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- Publications
- Influence
Mediator Kinase Inhibition Further Activates Super-Enhancer Associated Genes in AML
- Henry E. Pelish, Brian B Liau, +23 authors M. D. Shair
- Biology, Medicine
- Nature
- 28 September 2015
Super-enhancers (SEs), which are composed of large clusters of enhancers densely loaded with the Mediator complex, transcription factors and chromatin regulators, drive high expression of genes… Expand
Natural products reveal cancer cell dependence on oxysterol-binding proteins.
- Anthony W G Burgett, T. B. Poulsen, +14 authors M. D. Shair
- Biology, Medicine
- Nature chemical biology
- 1 September 2011
Cephalostatin 1, OSW-1, ritterazine B and schweinfurthin A are natural products that potently, and in some cases selectively, inhibit the growth of cultured human cancer cell lines. The cellular… Expand
Identification of Mediator Kinase Substrates in Human Cells using Cortistatin A and Quantitative Phosphoproteomics.
- Zachary Poss, Christopher C. Ebmeier, +7 authors D. Taatjes
- Biology, Medicine
- Cell reports
- 12 April 2016
Cortistatin A (CA) is a highly selective inhibitor of the Mediator kinases CDK8 and CDK19. Using CA, we now report a large-scale identification of Mediator kinase substrates in human cells (HCT116).… Expand
Secramine inhibits Cdc42-dependent functions in cells and Cdc42 activation in vitro
- Henry E. Pelish, J. Peterson, +7 authors T. Kirchhausen
- Materials Science, Medicine
- Nature chemical biology
- 2006
Inspired by the usefulness of small molecules to study membrane traffic, we used high-throughput synthesis and phenotypic screening to discover secramine, a molecule that inhibits membrane traffic… Expand
Itraconazole Inhibits Enterovirus Replication by Targeting the Oxysterol-Binding Protein
- J. R. Strating, L. van der Linden, +20 authors F. V. van Kuppeveld
- Biology, Medicine
- Cell Reports
- 29 January 2015
Summary
Itraconazole (ITZ) is a well-known antifungal agent that also has anticancer activity. In this study, we identify ITZ as a broad-spectrum inhibitor of enteroviruses (e.g., poliovirus,… Expand
Stereoselective Synthesis of over Two Million Compounds Having Structural Features Both Reminiscent of Natural Products and Compatible with Miniaturized Cell-Based Assays
- D. Tan, M. Foley, M. D. Shair, S. Schreiber
- Chemistry
- 8 August 1998
Understanding the cellular function of a protein usually requires a means to alter the function. This is commonly done by mutating the gene encoding the protein (genetic approach). It can also be… Expand
Mediator Kinase Phosphorylation of STAT1 S727 Promotes Growth of Neoplasms With JAK-STAT Activation
- Ioana I. Nitulescu, Sara C Meyer, +5 authors M. D. Shair
- Chemistry, Medicine
- EBioMedicine
- 21 November 2017
Constitutive JAK-STAT signaling drives the proliferation of most myeloproliferative neoplasms (MPN) and a subset of acute myeloid leukemia (AML), but persistence emerges with chronic exposure to JAK… Expand
Biomimetic synthesis of (-)-longithorone A.
- M. E. Layton, C. A. Morales, M. D. Shair
- Chemistry, Medicine
- Journal of the American Chemical Society
- 12 January 2002
An enantioseletive, biomimetic synthesis of (-)-longithorone A has been achieved using an intermolecular/transannular Diels-Alder sequence which provides some support for the proposed biosynthesis.… Expand
Enantioselective total synthesis of hyperforin.
- B. Sparling, D. Moebius, M. D. Shair
- Chemistry, Medicine
- Journal of the American Chemical Society
- 16 January 2013
A modular, 18-step total synthesis of hyperforin is described. The natural product was quickly accessed using latent symmetry elements, whereby a group-selective, Lewis acid-catalyzed epoxide-opening… Expand
Broad-range inhibition of enterovirus replication by OSW-1, a natural compound targeting OSBP.
- L. Albulescu, J. R. Strating, +4 authors F. V. van Kuppeveld
- Biology, Medicine
- Antiviral research
- 1 May 2015
Enteroviruses, e.g., polio-, coxsackie- and rhinoviruses, constitute a large genus within the Picornaviridae family of positive-strand RNA viruses and include many important pathogens linked to a… Expand