18934-81-1Relevant articles and documents
Synthetic micelle sensitive to IR light via a two-photon process
Goodwin, Andrew P.,Mynar, Justin L.,Ma, Yingzhong,Fleming, Graham R.,Frechet, Jean M. J.
, p. 9952 - 9953 (2005)
A micellar assembly of molecules constituted of poly(ethylene glycol) as the hydrophilic component and 2-diazo-1,2-naphthoquinone as the hydrophobic component was shown to be destroyed in a two-photon photoreaction triggered by infrared light with release of an encapsulated fluorescent probe molecule. Copyright
Molecular recognition of histidine-tagged molecules by metal-chelating lipids monitored by fluorescence energy transfer and correlation spectroscopy
Dorn, Ingmar T.,Neumaier, Klaus R.,Tampé, Robert
, p. 2753 - 2763 (1998)
Complex binding of proteins by metal-chelating lipids via surface- exposed or protein-engineered histidines provides an universal and powerful concept for the orientation and two-dimensional crystallization of proteins at self-organized interfaces. To dem
Preparation and application of three-branch RGD modified brain glioma targeting lipid material
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Paragraph 02=021, (2021/11/03)
The invention discloses a three-branch RGD-modified glioma targeting lipid material which is used for targeted delivery of brain glioma treatment drugs. One end of the novel lipid material is connected with cholesterol extending through polyethylene glycol, and the other end of the novel lipid material is connected with RGD peptide with brain glioma targeting function, and the novel lipid material can be used for integrin receptor α which is highly expressed on the surface of brain capillary endothelial cells and brain glioma cells. v β3 The affinity between the brain glioma is achieved through the affinity between the brain glioma, and the effective concentration of the therapeutic drug to the brain tumor is improved. The novel lipid lipid material can be used for liposome. The prepared paclitaxel liposome has obvious brain targeting property and tumor targeting property, and has wide application prospects.
HDAC DEGRADER
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Page/Page column 37; 71-72, (2021/07/31)
The disclosure provides compounds of formula (I). The compounds may be used to degrade the Histone Deacetylase (HDAC) family of enzymes, particularly HDAC1, 2 and 3 that exist in corepressor complexes. Accordingly, the compounds may
PROTAC-mediated degradation of class i histone deacetylase enzymes in corepressor complexes
Adams, Grace E.,Cowley, Shaun Michael,Hodgkinson, James T.,Millard, Christopher J.,Norris, James K. S.,Schwabe, John W. R.,Smalley, Joshua P.,Song, Yun
supporting information, p. 4476 - 4479 (2020/05/13)
We have identified a proteolysis targeting chimera (PROTAC) of class I HDACs 1, 2 and 3. The most active degrader consists of a benzamide HDAC inhibitor, an alkyl linker, and the von Hippel-Lindau E3 ligand. Our PROTAC increased histone acetylation levels and compromised colon cancer HCT116 cell viability, establishing a degradation strategy as an alternative to class I HDAC inhibition.
BIVALENT TARGETED CONJUGATES
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Page/Page column 71; 72, (2020/05/28)
The invention provides conjugates that comprise a bivalent targeting moiety, a nucleic acid, and optional linking groups as well as synthetic intermediates and synthetic methods useful for preparing the conjugates, compositions comprising the bidentate targeting ligands and the conjugates, as well as methods for targeting therapeutic nucleic acids with the bidentate conjugates. The conjugates are useful to target therapeutic nucleic acids.
THERAPEUTIC METHODS
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Page/Page column 204; 243; 244-245, (2020/05/28)
The invention provides methods and compositions for delivering a nucleic acid to a cell or the cytosol of the target cell. The method includes contacting the cell with, 1) a membrane-destabilizing polymer; and 2) a nucleic acid conjugate. The nucleic acid conjugate includes a targeting ligand bound to an optional linker and a nucleic acid.
IRAK DEGRADERS AND USES THEREOF
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Paragraph 1986; 1987, (2019/07/10)
The present invention provides compounds, compositions thereof, and methods of using the same.
COMPOUNDS AND METHODS FOR OPTICAL SENSING OF ELECTRICAL ACTIVITY IN BIOLOGICAL SYSTEMS
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Paragraph 0095, (2019/08/20)
Disclosed are tethered chromophore compositions comprising a membrane-spanning tether. The compounds can include covalently tethered fluorophore-quencher combinations useful for measuring action potentials and other fast electrical events in cells and tissues.
Norbornane-based cationic antimicrobial peptidomimetics targeting the bacterial membrane
Hickey, Shane M.,Ashton, Trent D.,Boer, Gareth,Bader, Christie A.,Thomas, Michael,Elliott, Alysha G.,Schmuck, Carsten,Yu, Heidi Y.,Li, Jian,Nation, Roger L.,Cooper, Matthew A.,Plush, Sally E.,Brooks, Douglas A.,Pfeffer, Frederick M.
supporting information, p. 9 - 22 (2018/10/20)
The design, synthesis and evaluation of a small series of potent amphiphilic norbornane antibacterial agents has been performed (compound 10 MIC = 0.25 μg/mL against MRSA). Molecular modelling indicates rapid aggregation of this class of antibacterial agent prior to membrane association and insertion. Two fluorescent analogues (compound 29 with 4-amino-naphthalimide and 34 with 4-nitrobenz-2-oxa-1,3-diazole fluorophores) with good activity (MIC = 0.5 μg/mL against MRSA) were also constructed and confocal microscopy studies indicate that the primary site of interaction for this family of compounds is the bacterial membrane.
