CMIDD - Center for Molecular Innovation and Drug Discovery

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2019

A novel strategy to block mitotic progression for targeted therapy

Chi, J. J., Li, H., Zhou, Z., Izquierdo-Ferrer, J., Xue, Y., Wavelet, C. M., Schiltz, G. E., Zhang, B., Cristofanilli, M., Lu, X., Bahar, I. & Wan, Y., Nov 2019, In : EBioMedicine. 49, p. 40-54 15 p.

Research output: Contribution to journalArticle

Open Access
3 Scopus citations

Development of Tetrahydroindazole-Based Potent and Selective Sigma-2 Receptor Ligands

Iyamu, I. D., Lv, W., Malik, N., Mishra, R. K. & Schiltz, G. E., Jul 3 2019, In : ChemMedChem. 14, 13, p. 1248-1256 9 p.

Research output: Contribution to journalArticle

Discovery of a novel class of potent and selective tetrahydroindazole-based sigma-1 receptor ligands

Iyamu, I. D., Lv, W., Malik, N., Mishra, R. K. & Schiltz, G. E., May 1 2019, In : Bioorganic and Medicinal Chemistry. 27, 9, p. 1824-1835 12 p.

Research output: Contribution to journalArticle

2 Scopus citations

Discovery of covalent enzyme inhibitors using virtual docking of covalent fragments

Chowdhury, S. R., Kennedy, S., Zhu, K., Mishra, R., Chuong, P., Nguyen, A. U., Kathman, S. G. & Statsyuk, A. V., Jan 1 2019, In : Bioorganic and Medicinal Chemistry Letters. 29, 1, p. 36-39 4 p.

Research output: Contribution to journalArticle

4 Scopus citations

Discovery of novel Mnk inhibitors using mutation-based induced-fit virtual high-throughput screening

Mishra, R. K., Clutter, M. R., Blyth, G. T., Kosciuczuk, E. M., Blackburn, A. Z., Beauchamp, E. M., Schiltz, G. E. & Platanias, L. C., Oct 1 2019, In : Chemical Biology and Drug Design. 94, 4, p. 1813-1823 11 p.

Research output: Contribution to journalArticle

1 Scopus citations

Modeling MEK4 Kinase Inhibitors through Perturbed Electrostatic Potential (ESP) Charges

Mishra, R. K., Deibler, K. K., Clutter, M. R., Vagadia, P. P., O'Connor, M., Schiltz, G. E., Bergan, R. & Scheidt, K. A., Jan 1 2019, (Accepted/In press) In : Journal of Chemical Information and Modeling.

Research output: Contribution to journalArticle

1 Scopus citations
2 Scopus citations

Regulation of MLL/COMPASS stability through its proteolytic cleavage by taspase1 as a possible approach for clinical therapy of leukemia

Zhao, Z., Wang, L., Volk, A. G., Birch, N. W., Stoltz, K. L., Bartom, E. T., Marshall, S. A., Rendleman, E. J., Nestler, C. M., Shilati, J., Schiltz, G. E., Crispino, J. D. & Shilatifard, A., Jan 1 2019, In : Genes and Development. 33, 1-2, p. 61-74 14 p.

Research output: Contribution to journalArticle

8 Scopus citations

Small-Molecule MYC Inhibitors Suppress Tumor Growth and Enhance Immunotherapy

Han, H., Jain, A. D., Truica, M. I., Izquierdo-Ferrer, J., Anker, J. F., Lysy, B., Sagar, V., Luan, Y., Chalmers, Z. R., Unno, K., Mok, H., Vatapalli, R., Yoo, Y. A., Rodriguez, Y., Kandela, I., Parker, J. B., Chakravarti, D., Mishra, R. K., Schiltz, G. E. & Abdulkadir, S. A., Nov 11 2019, In : Cancer Cell. 36, 5, p. 483-497.e15

Research output: Contribution to journalArticle

7 Scopus citations

Small molecules target the interaction between tissue transglutaminase and fibronectin

Sima, L. E., Yakubov, B., Zhang, S., Condello, S., Grigorescu, A. A., Nwani, N. G., Chen, L., Schiltz, G. E., Arvanitis, C., Zhang, Z. Y. & Matei, D., Jan 1 2019, In : Molecular cancer therapeutics. 18, 6, p. 1057-1068 12 p.

Research output: Contribution to journalArticle

Synthesis and Biological Evaluation of 3-Arylindazoles as Selective MEK4 Inhibitors

Deibler, K. K., Schiltz, G. E., Clutter, M., Mishra, R. K., Vagadia, P. P., O'Connor, M., George, M. D., Gordon, R., Fowler, G., Bergan, R. & Scheidt, K. A., Mar 22 2019, In : ChemMedChem. 14, 6, p. 615-620 6 p.

