Eur J Med Chem. 2017 Jan 5;125:975-991. doi: 10.1016/j.ejmech.2016.09.038. Epub 2016 Sep 13.

PMID:
27816890
4.

Antitumor Effect of KX-01 through Inhibiting Src Family Kinases and Mitosis.

Kim S, Min A, Lee KH, Yang Y, Kim TY, Lim JM, Park SJ, Nam HJ, Kim JE, Song SH, Han SW, Oh DY, Kim JH, Kim TY, Hangauer D, Lau JY, Im K, Lee DS, Bang YJ, Im SA.

Cancer Res Treat. 2017 Jul;49(3):643-655. doi: 10.4143/crt.2016.168. Epub 2016 Oct 6.

5.

Ion Current-Based Proteomic Profiling for Understanding the Inhibitory Effect of Tumor Necrosis Factor Alpha on Myogenic Differentiation.

Tu C, Bu Y, Vujcic M, Shen S, Li J, Qu M, Hangauer D, Clements JL, Qu J.

J Proteome Res. 2016 Sep 2;15(9):3147-57. doi: 10.1021/acs.jproteome.6b00321. Epub 2016 Aug 17.

PMID:
27480135
6.

Ligand binding cooperativity: Bioisosteric replacement of CO with SO2 among thrombin inhibitors.

Said AM, Hangauer DG.

Bioorg Med Chem Lett. 2016 Aug 15;26(16):3850-4. doi: 10.1016/j.bmcl.2016.07.024. Epub 2016 Jul 9.

PMID:
27445170
7.
8.

Additivity or cooperativity: which model can predict the influence of simultaneous incorporation of two or more functionalities in a ligand molecule?

Nasief NN, Hangauer D.

Eur J Med Chem. 2015 Jan 27;90:897-915. doi: 10.1016/j.ejmech.2014.11.056. Epub 2014 Nov 28.

PMID:
25559080
9.

Influence of neighboring groups on the thermodynamics of hydrophobic binding: an added complex facet to the hydrophobic effect.

Nasief NN, Hangauer D.

J Med Chem. 2014 Mar 27;57(6):2315-33. doi: 10.1021/jm401609a. Epub 2014 Mar 18.

PMID:
24479949
10.

Targeting SRC and tubulin in mucinous ovarian carcinoma.

Liu T, Hu W, Dalton HJ, Choi HJ, Huang J, Kang Y, Pradeep S, Miyake T, Song JH, Wen Y, Lu C, Pecot CV, Bottsford-Miller J, Zand B, Jennings NB, Ivan C, Gallick GE, Baggerly KA, Hangauer DG, Coleman RL, Frumovitz M, Sood AK.

Clin Cancer Res. 2013 Dec 1;19(23):6532-43. doi: 10.1158/1078-0432.CCR-13-1305. Epub 2013 Oct 7.

11.

A phase I trial of KX2-391, a novel non-ATP competitive substrate-pocket- directed SRC inhibitor, in patients with advanced malignancies.

Naing A, Cohen R, Dy GK, Hong DS, Dyster L, Hangauer DG, Kwan R, Fetterly G, Kurzrock R, Adjei AA.

Invest New Drugs. 2013 Aug;31(4):967-73. doi: 10.1007/s10637-013-9929-8. Epub 2013 Jan 30.

PMID:
23361621
12.

A phase 2 study of KX2-391, an oral inhibitor of Src kinase and tubulin polymerization, in men with bone-metastatic castration-resistant prostate cancer.

Antonarakis ES, Heath EI, Posadas EM, Yu EY, Harrison MR, Bruce JY, Cho SY, Wilding GE, Fetterly GJ, Hangauer DG, Kwan MF, Dyster LM, Carducci MA.

Cancer Chemother Pharmacol. 2013 Apr;71(4):883-92. doi: 10.1007/s00280-013-2079-z. Epub 2013 Jan 13.

13.

Dissecting the hydrophobic effect on the molecular level: the role of water, enthalpy, and entropy in ligand binding to thermolysin.

Biela A, Nasief NN, Betz M, Heine A, Hangauer D, Klebe G.

