114 results about "Cyclin" patented technology

The invention relates to the technical field of biology, in particular to application of active polypeptide in maintaining dryness of umbilical cord mesenchymal stem cells. The active polypeptide disclosed by the invention is PNC-27, and the amino acid sequence of the PNC-27 is as shown in SEQ ID NO: 1. Experiments find that the PCN-27 polypeptide can effectively promote proliferation of the umbilical cord mesenchymal stem cells by regulating expression of periodic proteins Cyclin-D1 and CDK1, and can also effectively maintain dryness of the umbilical cord mesenchymal stem cells by promoting expression of dry gene Oct-4 protein in the umbilical cord mesenchymal stem cells. Experiments fully prove that the PCN-27 polypeptide can effectively maintain the dryness of the umbilical cord mesenchymal stem cells and stimulate the potential application value of the umbilical cord mesenchymal stem cells in the fields of cell culture, biomedicine and the like.

The present application provides compounds of Formula (I):or a pharmaceutically acceptable salt thereof, that are inhibitors of cyclin-dependent kinase 4 (CDK4), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.

The present invention relates to an aryl substituent-containing degradation agent for cyclin-dependent kinase 12 / 13 (CDK12 / 13), a preparation method therefor, and a pharmaceutical composition and use thereof. The degradation agent for CDK12 / 13 of the present invention has a structure represented by formula (I). The compound can be used as a protein kinase degradation agent, and can effectively and highly selectively degrade a CDK12 / 13 protein and inhibit proliferation, migration, and invasion of various tumor cells.

The present disclosure provides certain bifunctional compounds that cause degradation of Cyclin-dependent kinase 2 (CDK2) via ubiquitin proteasome pathway and are therefore useful for the treatment of diseases mediated by CDK2. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

The invention relates to compounds which inhibit Cyclin-Dependent Kinases such as CDK2 (Cyclin-Dependent Kinase 2 or Cell Division protein Kinase 2) and CDK4 (Cyclin-Dependent Kinase 4 or Cell Division protein Kinase 4), and to processes for the preparation of said compounds, pharmaceutical compositions comprising said compounds, and use of said compounds in the treatment of conditions, diseases and disorders mediated by CDK2 and / or CDK4.

The present invention relates to pharmaceutical compounds of formula (I) and pharmaceutical compositions containing said compounds, processes for the preparation of said compounds, and the use of said compounds as inhibitors of cyclin-dependent kinase 7 (CDK7), and their use in the treatment of diseases, such as cancer. [Formula 1] TIFF2023554673000617.tif33128

The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases in a subject, wherein the proliferative diseases include cancer, benign neoplasm, angiogenesis, inflammatory disease, autoinflammatory disease, and autoimmune disease, and the cancer includes leukemia, melanoma, multiple myeloma. Treatment of a subject having a proliferative disease with the compounds or compositions of the present invention can inhibit abnormal activity of cyclin-dependent kinase 7, thus inducing apoptosis and / or inhibiting transcription in the subject.

The invention relates to compounds that have been identified as CDK4 (cyclin-dependent kinase enzyme) inhibitors for the first time, for use as a medication, in particular, for the treatment of cancers e.g. those with overexpression of the enzyme CDK4, and to pharmaceutical compositions comprising same. Said compounds target the interaction interface between CDK4 and its activating cyclin, whereas those drugs already approved for the treatment of cancers with overexpression of the enzyme CDK4 target the ATP-binding site.

Disclosed herein are methods of treating cancer by administering plinabulin and a cyclin-dependent kinase inhibitor, such as abamecril, in combination.

Use of a pyrimidine-based selective cyclin-dependent kinase 2 (CDK2) of structure: (Compound I), or a pharmaceutically acceptable salt thereof or morphic form described herein for the treatment of disorders characterized by aberrant cellular division having amplified cyclin E activation and / or expression or aberrant cellular division disorders, CDK4 / 6 resistance, and / or endocrine therapy resistance, including but not limited to the treatment of tumors and cancers.