Research output: Contribution to journalArticle

2 Scopus citations
2018

Selective disruption of TLR2/MyD88 interaction inhibits inflammation and attenuates Alzheimer's pathology

Rangasamy, S. B., Jana, M., Roy, A., Corbett, G. T., Kundu, M., Chandra, S., Mondal, S., Dasarathi, S., Mufson, E. J., Mishra, R. K., Luan, C-H., Bennett, D. A. & Pahan, K., Jul 10 2018, In : The Journal of clinical investigation.

Research output: Contribution to journalArticle

11 Scopus citations

Synthesis of a novel fused pyrrolodiazepine-based library with anti-cancer activity

Malik, N., Iyamu, I. D., Scheidt, K. A. & Schiltz, G. E., Apr 11 2018, In : Tetrahedron Letters. 59, 15, p. 1513-1516 4 p.

Research output: Contribution to journalArticle

3 Scopus citations

Targeting Processive Transcription Elongation via SEC Disruption for MYC-Induced Cancer Therapy

Liang, K., Smith, E. R., Aoi, Y., Stoltz, K. L., Katagi, H., Woodfin, A. R., Rendleman, E. J., Marshall, S. A., Murray, D. C., Wang, L., Ozark, P. A., Mishra, R. K., Hashizume, R., Schiltz, G. E. & Shilatifard, A., Oct 18 2018, In : Cell. 175, 3, p. 766-779.e17

Research output: Contribution to journalArticle

21 Scopus citations

Tissue tranglutaminase regulates interactions between ovarian cancer stem cells and the tumor niche

Condello, S., Sima, L., Ivan, C., Cardenas, H., Schiltz, G., Mishra, R. K. & Matei, D., Jun 1 2018, In : Cancer Research. 78, 11, p. 2990-3001 12 p.

Research output: Contribution to journalArticle

11 Scopus citations
2017

Cancer-Associated IDH1 Promotes Growth and Resistance to Targeted Therapies in the Absence of Mutation

Calvert, A. E., Chalastanis, A., Wu, Y., Hurley, L. A., Kouri, F., Bi, Y., Kachman, M., May, J. L., Bartom, E. T., Hua, Y., Mishra, R. K., Schiltz, G. E., Dubrovskyi, O., Mazar, A. P., Peter, M. E., Zheng, H., James, C. D., Burant, C. F., Chandel, N., Davuluri, R. V. & 2 others, Horbinski, C. M. & Stegh, A. H., May 30 2017, In : Cell reports. 19, 9, p. 1858-1873 16 p.

Research output: Contribution to journalArticle

43 Scopus citations

Development of GLUT4-selective antagonists for multiple myeloma therapy

Wei, C., Bajpai, R., Sharma, H., Heitmeier, M., Jain, A. D., Matulis, S. M., Nooka, A. K., Mishra, R. K., Hruz, P. W., Schiltz, G. E. & Shanmugam, M., Oct 20 2017, In : European Journal of Medicinal Chemistry. 139, p. 573-586 14 p.

Research output: Contribution to journalArticle

14 Scopus citations

Homology modeling of FFA2 identifies novel agonists that potentiate insulin secretion

Villa, S. R., Mishra, R. K., Zapater, J. L., Priyadarshini, M., Gilchrist, A., Mancebo, H., Schiltz, G. E. & Layden, B. T., Dec 1 2017, In : Journal of Investigative Medicine. 65, 8, p. 1116-1124 9 p.

Research output: Contribution to journalArticle

3 Scopus citations

Photoredox activation of carbon dioxide for amino acid synthesis in continuous flow

Seo, H., Katcher, M. H. & Jamison, T. F., May 1 2017, In : Nature chemistry. 9, 5, p. 453-456 4 p.

Research output: Contribution to journalArticle

135 Scopus citations
2016
23 Scopus citations

Method for identifying small molecule inhibitors of the protein-protein interaction between HCN1 and TRIP8b

Han, Y., Lyman, K. A., Clutter, M., Schiltz, G. E., Ismail, Q. A., Cheng, X., Luan, C. H. & Chetkovich, D. M., Nov 11 2016, In : Journal of Visualized Experiments. 2016, 117, e54540.

Research output: Contribution to journalArticle

4 Scopus citations
2015

Identification of small-molecule inhibitors of hyperpolarization-activated cyclic nucleotide-gated channels

Han, Y., Lyman, K., Clutter, M., Schiltz, G. E., Ismail, Q. A., Prados, D. B., Luan, C. H. & Chetkovich, D. M., Oct 22 2015, In : Journal of Biomolecular Screening. 20, 9, p. 1124-1131 8 p.

Research output: Contribution to journalArticle

13 Scopus citations

In Silico Modeling-based Identification of Glucose Transporter 4 (GLUT4)-selective Inhibitors for Cancer Therapy

Mishra, R. K., Wei, C., Hresko, R. C., Bajpai, R., Heitmeier, M., Matulis, S. M., Nooka, A. K., Rosen, S. T., Hruz, P. W., Schiltz, G. E. & Shanmugam, M., Jun 5 2015, In : Journal of Biological Chemistry. 290, 23, p. 14441-14453 13 p.

