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113 results about "Binding constant" patented technology

The binding constant, or association constant, is a special case of the equilibrium constant K, and is the inverse of the dissociation constant. It is associated with the binding and unbinding reaction of receptor (R) and ligand (L) molecules, which is formalized as: R + L ⇌ RL The reaction is characterized by the on-rate constant kₒₙ and the off-rate constant koff, which have units of M⁻¹ s⁻¹ and s⁻¹, respectively.

Small molecule inhibitors of autotaxin and methods of use

InactiveUS20110110886A1Inhibit and reduce and growthInhibit and reduce likelihoodHeavy metal active ingredientsBiocideDiseaseMetastatic melanoma
Autotaxin (ATX) is a prometastatic enzyme initially isolated from the conditioned media of human melanoma cells that stimulates a myriad of biological activities including angiogenesis and the promotion of cell growth, survival, and differentiation through the production of lysophosphatidic acid (LPA). ATX increases the aggressiveness and invasiveness of transformed cells, and ATX levels directly correlate with tumor stage and grade in several human malignancies. To study the role of ATX in the pathogenesis of malignant melanoma, we developed antibodies and small molecule inhibitors against recombinant human protein. Immunohistochemistry of paraffin embedded human tissue demonstrates that ATX levels are markedly increased in human primary and metastatic melanoma relative to benign nevi. Chemical screens identified several small molecule inhibitors with binding constants ranging from nanomolar to low micromolar. Cell migration and invasion assays with melanoma cell lines demonstrate that ATX markedly stimulates melanoma cell migration and invasion, an effect suppressed by ATX inhibitors. The migratory phenotype can be rescued by the addition of ATX's enzymatic product, LPA, confirming that the observed inhibition is linked to suppression of LPA production by ATX. Chemical analogues of the inhibitors demonstrate structure activity relationships important for ATX inhibition and indicate pathways for their optimization. These studies suggest that ATX is an approachable molecular target for the rational design of chemotherapeutic agents directed against human malignancies driven by the ATX/LPA axis, especially including malignant melanoma, among numerous others including breast and ovarian cancers.
Owner:YALE UNIV

Preparation method of supramolecular quadruple hydrogen-bond ureido-pyrimidinone (UPy) unit modified polyvinyl chloride (PVC) special resin

The invention relates to a preparation method of supramolecular quadruple hydrogen-bond ureido-pyrimidinone (UPy) unit modified polyvinyl chloride (PVC) special resin. UPy-containing acrylate crosslinking agents are used for modifying PVC, and UPy-containing styrene crosslinking agents are used for modifying the PVC. Compared with the existing crosslinking agents, the crosslinking agents selectedfor use in the method have the beneficial effects that UPy quadruple hydrogen-bond system can form a self-complementary quadruple hydrogen-bond interaction, and is good in stability, strong in self-polymerization ability and very high in binding constant; furthermore, the strong non-covalent cross-linking effect is reversible and has a self-recovery ability; high molecular polymers are formed by means of self-assembly through the interaction of non-covalent hydrogen bonds; the combination of repeating units is based on the interaction of the hydrogen bonds, so that the repeating units can be separated and recombined under appropriate conditions and are reversible; therefore, the PVC polymer not only has the properties of the traditional polymers, but also has the excellent characteristicsof stimulative responsibility, self-repairing property, easy processing and the like, and can be used as special resin for smart materials and self-healing materials.
Owner:XINJIANG INST OF ENG

Hyperpolarization <129>Xe switch type magnetic resonance molecular probe for identifying diamine oxidase

The invention belongs to the technical field of biochemical analysis and particularly relates to a hyperpolarization <129>Xe switch type magnetic resonance molecular probe for identifying diamine oxidase. The hyperpolarization <129>Xe switch type magnetic resonance molecular probe comprises cucurbit[6]uril and putrescine hydrochloride. The principle of the molecular probe is characterized in thata substrate (putrescine hydrochloride) with high cucurbit[6]uril binding force is converted by diamine oxidase into a product (1-pyrroline) which does not combine with cucurbit[6]uril; before enzymatic reaction, a <129>Xe hyperpolarization chemical exchange saturation transfer signal in the cucurbit[6]uril is inhibited by strong cucurbit[6]uril conjugate until the enzymatic reaction oxidizes the substrate into the product; due to the fact that the binding constant of putrescine hydrochloride@cucurbit[6]uril is several magnitude orders larger than that of <129>Xe@cucurbit[6]uril and (1-pyrroline)@cucurbit[6]uril cannot combine, the <129>Xe hyperpolarization chemical exchange saturation transfer signal in the cucurbit[6]uril appears after the enzymatic reaction through enhanced <129>Xe cucurbit[6]uril interaction, and diamine oxidase identification is achieved through the <129>Xe hyperpolarization chemical exchange saturation transfer signal in the cucurbit[6]uril.
Owner:WUHAN INST OF PHYSICS & MATHEMATICS CHINESE ACADEMY OF SCI

Tea geometrid odorant binding protein-based plant attractant screening method

The invention discloses a tea geometrid odorant binding protein-based plant attractant screening method and belongs to the technical field of bioengineering. The tea geometrid odorant binding protein-based plant attractant screening method comprises the following processes of collecting tea geometrid antenna total RNA, acquiring total length of a tea geometrid odorant binding protein by RT-PCR, constructing a prokaryotic expression vector of the tea geometrid odorant binding protein, inducing the expression of the recombinant tea geometrid odorant binding protein by IPTG, carrying out the purification of the recombinant tea geometrid odorant binding protein by nickel sepharose gel affinity column, acquiring a binding reaction spectrum of the recombinant tea geometrid odorant binding protein and tea leaf smell volatiles by a competitive fluorescent combination method, and determining that the tea leaf smell volatile reducing relative fluorescence intensity of 1-NPN to less than 50% and having the binding constant of 13-45 micromoles per liter is the plant attractant of tea geometrid. The tea geometrid odorant binding protein-based plant attractant screening method provides a novel means for screening and designing a formula of a plant tea geometrid smell information attractant.
Owner:HANGZHOU ACAD OF AGRI SCI +1

Compound and preparation method, fluorescent dye and fluorescent probe thereof

The invention provides a compound. The compound is shown in a formula (I), wherein R1 and R2 are selected from H or groups shown in a formula (II) independently, and at least one of the R1 and R2 is agroup selected from the formula (II); R3 is selected from groups consisting of H, F, Cl, Br, OH, OCH3, N(CH3)2 or C1-C6 alkyl groups, and R4 is selected from the C1-C6 alkyl groups. Compared with anexisting embedded fluorescent probe, since a fluorescent probe provided by the invention is provided with a large electron conjugated system and a large plane, the fluorescence emission intensity of the molecule of the fluorescent probe can be influenced by the intensity of a charge transfer effect in the molecule of the fluorescent probe, and when the fluorescent probe combines with G-quadruplexRNA specifically, the flexibility of rotary intramolecular double bonds is limited, so that the effect of intramolecular charge transfer is enhanced, and thus the fluorescence intensity is increased;the fluorescent probe provided by the invention has no biological toxicity, no phototoxicity and no fluorescence quenching, meanwhile, the solubility in water and the cellular permeability are greatlyimproved, and the fluorescent probe has a high binding constant in detection and an extremely low limit of detection.
Owner:GUANGDONG UNIV OF TECH
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