131 results about "Peptide modification" patented technology

The disclosed invention relates to methods of modifying peptide compositions to increase stability and delivery efficiency. Specifically, the disclosed invention relates to methods to increase the stability and delivery efficiency of protein kinase C (PKC) modulatory peptide compositions. A “therapeutic peptide composition” comprises a “carrier peptide” and a “cargo peptide.” A “carrier peptide” is a peptide or amino acid sequence within a peptide that facilitates the cellular uptake of the therapeutic peptide composition. The “cargo peptide” is a PKC modulatory peptide. Peptide modifications to either the carrier peptide, the cargo peptide, or both, which are described herein increase the stability and delivery efficiency of therapeutic peptide compositions by reducing disulfide bond exchange, physical stability, reducing proteolytic degradation, and increasing efficiency of cellular uptake.

A method is disclosed for data-dependent neutral loss analysis of biomolecules and other materials in a hybrid mass spectrometer. Candidate product ions are selected by identifying peaks in a MS/MS spectrum acquired in a first mass analyzer that exhibit a specified nominal neutral loss value, which may be representative of the mass of a peptide modification, such as phosphate. High mass accuracy MS and MS/MS spectra acquired at a second mass analyzer, such as an FTICR or Orbitrap, are processed to determine if the mass difference between a candidate product ion and its corresponding precursor matches an accurate neutral loss value. In one embodiment, MS³ analysis is performed only on the candidate product ions that satisfy the accurate mass neutral loss value test.

The invention provides application of novel glucagon peptide 1 fatty acid modified or unmodified dimer different in configuration in pancreas protection or hypoglycemic effect during treatment of II-type diabetes. The dimer is formed by connecting two identical GLP-1 monomers containing cysteine through disulfide bond formed by cysteine oxidation. Hypoglycemic duration of GLP-1 dimer is remarkablyprolonged without lowering activity of H-shaped GLP-1 homodimer (the disulfide bond is formed inside peptide chain), in-vivo continuous activity of GLP-1 analogue dimer can last for 19d while in-vivoactivity of liraglutide which is positive control drug is 3d, or in-vivo activity duration is remarkably prolonged when compared with long-acting GLP1 similar peptide which has already been reportedat present, so that technical progress of long-acting GLP1 drug is greatly promoted while convenience is brought to clinical application and popularization of the same. U-shaped homodimer (the disulfide bond is formed at the terminal C of the peptide chain) does not have impact on blood glucose but can obviously protect exocrine portion cells like pancreatic acini and catheters, thereby having a pancreas protecting function.

The invention relates to preparation and application of a nano-micelle imaging agent for a cervical cancer sentinel node. A nanometer imaging agent high polymer PEG-PLGA is used as a carrier, micelleparticles are formed through polymerization, indocyanine green is loaded inside, TMTP1 targeting peptide is modified on the surface of a micelle, and maleic amide connected with a surface hydrophilicgroup PEG end of the micelle is connected with a sulfhydryl group of TMTP1 with ring formation by amido bonds at the head and the tail. The near infrared fluorescence nano-micelle diagnosis reagent provided by the invention can image the cervical cancer sentinel node in real time, can distinguish whether tumor cell metastasis occurs or not, and offers the assistance for the imaging diagnosis of intraoperative lymph nodes of cervical cancer in clinic in the future and the guidance of individualized treatment of tumor patients.

The invention discloses a self-assembly polypeptide d-RADA16-RGD and a preparation method and application thereof. A polypeptide sequence is Ac-(Arg-Ala-Asp-Ala-Arg-Ala-Asp-Ala)2-Gly-Gly-Arg-Gly-Asp-Ser-CONH2. The self-assembly polypeptide d-RADA16-RGD is modified by a functional motif (FM) RGD and is obtained through the synthesis of amino acids, and a formed three dimensional stent has good histocompatibility and biological activity. The self-assembly polypeptide can serve as a carrier for slowly releasing growth factors and medicines, and the functional motif, such as the RGD, is also applied to short peptide modification, and the bone inductivity and osteogenic capability can be significantly improved. The preparation method is simple, convenient to operate and good in bone repair effect, has an important promoting role on bone repair and can be widely applied to clinical bone defect diseases.

