- In Silico Fragment-Based Design Identifies Subfamily B1 Metallo-β-lactamase Inhibitors
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Zinc ion-dependent β-lactamases (MBLs) catalyze the hydrolysis of almost all β-lactam antibiotics and resist the action of clinically available β-lactamase inhibitors. We report how application of in silico fragment-based molecular design employing thiol-
- Cain, Ricky,Brem, Jürgen,Zollman, David,McDonough, Michael A.,Johnson, Rachel M.,Spencer, James,Makena, Anne,Abboud, Martine I.,Cahill, Samuel,Lee, Sook Y.,McHugh, Peter J.,Schofield, Christopher J.,Fishwick, Colin W. G.
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Read Online
- For detecting glutathione fluorescence probe and its preparation method and application
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The invention provides a fluorescence probe for detecting glutathione. The structural formula of the fluorescence probe is as shown in the specification. A preparation process and an aftertreatment process are relatively simple, selectivity is good, sensi
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- Novel amphiphilic PEG-hydroxycamptothecin conjugates as glutathione-responsive prodrug nanocapsules for cancer chemotherapy
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A series of novel hydroxycamptothecin (HCPT) conjugates (13a–14d), which contained a polyethylene glycol moiety and disulfide bond, were designed and synthesized in five to six steps, with overall yields of 20–39%. The anticancer activities and toxicities of these new conjugates were evaluated using an in vitro MTT assay in K562, HepG2, and HT-29 cell lines and HUVECs. The conjugates displayed enhanced antitumor activity and reduced toxicity in comparison with their parent molecule, HCPT. Among these conjugates, compound 13a exhibited 100-fold better selectivity to the tumor cells than to HUVECs. TEM and DLS experiments demonstrated that 13a formed nanosized micelles with a diameter of approximately 200?nm in aqueous solution and that the conjugate could undergo glutathione-responsive degradation to release HCPT at the tumor site. The improved potency and reduced toxicity of these conjugates may be caused by the enhanced permeation and retention (EPR) effect of nanoparticles.
- Guo, Na,Hao, Tiantian,Shang, Xiuzhuan,Zhang, Tianle,Liu, Huan,Zhang, Qian,Wang, Jing,Jiang, Du,Rong, Yao,Teng, Yuou,Yu, Peng
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- Reactive sulfhydryl compound probe and preparation method thereof
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The invention discloses a reactive sulfhydryl compound probe and a preparation method of the probe. A sensing molecule releases a rhodamine dye molecule monomer based on a thiol participated disulfide bond cleavage reaction, the fluorescence intensity is significantly improved, an obvious color change is accompanied, and selected interfering ions and the like almost have no influence on a detection effect, so that specific recognition response to a sulfhydryl compound is realized, and a detection limit reaches 0.124 micrometers.
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- NOVEL COMPOUNDS
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Novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR? provided by the present invention.
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- Targeted and armed oncolytic adenovirus via chemoselective modification
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Oncolytic adenoviruses (Ads) are an emerging alternative therapy for cancer; however, clinical trial have not yet demonstrated sufficient efficacy. When oncolytic Ads are used in combination with taxoids a synergistic increase in both cytotoxicity and viral replication is observed. In order to generate a next generation oncolytic adenovirus, virion were physically conjugated to a highly potent taxoid, SB-T-1214, and a folate targeting motif. Conjugation was enabled via the metabolic incorporation of non-canonical monosaccharides (O-GlcNAz) and amino acids (homopropargylglycine), which served as sites for chemoselective modification.
- Banerjee, Partha S.,Zuniga, Edison S.,Ojima, Iwao,Carrico, Isaac S.
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p. 4985 - 4988
(2011/10/09)
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- Mechanism-based tumor-targeting drug delivery system. Validation of efficient vitamin receptor-mediated endocytosis and drug release
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An efficient mechanism-based tumor-targeting drug delivery system, based on tumor-specific vitamin-receptor mediated endocytosis, has been developed. The tumor-targeting drug delivery system is a conjugate of a tumor-targeting molecule (biotin: vitamin H
- Chen, Shuyi,Zhao, Xianrui,Chen, Jingyi,Chen, Jin,Kuznetsova, Larisa,Wong, Stanislaus S.,Ojima, Iwao
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scheme or table
p. 979 - 987
(2011/02/22)
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- A general and efficient approach to aryl thiols: Cul-catalyzed coupling of aryl iodides with sulfur and subsequent reduction
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A Cul-catalyzed coupling reaction of aryl iodides and sulfur powder takes place in the presence of K2CO3 at 90 °C. The coupling mixture is directly treated with NaBH4 or triphenylphosphine to afford aryl thiols in good to
- Jiang, Yongwen,Qin, Yuxia,Xie, Siwei,Zhang, Xiaojing,Dong, Jinhua,Ma, Dawei
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supporting information; scheme or table
p. 5250 - 5253
(2009/12/28)
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- Drug conjugates
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A compound having the formula Y-A-Z, wherein: A is a 5, 6, or 7 member ring that is monocyclic or is fused to 1 to 3 additional 4 to 8 member rings; wherein ring A and, independently, the fused additional rings are carbocyclic or heterocyclic, and saturat
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Page/Page column 9
(2008/06/13)
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