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Items: 1 to 20 of 111

1.

Lead optimization and efficacy evaluation of quinazoline-based BET family inhibitors for potential treatment of cancer and inflammatory diseases.

Yang SM, Yoshioka M, Strovel JW, Urban DJ, Hu X, Hall MD, Jadhav A, Maloney DJ.

Bioorg Med Chem Lett. 2019 Mar 12. pii: S0960-894X(19)30143-X. doi: 10.1016/j.bmcl.2019.03.014. [Epub ahead of print]

PMID:
30905542
2.

KDM5 Histone Demethylase Activity Links Cellular Transcriptomic Heterogeneity to Therapeutic Resistance.

Hinohara K, Wu HJ, Sébastien Vigneau, McDonald TO, Igarashi KJ, Yamamoto KN, Madsen T, Fassl A, Egri SB, Papanastasiou M, Ding L, Peluffo G, Cohen O, Kales SC, Lal-Nag M, Rai G, Maloney DJ, Jadhav A, Simeonov A, Wagle N, Brown M, Meissner A, Sicinski P, Jaffe JD, Jeselsohn R, Gimelbrant AA, Michor F, Polyak K.

Cancer Cell. 2019 Feb 11;35(2):330-332. doi: 10.1016/j.ccell.2019.01.012. No abstract available.

3.

A high-throughput screen to identify novel small molecule inhibitors of the Werner Syndrome Helicase-Nuclease (WRN).

Sommers JA, Kulikowicz T, Croteau DL, Dexheimer T, Dorjsuren D, Jadhav A, Maloney DJ, Simeonov A, Bohr VA, Brosh RM Jr.

PLoS One. 2019 Jan 9;14(1):e0210525. doi: 10.1371/journal.pone.0210525. eCollection 2019.

4.

Molecular basis for activation of lecithin:cholesterol acyltransferase by a compound that increases HDL cholesterol.

Manthei KA, Yang SM, Baljinnyam B, Chang L, Glukhova A, Yuan W, Freeman LA, Maloney DJ, Schwendeman A, Remaley AT, Jadhav A, Tesmer JJ.

Elife. 2018 Nov 27;7. pii: e41604. doi: 10.7554/eLife.41604.

5.

KDM5 Histone Demethylase Activity Links Cellular Transcriptomic Heterogeneity to Therapeutic Resistance.

Hinohara K, Wu HJ, Vigneau S, McDonald TO, Igarashi KJ, Yamamoto KN, Madsen T, Fassl A, Egri SB, Papanastasiou M, Ding L, Peluffo G, Cohen O, Kales SC, Lal-Nag M, Rai G, Maloney DJ, Jadhav A, Simeonov A, Wagle N, Brown M, Meissner A, Sicinski P, Jaffe JD, Jeselsohn R, Gimelbrant AA, Michor F, Polyak K.

Cancer Cell. 2018 Dec 10;34(6):939-953.e9. doi: 10.1016/j.ccell.2018.10.014. Epub 2018 Nov 21. Erratum in: Cancer Cell. 2019 Feb 11;35(2):330-332.

PMID:
30472020
6.

Predicting Novel Therapies and Targets: Regulation of Notch3 by the Bromodomain Protein BRD4.

Villar-Prados A, Wu SY, Court KA, Ma S, LaFargue C, Chowdhury MA, Engelhardt MI, Ivan C, Ram PT, Wang Y, Baggerly K, Rodriguez-Aguayo C, Lopez-Berestein G, Ming-Yang S, Maloney DJ, Yoshioka M, Strovel JW, Roszik J, Sood AK.

Mol Cancer Ther. 2019 Feb;18(2):421-436. doi: 10.1158/1535-7163.MCT-18-0365. Epub 2018 Nov 12.

PMID:
30420565
7.

Structure-Based Engineering of Irreversible Inhibitors against Histone Lysine Demethylase KDM5A.

Horton JR, Woodcock CB, Chen Q, Liu X, Zhang X, Shanks J, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Cyr M, Pohida K, Hu X, Shah P, Xu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Cheng X.

J Med Chem. 2018 Nov 15. doi: 10.1021/acs.jmedchem.8b01219. [Epub ahead of print]

PMID:
30392349
8.

Discovery and lead identification of quinazoline-based BRD4 inhibitors.

Yang SM, Urban DJ, Yoshioka M, Strovel JW, Fletcher S, Wang AQ, Xu X, Shah P, Hu X, Hall MD, Jadhav A, Maloney DJ.

Bioorg Med Chem Lett. 2018 Nov 15;28(21):3483-3488. doi: 10.1016/j.bmcl.2018.08.039. Epub 2018 Aug 31.

PMID:
30268702
9.

Inhibition of spinal 15-LOX-1 attenuates TLR4-dependent, nonsteroidal anti-inflammatory drug-unresponsive hyperalgesia in male rats.

Gregus AM, Buczynski MW, Dumlao DS, Norris PC, Rai G, Simeonov A, Maloney DJ, Jadhav A, Xu Q, Wei SC, Fitzsimmons BL, Dennis EA, Yaksh TL.

Pain. 2018 Dec;159(12):2620-2629. doi: 10.1097/j.pain.0000000000001373.

PMID:
30130298
10.

KDM5 histone demethylases repress immune response via suppression of STING.

Wu L, Cao J, Cai WL, Lang SM, Horton JR, Jansen DJ, Liu ZZ, Chen JF, Zhang M, Mott BT, Pohida K, Rai G, Kales SC, Henderson MJ, Hu X, Jadhav A, Maloney DJ, Simeonov A, Zhu S, Iwasaki A, Hall MD, Cheng X, Shadel GS, Yan Q.