The invention discloses an application of a transdermal peptide modified pueraria thomsonii exosome nano preparation in preparation of an anti-skin aging product. The pueraria thomsonii exosome nano preparation modified by the transdermal peptide can effectively penetrate through the cuticle of the skin and is efficiently taken by skin cells such as skin fibroblasts, so that the obvious function of resisting skin (cell) aging is exerted, and a new strategy is provided for skin aging resistance; The transdermal peptide modified pueraria thomsonii exosome can be used as a novel skin anti-aging beauty product which is efficient, safe and convenient to prepare, can also be applied to aging resistance of other cells and tissues, and is used for delaying aging and function decline of body tissues and organs; therefore, great market development prospects are realized in the fields of medical products and beauty cosmetics.

The invention discloses a preparation method and application of a targeting peptide modified traditional Chinese medicine multi-component exosome-like fusion nanoparticle, the nanoparticle is mainly formed by fusing a functionalized liposome and an exosome, the functionalized liposome is mainly composed of a targeted peptide, phospholipid and a traditional Chinese medicine fat-soluble active drug, the exosome is loaded with a traditional Chinese medicine water-soluble active medicine. The preparation method of the fusion nanoparticles comprises a polyethylene glycol induction method, a repeated freezing and thawing method, an extrusion method, an ultrasonication method and an incubation method. The preparation process is simple, the condition is mild, the cost is low, and the prepared nanoparticles have the advantages of various drug loading types, high penetrability, biological targeting regulation, therapeutic mechanism complementation, biological safety and the like. According to the nano-drug delivery platform, co-delivery, combined administration and collaborative precise treatment of multiple components of traditional Chinese medicine can be achieved, collaborative targeted treatment of complex progressive diseases such as tumors and neurodegenerative diseases can be achieved, and the nano-drug delivery platform has good application prospects.

The invention discloses 1-(4-isopropyl propyl)-beta-carboline-3-formyl-Trp-Trp-Trp-Lys-Glu structured as follows, a preparation method therefor, a nanostructure thereof, antitumor action thereof, action thereof in resisting adhesion and invasion and migration of tumor cells, and illustrates application thereof in medical science. The formula is shown in the description.

The invention discloses a preparation method and application of a high-density RGD peptide modified material. The preparation method comprises the following steps: dispersing a material, modified in the way that the surface is provided with an active group, into methylbenzene, adding a catalytic amount of 4-dimethylamino-pyridine, and slowly dropwise adding triethylamine and 2-bromoisobutyryl bromide under ice-bath, so as to prepare an initiator; adding cuprous bromide, 2,2'-dipyridyl and poly(ethylene glycol) methyl ether methacrylate into the initiator, so as to obtain a macromolecular polymer; adding the macromolecular polymer into a dimethylformamide solution containing an activating agent and 4-dimethylamino-pyridine to obtain an activated polymer brush, and adding RGD peptide for performing reaction in the dark at the room temperature for 18 hours; transferring a cell into the RGD peptide modified polymer brush, and performing reaction on a shaking table at the temperature of 4 DEG C for 20 minutes by adopting a phosphate buffer solution as a suspension liquid, so as to obtain the high-density RGD peptide modified material. The method is moderate in reaction conditions, simple, convenient and feasible in procedures, and achieves the purpose of fixing a cell on the surface of a solid material with high concentration and high density.

The invention belongs to the technical field of a tumor targeting deliverying and slow release administration system. The invention relates to a bufalin-loaded valine-arginine-glycine-aspartic acid-glutamic acid cyclopeptide (cRGD)-modified poly(oligo(ethylene glycol)methacrylate)-polycaprolactone (Ph PCL b P(OEGMA co RGD) bufalin) nanometer particle and a preparation method thereof. Ph-PCL-b-P(OEGMA-co-GMA) as a base material is modified through cRGD to form Ph-PCL-b-P(OEGMA-co-RGD) and bufalin is wrapped by micelle of the Ph-PCL-b-P(OEGMA-co-RGD) so that (Ph PCL b P(OEGMA co RGD) bufalin) nanometer particles are prepared. The nanometer preparation can effectively reduce toxic or side effect of bufalin and improve water solubility and tumor targeting ability. The bufalin is slowly released along with material degradation so that long-term treatment effects are obtained.