Angew Chem Int Ed Engl. 2013 Feb 4;52(6):1822-8. doi: 10.1002/anie.201208561. Epub 2013 Jan 2. No abstract available.

PMID:
23283700
14.
16.

Peptidomimetic Src/pretubulin inhibitor KX-01 alone and in combination with paclitaxel suppresses growth, metastasis in human ER/PR/HER2-negative tumor xenografts.

Anbalagan M, Ali A, Jones RK, Marsden CG, Sheng M, Carrier L, Bu Y, Hangauer D, Rowan BG.

Mol Cancer Ther. 2012 Sep;11(9):1936-47. doi: 10.1158/1535-7163.MCT-12-0146. Epub 2012 Jul 10.

17.

Impact of ligand and protein desolvation on ligand binding to the S1 pocket of thrombin.

Biela A, Khayat M, Tan H, Kong J, Heine A, Hangauer D, Klebe G.

J Mol Biol. 2012 May 18;418(5):350-66. doi: 10.1016/j.jmb.2012.01.054. Epub 2012 Feb 21.

PMID:
22366545
18.

Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities.

Fallah-Tafti A, Foroumadi A, Tiwari R, Shirazi AN, Hangauer DG, Bu Y, Akbarzadeh T, Parang K, Shafiee A.

Eur J Med Chem. 2011 Oct;46(10):4853-8. doi: 10.1016/j.ejmech.2011.07.050. Epub 2011 Aug 4.

19.

Protection from impulse noise-induced hearing loss with novel Src-protein tyrosine kinase inhibitors.

Bielefeld EC, Hangauer D, Henderson D.

Neurosci Res. 2011 Dec;71(4):348-54. doi: 10.1016/j.neures.2011.07.1836. Epub 2011 Aug 5.

20.

KX-01, a novel Src kinase inhibitor directed toward the peptide substrate site, synergizes with tamoxifen in estrogen receptor α positive breast cancer.

Anbalagan M, Carrier L, Glodowski S, Hangauer D, Shan B, Rowan BG.

Breast Cancer Res Treat. 2012 Apr;132(2):391-409. doi: 10.1007/s10549-011-1513-3. Epub 2011 Apr 21.

PMID:
21509526
21.

Congeneric but still distinct: how closely related trypsin ligands exhibit different thermodynamic and structural properties.

Brandt T, Holzmann N, Muley L, Khayat M, Wegscheid-Gerlach C, Baum B, Heine A, Hangauer D, Klebe G.

J Mol Biol. 2011 Feb 4;405(5):1170-87. doi: 10.1016/j.jmb.2010.11.038. Epub 2010 Nov 25.

PMID:
21111747
22.

Displacement of disordered water molecules from hydrophobic pocket creates enthalpic signature: binding of phosphonamidate to the S₁'-pocket of thermolysin.

Englert L, Biela A, Zayed M, Heine A, Hangauer D, Klebe G.

Biochim Biophys Acta. 2010 Nov;1800(11):1192-202. doi: 10.1016/j.bbagen.2010.06.009. Epub 2010 Jul 1.

PMID:
20600625
23.

Non-additivity of functional group contributions in protein-ligand binding: a comprehensive study by crystallography and isothermal titration calorimetry.

Baum B, Muley L, Smolinski M, Heine A, Hangauer D, Klebe G.

J Mol Biol. 2010 Apr 9;397(4):1042-54. doi: 10.1016/j.jmb.2010.02.007. Epub 2010 Feb 12.

PMID:
20156458
24.

Enhancement of hydrophobic interactions and hydrogen bond strength by cooperativity: synthesis, modeling, and molecular dynamics simulations of a congeneric series of thrombin inhibitors.

Muley L, Baum B, Smolinski M, Freindorf M, Heine A, Klebe G, Hangauer DG.

J Med Chem. 2010 Mar 11;53(5):2126-35. doi: 10.1021/jm9016416.

PMID:
20148533
25.

Think twice: understanding the high potency of bis(phenyl)methane inhibitors of thrombin.

Baum B, Muley L, Heine A, Smolinski M, Hangauer D, Klebe G.