Research output: Contribution to journalArticle

33 Scopus citations

Virtual High-Throughput Screening to Identify Novel Activin Antagonists

Zhu, J., Mishra, R. K., Schiltz, G. E., Makanji, Y., Scheidt, K. A., Mazar, A. P. & Woodruff, T. K., Jul 23 2015, In : Journal of Medicinal Chemistry. 58, 14, p. 5637-5648 12 p.

Research output: Contribution to journalArticle

8 Scopus citations
2014

Design and synthesis of potent macrocyclic HIV-1 protease inhibitors involving P1-P2 ligands

Ghosh, A. K., Schiltz, G. E., Rusere, L. N., Osswald, H. L., Walters, D. E., Amano, M. & Mitsuya, H., Sep 21 2014, In : Organic and Biomolecular Chemistry. 12, 35, p. 6842-6854 13 p.

Research output: Contribution to journalArticle

14 Scopus citations
9 Scopus citations

Mechanistic investigations of palladium-catalyzed allylic fluorination

Katcher, M. H., Norrby, P. O. & Doyle, A. G., May 12 2014, In : Organometallics. 33, 9, p. 2121-2133 13 p.

Research output: Contribution to journalArticle

47 Scopus citations

The discovery of reverse tricyclic pyridone JAK2 inhibitors. Part 2: Lead optimization

Siu, T., Kumarasinghe, S. E., Altman, M. D., Katcher, M., Northrup, A., White, C., Rosenstein, C., Mathur, A., Xu, L., Chan, G., Bachman, E., Bouthillette, M., Dinsmore, C. J., Marshall, C. G. & Young, J. R., Mar 15 2014, In : Bioorganic and Medicinal Chemistry Letters. 24, 6, p. 1466-1471 6 p.

Research output: Contribution to journalArticle

3 Scopus citations
2013

Carbofluorination via a palladium-catalyzed cascade reaction

Braun, M. G., Katcher, M. H. & Doyle, A. G., Feb 4 2013, In : Chemical Science. 4, 3, p. 1216-1220 5 p.

Research output: Contribution to journalArticle

55 Scopus citations

Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5] cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met

Northrup, A. B., Katcher, M. H., Altman, M. D., Chenard, M., Daniels, M. H., Deshmukh, S. V., Falcone, D., Guerin, D. J., Hatch, H., Li, C., Lu, W., Lutterbach, B., Allison, T. J., Patel, S. B., Reilly, J. F., Reutershan, M., Rickert, K. W., Rosenstein, C., Soisson, S. M., Szewczak, A. A. & 5 others, Walker, D., Wilson, K., Young, J. R., Pan, B. S. & Dinsmore, C. J., Mar 28 2013, In : Journal of Medicinal Chemistry. 56, 6, p. 2294-2310 17 p.

Research output: Contribution to journalArticle

23 Scopus citations
2011

Palladium-catalyzed regio- and enantioselective fluorination of acyclic allylic halides

Katcher, M. H., Sha, A. & Doyle, A. G., Oct 12 2011, In : Journal of the American Chemical Society. 133, 40, p. 15902-15905 4 p.

Research output: Contribution to journalArticle

120 Scopus citations
2010

Palladium-catalyzed asymmetric synthesis of allylic fluorides

Katcher, M. H. & Doyle, A. G., Dec 15 2010, In : Journal of the American Chemical Society. 132, 49, p. 17402-17404 3 p.

Research output: Contribution to journalArticle

137 Scopus citations
2007

A new strategy for the synthesis of benzylic sulfonamides: Palladium-catalyzed arylation and sulfonamide metathesis

Grimm, J. B., Katcher, M. H., Witter, D. J. & Northrup, A. B., Oct 12 2007, In : Journal of Organic Chemistry. 72, 21, p. 8135-8138 4 p.

Research output: Contribution to journalArticle

23 Scopus citations
2006

Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the P′2-ligands

Ghosh, A. K., Schiltz, G., Perali, R. S., Leshchenko, S., Kay, S., Walters, D. E., Koh, Y., Maeda, K. & Mitsuya, H., Apr 1 2006, In : Bioorganic and Medicinal Chemistry Letters. 16, 7, p. 1869-1873 5 p.

Research output: Contribution to journalArticle

82 Scopus citations
2002

Multicomponent reactions: Synthesis of spirocyclic tetrahydropyran derivatives by prins cyclization

Ghosh, A. K., Shin, D. & Schiltz, G., Nov 22 2002, In : Heterocycles. 58, p. 659-666 8 p.

Research output: Contribution to journalArticle

15 Scopus citations