10 results about "Enkephalin" patented technology

Bifunctional compounds, which find utility as modulators of B-cell lymphoma 6 protein (BCL6; target protein), are described herein. In particular, the bifunctional compounds of the present disclosure contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand that binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The bifunctional compounds of the present disclosure exhibit a broad range of pharmacological activities associated with degradation / inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

The invention is applicable to the technical field of biological medicines, and provides application of thienphine in preparation of a medicine for treating premature ovarian failure. The thiephine is used in combination with the MSC. The thiephine protects endogenous opioid peptides by inhibiting NEP activity, reduces follicular atresia and improves the ovarian microenvironment. The invention analyzes and studies that Thiorphan (NPE inhibitor) can inhibit NEP activity, protect endogenous opioid peptide (such as enkephalin), reduce follicular atresia and improve ovarian microenvironment, MSC can promote follicular survival and angiogenesis through paracrine (such as VEGF and IGF-1) and immunoregulation (such as inhibition of TNF-alpha and IL-6), and the combination of Thiorphan and MSC can achieve the effect of inhibiting tumor cells through dual mechanisms of drug protection and cell repair. A new thought is provided for treating premature ovarian failure.

The present application relates to a method for synthesizing leu-enkephalin by Fmoc method, which uses Fmoc-protected amino acid as monomer, and sequentially connects amino acid to resin. In the synthesis of leu-enkephalin, all the amino acids do not have any side chain protection group. The Fmoc protection group is removed by using a solution of 1.00 mol / L imidazole and 0.02 mol / L tricyclohexylphosphine in tetrahydrofuran, and finally leu-enkephalin is obtained by removing the resin with aqueous trifluoroacetic acid. The present application first uses imidazole and tricyclohexylphosphine as components of Fmoc deprotection agent, instead of traditional pyridine. The deprotection agent is not controlled by "controlled chemicals", is cheap and easy to obtain, is stable in nature, and is low in toxicity, volatility and corrosion. The deprotection agent has excellent Fmoc removal ability, does not cause phenolic ring acylation side reaction of tyrosine side chain, does not need any side chain protection, simplifies the production process of polypeptide, reduces the preparation cost of polypeptide, and provides great improvement space for the design of synthesis strategy of polypeptide containing basic sensitive side chain protection group.

The invention provides an active peptide composition for regulating emotion and improving side effects of drugs, and relates to the technical field of active peptide compositions. The active peptide composition provided by the invention comprises an emotion regulating component and a nerve recovery promoting component, the emotion regulating component comprises theanine, gamma-aminobutyric acid (GABA), a perilla leaf extract, nano curcumin and a black pepper extract, and the components have a synergistic effect to jointly inhibit depression and central nervous system hyperexcitation and regulate emotion; the nerve recovery promoting component comprises N-acetylneuraminic acid, phosphatidylserine, brain peptide VVAVP and a perilla leaf extract, and the components cooperate with one another, so that brain recovery is promoted, anxiety is reduced, and memory is improved; the emotion regulating component and the nerve recovery promoting component cooperate with each other, the dosage of the components is optimized, depression and central nervous hyperexcitation are jointly inhibited, emotion is regulated, brain recovery is promoted, anxiety is reduced, memory is improved, the digestion and absorption effects are good, and burden on intestines and stomach is small.

The present invention provides selected dihydrobenzimidazolones which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.

The present invention relates to: an improved small molecule compound having excellent cereblon (CRBN)-binding activity and enhanced anticancer activity; and a use thereof. The compound according to the present invention can effectively act as a novel anticancer agent for the treatment of various solid cancers and blood cancers on the basis of the binding affinity to cereblon.

Described herein are compounds or conjugates of Formula II and pharmaceutically acceptable salts, solvates, or stereoisomers thereof, as well as their uses (e.g., as cereblon-binding agents or bifunctional degraders for degrading certain proteins).

The invention discloses a gene-coded opioid receptor fluorescent probe as well as a preparation method and application thereof, the opioid receptor fluorescent probe comprises fusion of a human Mu-chip receptor and a green fluorescent protein, and the amino acid sequence of the opioid receptor fluorescent probe is shown as SEQ ID NO.1. The opioid receptor fluorescent probe constructed by the invention has good membrane positioning capability, good fluorescence signal stability and specificity and large detection range; the compound shows specific response to opioid drugs and endogenous opioid peptides (such as beta-enkephalin and enkephalin) in HEK293T cells, the fluorescence intensity and the ligand concentration are dose-dependent, the compound can be blocked by an antagonist, and the compound has excellent selectivity and pharmacological characteristics. The probe constructed by the invention can be used for novel analgesic drug development, pain mechanism research and addiction behavior monitoring.

The invention relates to the technical field of biomedicine, in particular to application of methionine enkephalin in promoting liver maturation. The invention finds that the split product methionine enkephalin Met-ENK of the proenkephalin can promote the maturation of the liver, and can be directly injected in vivo or added into a culture medium for application, so that not only can the expression of embryo liver related genes be reduced, but also the expression of mature liver related genes can be increased, and the maturation of the liver can be promoted. The invention is helpful for research and application of liver organs in the aspects of disease pathology mechanism exploration, drug in-vitro screening and research and development and regenerative medicine.

The present intention relates to compound comprising the general structure P-L-J-E, wherein P is a phosphoinositide 3-kinase (PI3K) binding moiety that binds class 1 phosphoinositide 3-kinase (PI3K), L is a linker with a linker length of 12 to 21 atoms, J is a junction selected from (formula I), (formula II) and (formula III), wherein R7 is selected from H and the group consisting of -C1-C3 alkyl; E is an E3 ubiquitin ligase binding moiety that binds cereblon, J is a junction selected from (formula IV), (formula I), (formula II) and (formula III), R7 is selected from H and the group consisting of -C1-C3 alkyl; and SP is chosen in such way that the length of the linker L is 12 to 21 atoms.