J Mol Biol. 2009 Aug 21;391(3):552-64. doi: 10.1016/j.jmb.2009.06.016. Epub 2009 Jun 9.

PMID:
19520086
26.

More than a simple lipophilic contact: a detailed thermodynamic analysis of nonbasic residues in the s1 pocket of thrombin.

Baum B, Mohamed M, Zayed M, Gerlach C, Heine A, Hangauer D, Klebe G.

J Mol Biol. 2009 Jul 3;390(1):56-69. doi: 10.1016/j.jmb.2009.04.051. Epub 2009 May 3.

PMID:
19409395
27.

Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro.

Lau GM, Lau GM, Yu GL, Gelman IH, Gutowski A, Hangauer D, Fang JW.

Dig Dis Sci. 2009 Jul;54(7):1465-74. doi: 10.1007/s10620-008-0519-0. Epub 2008 Nov 1.

PMID:
18979199
28.

Thermodynamic inhibition profile of a cyclopentyl and a cyclohexyl derivative towards thrombin: the same but for different reasons.

Gerlach C, Smolinski M, Steuber H, Sotriffer CA, Heine A, Hangauer DG, Klebe G.

Angew Chem Int Ed Engl. 2007;46(44):8511-4. No abstract available.

PMID:
17902081
29.

Prevention of noise-induced hearing loss with Src-PTK inhibitors.

Harris KC, Hu B, Hangauer D, Henderson D.

Hear Res. 2005 Oct;208(1-2):14-25. Epub 2005 Jun 13.

PMID:
15950415
30.
31.

The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 2: hydroxyindole derivatives.

Milkiewicz KL, Marsilje TH, Woodworth RP Jr, Bifulco N Jr, Hangauer MJ, Hangauer DG.

Bioorg Med Chem Lett. 2000 Mar 6;10(5):483-6.

PMID:
10743953
32.
33.

The design, synthesis and activity of pentapeptide pp60c-src inhibitors containing L-phosphotyrosine mimics.

Lai JH, Marsilje TH, Choi S, Nair SA, Hangauer DG.

J Pept Res. 1998 Apr;51(4):271-81.

PMID:
9560002
34.

The design and synthesis of substituted biphenyl libraries.

Pavia MR, Cohen MP, Dilley GJ, Dubuc GR, Durgin TL, Forman FW, Hediger ME, Milot G, Powers TS, Sucholeiki I, Zhou S, Hangauer DG.

Bioorg Med Chem. 1996 May;4(5):659-66.

PMID:
8804530
35.

Synthesis of a Vicinal Tricarbonyl Amide Derivative of L-Phenylalanine.

Lai JH, Pham H, Hangauer DG.

J Org Chem. 1996 Mar 8;61(5):1872-1874. No abstract available.

PMID:
11667067
36.

Identification of efficient pentapeptide substrates for the tyrosine kinase pp60c-src.

Nair SA, Kim MH, Warren SD, Choi S, Songyang Z, Cantley LC, Hangauer DG.

J Med Chem. 1995 Oct 13;38(21):4276-83.

PMID:
7473555
38.

Synthesis and use of 3-amino-4-phenyl-2-piperidones and 4-amino-2-benzazepin-3-ones as conformationally restricted phenylalanine isosteres in renin inhibitors.

de Laszlo SE, Bush BL, Doyle JJ, Greenlee WJ, Hangauer DG, Halgren TA, Lynch RJ, Schorn TW, Siegl PK.

J Med Chem. 1992 Mar 6;35(5):833-46.

PMID:
1548675
39.

Design of a selective insulin receptor tyrosine kinase inhibitor and its effect on glucose uptake and metabolism in intact cells.

Saperstein R, Vicario PP, Strout HV, Brady E, Slater EE, Greenlee WJ, Ondeyka DL, Patchett AA, Hangauer DG.

Biochemistry. 1989 Jun 27;28(13):5694-701.

PMID:
2550060
40.

Modeling the mechanism of peptide cleavage by thermolysin.

Hangauer DG, Gund P, Andose JD, Bush BL, Fluder EM, McIntyre EF, Smith GM.

Ann N Y Acad Sci. 1985;439:124-39. No abstract available.

PMID:
2988395
41.

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