The invention discloses a preparation method of an adriamycin-dipeptide compound. Dipeptide or polypeptide containing proline residue is connected to amino of the adriamycin by the acylation through the technique of peptide modification; the toxicity of the adriamycin can be reduced and at the same time the pro-drug can release the adriamycin under the action of tumor interstitial cells so as to ensure that the adriamycin can enrich around tumor tissue to improve the selectivity of the adriamycin to the tumor tissue. The preparation method of the invention has the advantages of fast reaction rate, short term, relatively high productive rate and purity.

The invention provides an adriamycin-carrying lipid nanoscale ultrasound contrast agent targeting tumor-related fibroblasts and a preparation method of the adriamycin-carrying lipid nanoscale ultrasound contrast agent. The surface of the contrast agent is modified by a high affinity ligand (FH short peptide) for specifically expressing a TNC protein by the tumor-related fibroblasts, the FH short peptide is used as a targeting ligand, lipid is used as a shell membrane material, and adriamycin and gaseous fluorocarbon are wrapped inside the shell membrane. The targeted ultrasound contrast agentis in nanoscale, has ultrasound imaging capability, can be used for targeted delivery of drugs into the tumor-related fibroblasts, and specifically kills the tumor-related fibroblasts, and a tumor treatment effect is achieved through intervention on a tumor microenvironment.

The present invention relates to peptide modifier compounds of Formula (1), or a salt thereof, wherein: a is an integer from 1 to 10, more preferably from 1 to 3; b is an integer from 0 to 7; Z is a terminal group and Y is a bivalent group. Further aspects of the invention relate to intermediates in the preparation of compounds of Formula (1), and the use of compounds of Formula 1 in the synthesis of peptide derivatives.

The invention discloses KRGD peptide-modified carbolino-hexahydropyrazine-1,4-diketones, which are three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD peptide and are shown in the general formula I. In the general formula I, R represents Lys-Arg-Gly-Asp-Val, Lys-Arg-Gly-Asp-Phe or Lys-Arg-Gly-Asp-Ser. The invention also discloses heterocyclic nucleuses of the novel conjugates, wherein R represents OH. The invention also discloses a preparation method and in-vitro anti-platelet aggregation effects of the novel conjugates, and also discloses an antithrombotic use of the novel conjugates in a rat thrombus formation model. A result shows that the three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and RGD peptide (wherein R represents Lys-Arg-Gly-Asp-Val, Lys-Arg-Gly-Asp-Phe or Lys-Arg-Gly-Asp-Ser) and their heterocyclic nucleuses (wherein R represents OH) have good antithrombotic activity and clear application prospects in antithrombotic agent preparation.

The invention relates to a specific peptide modified colorimetric sensor and a making method thereof. The colorimetric sensor is used for detecting copper ions. The sensor uses a gold-mercapto key to make the surface of gold nanoparticles to be modified by a specific peptide, the addition of copper ions to be measured changes the conformation of the specific polypeptide from alpha-helix to beta-folding, and the gold nanoparticles mutually aggregate by using beta-folding fragments formed by the surface modification specific polypeptide in order to change the absorbance of a solution and generate color difference. The copper ions are detected by the gold nanoparticles modified by the specific peptide for the first time, and the colorimetric sensor of the gold nanoparticles modified by the specific polypeptide has very high sensitivity, simplicity and specificity on the copper ions, has a wide detection range, has potential application values in the detection of the content of the copper ions in drinking water, serum, rivers, sewage and other solutions, and also has the advantages of convenient operation, high sensitivity and wide application prospect.

A method of selectively arraying ferritin and inorganic particles on a silicon oxide substrate having a chromium, niobium or tungsten portion. An aspect of the method includes steps of: preparing a solution which contains ferritin modified at an N-terminal part of a subunit with a peptide set out in SEQ ID NO: 1, and a nonionic surfactant; and a binding step of bringing the solution in contact with the silicon oxide substrate to selectively array peptide-modified ferritin to the chromium, niobium or, tungsten portion. Another aspect of the method includes selectively arraying ferritin modified with the peptide set out in SEQ ID NO: 1, and the inorganic particles contained in ferritin at the chromium, niobium, or tungsten portion by removing the solution.