PLoS Biol. 2018 Aug 6;16(8):e2006134. doi: 10.1371/journal.pbio.2006134. eCollection 2018 Aug.

11.

Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity.

Yang SM, Martinez NJ, Yasgar A, Danchik C, Johansson C, Wang Y, Baljinnyam B, Wang AQ, Xu X, Shah P, Cheff D, Wang XS, Roth J, Lal-Nag M, Dunford JE, Oppermann U, Vasiliou V, Simeonov A, Jadhav A, Maloney DJ.

J Med Chem. 2018 Jun 14;61(11):4883-4903. doi: 10.1021/acs.jmedchem.8b00270. Epub 2018 May 31.

12.

Correction: A High-Content Assay Enables the Automated Screening and Identification of Small Molecules with Specific ALDH1A1-Inhibitory Activity.

Yasgar A, Titus SA, Wang Y, Danchik C, Yang SM, Vasiliou V, Jadhav A, Maloney DJ, Simeonov A, Martinez NJ.

PLoS One. 2018 May 15;13(5):e0197292. doi: 10.1371/journal.pone.0197292. eCollection 2018.

13.

DDB2 represses ovarian cancer cell dedifferentiation by suppressing ALDH1A1.

Cui T, Srivastava AK, Han C, Wu D, Wani N, Liu L, Gao Z, Qu M, Zou N, Zhang X, Yi P, Yu J, Bell EH, Yang SM, Maloney DJ, Zheng Y, Wani AA, Wang QE.

Cell Death Dis. 2018 May 1;9(5):561. doi: 10.1038/s41419-018-0585-y.

14.

Insights into the Action of Inhibitor Enantiomers against Histone Lysine Demethylase 5A.

Horton JR, Liu X, Wu L, Zhang K, Shanks J, Zhang X, Rai G, Mott BT, Jansen DJ, Kales SC, Henderson MJ, Pohida K, Fang Y, Hu X, Jadhav A, Maloney DJ, Hall MD, Simeonov A, Fu H, Vertino PM, Yan Q, Cheng X.

J Med Chem. 2018 Apr 12;61(7):3193-3208. doi: 10.1021/acs.jmedchem.8b00261. Epub 2018 Mar 23.

15.

Irreversible inhibition of cytosolic thioredoxin reductase 1 as a mechanistic basis for anticancer therapy.

Stafford WC, Peng X, Olofsson MH, Zhang X, Luci DK, Lu L, Cheng Q, Trésaugues L, Dexheimer TS, Coussens NP, Augsten M, Ahlzén HM, Orwar O, Östman A, Stone-Elander S, Maloney DJ, Jadhav A, Simeonov A, Linder S, Arnér ESJ.

Sci Transl Med. 2018 Feb 14;10(428). pii: eaaf7444. doi: 10.1126/scitranslmed.aaf7444.

PMID:
29444979
16.

Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).

Rai G, Brimacombe KR, Mott BT, Urban DJ, Hu X, Yang SM, Lee TD, Cheff DM, Kouznetsova J, Benavides GA, Pohida K, Kuenstner EJ, Luci DK, Lukacs CM, Davies DR, Dranow DM, Zhu H, Sulikowski G, Moore WJ, Stott GM, Flint AJ, Hall MD, Darley-Usmar VM, Neckers LM, Dang CV, Waterson AG, Simeonov A, Jadhav A, Maloney DJ.

J Med Chem. 2017 Nov 22;60(22):9184-9204. doi: 10.1021/acs.jmedchem.7b00941. Epub 2017 Nov 9.

17.

Inhibition of 12/15-Lipoxygenase Protects Against β-Cell Oxidative Stress and Glycemic Deterioration in Mouse Models of Type 1 Diabetes.

Hernandez-Perez M, Chopra G, Fine J, Conteh AM, Anderson RM, Linnemann AK, Benjamin C, Nelson JB, Benninger KS, Nadler JL, Maloney DJ, Tersey SA, Mirmira RG.

Diabetes. 2017 Nov;66(11):2875-2887. doi: 10.2337/db17-0215. Epub 2017 Aug 25.

18.

Parallel Chemistry Approach to Identify Novel Nuclear Receptor Ligands Based on the GW0742 Scaffold.

Teske KA, Rai G, Nandhikonda P, Sidhu PS, Feleke B, Simeonov A, Yasgar A, Jadhav A, Maloney DJ, Arnold LA.

ACS Comb Sci. 2017 Oct 9;19(10):646-656. doi: 10.1021/acscombsci.7b00066. Epub 2017 Sep 5.

19.

First Selective 12-LOX Inhibitor, ML355, Impairs Thrombus Formation and Vessel Occlusion In Vivo With Minimal Effects on Hemostasis.

Adili R, Tourdot BE, Mast K, Yeung J, Freedman JC, Green A, Luci DK, Jadhav A, Simeonov A, Maloney DJ, Holman TR, Holinstat M.

Arterioscler Thromb Vasc Biol. 2017 Oct;37(10):1828-1839. doi: 10.1161/ATVBAHA.117.309868. Epub 2017 Aug 3.

20.

12-Lipoxygenase Inhibitor Improves Functions of Cytokine-Treated Human Islets and Type 2 Diabetic Islets.

Ma K, Xiao A, Park SH, Glenn L, Jackson L, Barot T, Weaver JR, Taylor-Fishwick DA, Luci DK, Maloney DJ, Mirmira RG, Imai Y, Nadler JL.

J Clin Endocrinol Metab. 2017 Aug 1;102(8):2789-2797. doi: 10.1210/jc.2017-00267.

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