- Photoswitched cell adhesion on surfaces with RGD peptides
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Coating of surfaces by RGD peptides is well-known. Herein we describe the possibility to switch cell adhesion properties by changing the distance and orientation of the RGD peptides to the surface. A set of RGD peptides of the type cyclo(-RGDfK-) was synt
- Auernheimer, Joerg,Dahmen, Claudia,Hersel, Ulrich,Bausch, Andreas,Kessler, Horst
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- Effect of Association on Nucleophilic Addition of (Meth)acrylic Aminoamides to Acrylic Acids in Aqueous Solutions
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Reactions of nucleophilic addition of N-(3-dimethylaminoalkyl)(meth)acrylamides to acrylic, N-acryloylaminoacetic, and 2-acrylamido-2-methylpropanesulfonic acid with the formation of betaines revealed an unusual dependence of the initial rate and equilibrium conversion on concentration of the reagents. The observed effects were explained by structural features of the reagents and the products.
- Kazantsev,Baruta,Kamorin,Shirshin,Sivokhin
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- COMPOSITIONS AND METHODS FOR INHIBITING PROTEIN EMBRYONIC ECTODERM DEVELOPMENT ACTIVITY AND TREATING DISEASE
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The invention provides compounds that are inhibitors of the protein embryonic ectoderm development (EED), pharmaceutical compositions, their use in modulating the activity of EED, and their use in the treatment of medical disorders, such as cancer. The invention further provides methods of treating medical disorders, such as cancer, and covalently modifying and/or modulating the activity of EED, using an agent that reacts with, and forms a covalent bond to, cysteine324 of EED.
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Paragraph 0897
(2021/10/02)
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- COVALENT TARGETING OF E3 LIGASES
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Disclosed herein, inter alia, are compositions and methods for targeting E3 ligases. In an aspect is a targeted protein degrader including 1) a targeted protein binder and 2) an E3 Ubiquitin ligase binder, wherein the E3 Ubiquitin ligase is human RNF4 or human RNF114. In an aspect is provided a pharmaceutical composition including a compound as described herein, including embodiments, and a pharmaceutically acceptable excipient.
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Paragraph 0591; 0608; 0700; 0732
(2020/05/19)
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- FREE-STANDING NON-FOULING POLYMERS, THEIR COMPOSITIONS, AND RELATED MONOMERS
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Free-standing non-fouling polymers and polymeric compositions, monomers and macromonomers for making the polymers and polymeric compositions, objects made from the polymers and polymeric compositions, and methods for making and using the polymers and polymeric compositions.
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Page/Page column 42
(2017/01/23)
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- Poly(n-acryl amino acids): A new class of biologically active polyanions
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Poly(N-acryl amino acids) bearing side groups with a lipophilic character or having charged functional groups (i.e. -NH2, -COOH, -SH, -OH, and phenols) were synthesized from the radical polymerization of N-acryl amino acid monomers. Monomers were prepared from the reaction of acryloyl chloride and amino acid esters in dry solvents. Polymers of a broad molecular weight ranging from 3 000 to 60 000 Da were obtained. The polymers were optically active, and their structures were confirmed by 1H NMR and IR spectra and elemental analysis. Hydroxyl-containing polymers were sulfated in high conversion yields by SO3/pyridine complex. The newly synthesized linear homopolyanions were tested for heparin-like activities: (i) inhibition of heparanase enzyme, (ii) release of basic fibroblast growth factor (bFGF) from the extracellular matrix (ECM), and (iii) inhibition of smooth muscle cell (SMC) proliferation. Polymers based on tyrosine and leucine were highly active in all three tests (microgram level). Polymers based on phenylalanine, tert-leucine, and proline were active as heparanase inhibitors and FGF release, and polymers of trans-hydroxyproline, glycine, and serine were active only as heparanase inhibitors. The polymer of cis-hydroxyproline was inactive. It was found that a net anionic charge (i.e. carboxylic acid) is essential for biological activity. Thus, methyl ester derivatives of the active polymers, zwitterionic amino acid pendent groups (lysine, histidine), and decarboxylated amino acids (tyramine, ethanolamine) were inactive. The above active polymers did not exhibit anticoagulation activity which is considered the main limitation of heparin and heparinomimetics for clinical use. These synthetic poly(N-acryl amino acids) may have potential use in the inhibition of heparanase-mediated degradation of basement membranes associated with tumor metastasis, inflammation, and autoimmunity.
- Bentolila, Alfonso,Vlodavsky, Israel,Ishai-Michaeli, Rivka,Kovalchuk, Olga,Haloun, Christine,Domb, Abraham J.
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p. 2591 - 2600
(2007/10/03)
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- Water soluble polymers containing amino acid residues for dental restoratives
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Glass ionomer cements for dental restoratives with improved physical properties are produced by the present invention. Acryloyl and methacryloyl derivatives of amino acids are used in the invention to copolymerize with acrylic acid, methacrylic acid or various acrylic acid-comonomer mixtures to produce water soluble polycarboxylic acids.
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- Immune-stimulating and cancerostatic 1-acyl-2-cyanoaziridines
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1-Acyl-2-cyanoaziridines of the formula STR1 wherein R is an acyl radical of a carboxylic, sulphonic, sulphinic, sulphenic, phosphonic or phosphoric acid, exhibit immune-stimulating and cancerostatic activities.
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