The invention discloses arg-gly-asp (RGD)-fused porcine circovirus 2 (PCV2) virus-like particles (VLPs), an infectious clone and a preparation method of the RGD-fused PCV2 VLPs, and application of theRGD-fused PCV2 VLPs and the infectious clone. According to the RGD-fused PCV2 VLPs, RGD oligopeptides are fused on PCV2 Cap proteins. According to the RGD-fused PCV2 VLPs, the PCV2 Cap proteins are subjected to RGD polypeptide sequence oligopeptide modification, the RGD oligopeptides are fused on the PCV2 Cap proteins, and the PCV2 VLPs with RGD-fused on the surfaces are assembled in vitro. Compared with wild PCV2 VLPs, the levels of PCV2 specific IgM and IgG antibodies generated by RGD-fused PCV2 VLP immune mice are significantly increased, high-titer PCV2 antibodies can be generated in an induced mode, and the RGD-fused PCV2 VLPs enhance humoral immunity response. The RGD-fused PCV2 VLPs can be applied to development of enhanced VLPs and differential diagnosis molecular label VLPs vaccines, and a new idea is provided for research and development of PCV2 vaccines.

The invention provides a mesenchymal stem cell exosome agent based on a DNA tetrahedron, a preparation method and application of the mesenchymal stem cell exosome agent. The exosome preparation is an exosome agent Exo-TDN which is obtained by loading a DNA tetrahedral nano material on the surface of a mesenchymal stem cell exosome; or the exosome agent is an exosome preparation PCM-Exo-TDN which is obtained by loading a DNA tetrahedral nano material on a mesenchymal stem cell exosome and modifying a myocardial specific targeting peptide PCM on the surface of the exosome through a cross-linking agent phospholipid polyethylene glycol maleimide. Exo-TDN is mainly enriched in a liver area, the chemotherapeutic drug DOX can be captured by the Exo-TDN when reaching the liver, the DOX is inhibited from entering a cell nucleus, and the function of protecting cells is achieved; a myocardial specific targeting peptide PCM is further modified, and PCM-Exo-TDN is synthesized and used for relieving myocardial damage caused by DOX.

The invention discloses TRGD peptide-modified carbolino-hexahydropyrazine-1,4-diketones, which are three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and TRGD peptide and are shown in the general formula I. In the general formula I, R represents Thr-Arg-Gly-Asp-Val, Thr-Arg-Gly-Asp-Phe or Thr-Arg-Gly-Asp-Ser. The invention also discloses heterocyclic nucleuses of the novel conjugates, wherein R represents OH. The invention also discloses a preparation method and in-vitro anti-platelet aggregation effects of the novel conjugates, and also discloses an antithrombotic use of the novel conjugates in a rat thrombus formation model. A result shows that the three novel conjugates of carbolino-hexahydropyrazine-1,4-diketone and TRGD peptide (wherein R represents Thr-Arg-Gly-Asp-Val, Thr-Arg-Gly-Asp-Phe or Thr-Arg-Gly-Asp-Ser) and their heterocyclic nucleuses (wherein R represents OH) have good antithrombotic activity and clear application prospects in antithrombotic agent preparation.

The invention discloses an elastin-like polypeptide temperature-responsive nano-material, and a preparation method and application thereof. The nano-material disclosed by the invention is a material prepared by modifying a nanoparticle with an elastin-like polypeptide. The elastin-like polypeptide has responsiveness to a tumor microenvironment and is A1) or A2), wherein A1) refers to a protein with an amino acid sequence as shown in a sequence 1 in a sequence table, A2) refers to a protein which is obtained by inserting a cysteine residue or a polypeptide containing the cysteine residue into the amino acid sequence of a protein P and has same functions, and the protein P is prepared by subjecting a polypeptide as shown in site 17 to 21 in the sequence 1 to repetition 30 to 100 times. The nanoparticle has surface plasmon resonance effect and is a gold nanoparticle, silver nanoparticle, platinum nanoparticle or gold-silver nanoparticle. Experimental results show that the nano-material provided by the invention has a high photothermal conversion rate and good tumor inhibitory effect and can be used for treating tumors.