- Degrasyn exhibits antibiotic activity against multi-resistant: Staphylococcus aureus by modifying several essential cysteines
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Degrasyn inhibits deubiquitination enzymes and has anti-cancer activity. We here show that it also exhibits antimicrobial activity against multi-resistant Staphylococcus aureus. Structure activity relationship studies demonstrate an important role of the
- Hacker, Stephan M.,Le, Philipp,Lee, Kyu Myung,Sieber, Stephan A.
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- COMPOSITIONS AND METHODS OF DELIVERY OF DEUBIQUITINASE INHIBITORS
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Described herein are compositions comprising deubiquitinase inhibitors in combination with albumin, methods of making such compositions, and methods of using such compositions in the treatment of conditions, diseases, or disorders that would benefit from
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Paragraph 00348
(2015/12/17)
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- Degrasyn-like symmetrical compounds: Possible therapeutic agents for multiple myeloma (MM-I)
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A series of degrasyn-like symmetrical compounds have been designed, synthesized, and screened against B cell malignancy (multiple myeloma, mantle cell lymphoma) cell lines. The lead compounds T5165804 and CP2005 showed higher nanomolar potency against the
- Peng, Zhenghong,Maxwell, David S.,Sun, Duoli,Bhanu Prasad, Basvoju A.,Schuber Jr., Paul T.,Pal, Ashutosh,Ying, Yunming,Han, Dongmei,Gao, Liwei,Wang, Shimei,Levitzki, Alexander,Kapuria, Vaibhav,Talpaz, Moshe,Young, Matthew,Showalter, Hollis D.,Donato, Nicholas J.,Bornmann, William G.
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p. 1450 - 1458
(2014/03/21)
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- Deubiquitinase Inhibitors and Methods for Use of the Same
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Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of
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Page/Page column 33-34
(2012/04/05)
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- Tyrphostin-like compounds with ubiquitin modulatory activity as possible therapeutic agents for multiple myeloma
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With the goal of developing small molecules as novel regulators of signal transduction and apoptosis, a series of tyrphostin-like compounds were synthesized and screened for their activity against MM-1 (multiple myeloma) cells and other cell lines representing this malignancy. Synthesis was completed in solution-phase initially and then adopted to solid-phase for generating a more diverse set of compounds. A positive correlation was noted between compounds capable of inducing apoptosis and their modulation of protein ubiquitination. Further analysis suggested that ubiquitin modulation occurs through inhibition of cellular deubiquitinase activity. Bulky groups on the sidechain near the α,β-unsaturated ketone caused a complete loss of activity, whereas cyclization on the opposite side was tolerated. Theoretical calculations at the B3LYP/LACV3P** level were completed on each molecule, and the resulting molecular orbitals and Fukui reactivity values for Cβ carbon were utilized in developing a model to explain the compound activity.
- Peng, Zhenghong,Pal, Ashutosh,Han, Dongmei,Wang, Shimei,Maxwell, David,Levitzki, Alexander,Talpaz, Moshe,Donato, Nicholas J.,Bornmann, William
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experimental part
p. 7194 - 7204
(2012/01/06)
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