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- Publications
- Influence
Selective inhibition of BET bromodomains
- P. Filippakopoulos, J. Qi, +22 authors J. Bradner
- Biology, Medicine
- Nature
- 24 September 2010
Epigenetic proteins are intently pursued targets in ligand discovery. So far, successful efforts have been limited to chromatin modifying enzymes, or so-called epigenetic ‘writers’ and ‘erasers’.… Expand
A molecular mechanism of artemisinin resistance in Plasmodium falciparum malaria
- Alassane Mbengue, Souvik Bhattacharjee, +16 authors K. Haldar
- Biology, Medicine
- Nature
- 9 April 2015
Artemisinins are the cornerstone of anti-malarial drugs. Emergence and spread of resistance to them raises risk of wiping out recent gains achieved in reducing worldwide malaria burden and threatens… Expand
Histone deacetylase inhibitor treatment dramatically reduces cholesterol accumulation in Niemann-Pick type C1 mutant human fibroblasts
- N. H. Pipalia, C. C. Cosner, +6 authors F. Maxfield
- Biology, Medicine
- Proceedings of the National Academy of Sciences
- 21 March 2011
Niemann-Pick type C (NPC) disease is predominantly caused by mutations in the NPC1 protein that affect intracellular cholesterol trafficking and cause accumulation of unesterified cholesterol and… Expand
Blueprint for antimicrobial hit discovery targeting metabolic networks
- Y. Shen, J. Liu, +7 authors Z. Oltvai
- Biology, Medicine
- Proceedings of the National Academy of Sciences
- 5 January 2010
Advances in genome analysis, network biology, and computational chemistry have the potential to revolutionize drug discovery by combining system-level identification of drug targets with the… Expand
Computational studies of the cholesterol transport between NPC2 and the N-terminal domain of NPC1 (NPC1(NTD)).
- Guillermina L Estiú, Nazir Khatri, O. Wiest
- Chemistry, Medicine
- Biochemistry
- 19 September 2013
The transport of cholesterol from NPC2 to NPC1 is essential for the maintenance of cholesterol homeostasis in late endosomes. On the basis of a rigid docking model of the crystal structures of the… Expand
Structural origin of selectivity in class II-selective histone deacetylase inhibitors.
- Guillermina L Estiú, E. Greenberg, +4 authors O. Wiest
- Chemistry, Medicine
- Journal of medicinal chemistry
- 16 April 2008
The development of class- and isoform-selective histone deacetylase (HDAC) inhibitors is highly desirable for the study of the complex interactions of these proteins central to transcription… Expand
Toward selective histone deacetylase inhibitor design: homology modeling, docking studies, and molecular dynamics simulations of human class I histone deacetylases.
- D. Wang, P. Helquist, N. L. Wiech, O. Wiest
- Chemistry, Medicine
- Journal of medicinal chemistry
- 12 October 2005
Histone deacetylases (HDACs) play an important role in gene transcription. Inhibitors of HDACs induce cell differentiation and suppress cell proliferation in tumor cells. Although many HDAC… Expand
Thiadiazole carbamates: potent inhibitors of lysosomal acid lipase and potential Niemann-Pick type C disease therapeutics.
- A. Rosenbaum, Casey C Cosner, Christopher J. Mariani, F. Maxfield, O. Wiest, P. Helquist
- Chemistry, Medicine
- Journal of medicinal chemistry
- 22 July 2010
Niemann-Pick type C (NPC) disease is a lysosomal storage disorder characterized at the cellular level by abnormal accumulation of cholesterol and other lipids in lysosomal storage organelles.… Expand
The cytoplasmic prolyl-tRNA synthetase of the malaria parasite is a dual-stage target of febrifugine and its analogs
- J. D. Herman, L. R. Pepper, +21 authors Ralph Mazitschek
- Chemistry, Biology
- Science Translational Medicine
- 1 May 2015
The cytoplasmic prolyl-tRNA synthetase of Plasmodium falciparum is a dual-stage therapeutic target for drug development. An ancient remedy for a modern scourge Malaria is a devastating disease. It is… Expand
Discovery of selective small-molecule HDAC6 inhibitor for overcoming proteasome inhibitor resistance in multiple myeloma
- T. Hideshima, J. Qi, +18 authors J. Bradner
- Biology, Medicine
- Proceedings of the National Academy of Sciences
- 31 October 2016
Significance Proteasome inhibitors show remarkable anti-multiple myeloma (MM) activity in preclinical and clinical studies. However, resistance develops in the majority of patients, and novel… Expand