The present invention relates to pharmaceutical compounds of Formula (I) and pharmaceutical compositions comprising said compounds, methods for preparing said compounds and the use of said compounds as Cyclin-Dependent Kinase 7 (CDK7) inhibitors and their use in the treatment of diseases, such as cancer.

The application discloses a bifunctional compound and use thereof, the bifunctional compound is a bifunctional compound with K-L-S structure, wherein: K is a targeting group of cyclin 7CDK7;S is a covalent group targeting cysteine or lysine on CDK7 protein;L is a divalent linking group chemically connecting the targeting group K and the covalent group S;The bifunctional compound or does not contain divalent linking group L, and the targeting group K is directly connected with the covalent group S.The bifunctional compound or its pharmaceutically acceptable salt, ester, hydrate, solvate or stereoisomer and the pharmaceutical composition containing the same show pharmacological activity related to degradation, inhibition of target protein CDK7, and can be used for preventing and treating CDK7 related diseases or disorders.

Disclosed herein are methods and agents for the treatment and / or prevention of cyclin-dependent kinase-like 5 (CDKL5) deficiency. In particular, disclosed herein are compounds or compositions for increasing cyclin-dependent kinase-like 2 (CDKL2) in a subject, for example, in the brain of a subject, and the use of such compounds and compositions in methods for treating CDKL5 deficiency.

Disclosed is an application of a protein kinase inhibitor in preparation of a medicine for inhibiting uterine leiomyosarcoma, wherein the protein kinase inhibitor can effectively inhibit tumor growth in vitro and in vivo, and has better efficacy and safety compared with traditional chemotherapy. The protein kinase is one of the following: Wee1-like protein kinase, cyclin-dependent kinase 1, serine / threonine protein kinase 1 and serine / threonine protein kinase ATR.

This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions. The inhibitors are pyrimidine-based N-heterocyclic compounds of formula:

The present invention relates to a compound of formula (I), a compound-linker construct comprising the compound, and a conjugate comprising the compound-linker and a targeting moiety. The compound of the present invention has the ability to stimulate and / or induce, particularly induce degradation of a target protein. Such a target protein may be a protein involved in diseases, like cancer, metabolic disorder, infectious disease and / or neurological disorder, namely in particular cyclin K (CCNK) and / or CDK12 and / or CDK13. The present invention also relates to the compound, the compound-linker construct and the conjugate for use as medicament, preferably for use in treating specific diseases as disclosed herein.

This invention discloses *Bifidobacterium longum* with anti-aging functions and its applications, belonging to the field of microbial technology. The *Bifidobacterium longum* BBS 02 provided by this invention can promote cell vitality and proliferation, inhibit the high activity of β-galactosidase in senescent cells, and inhibit the high expression of the cyclin-dependent kinase inhibitor gene Cdkn1a, thereby achieving an anti-aging effect. The *Bifidobacterium longum* BBS 02 can be used to prepare edible nutrients or skin nutrients.

The present disclosure relates to a pharmaceutically acceptable salt or co-crystal of a cyclin-dependent kinase inhibitor, crystalline forms thereof and uses thereof. In particular, the present disclosure relates to a cyclin-dependent kinase inhibitor having the structure shown below.

The present invention relates to pharmaceutical compounds of Formula (I) and pharmaceutical compositions comprising said compounds, to methods for preparing said compounds and to the use of said compounds as inhibitors of cyclin-dependent kinase 7 (CDK7) and their use in the treatment of diseases, such as cancer.

This document provides pharmaceutical combinations, compositions, and methods using compounds with estrogen receptor (ER) degradation activity and cyclin-dependent kinase (CDK) inhibitors, wherein the compounds are such as compounds of formula (I) or their tautomers, stereoisomers, or mixtures of stereoisomers, or pharmaceutically acceptable salts or hydrates, wherein R1, Y, R 22 R 33 R2, p, X3, X4 and Z are defined in this paper.

The present application provides compounds of Formula (I):or a pharmaceutically acceptable salt thereof, that are inhibitors of cyclin-dependent kinase 4 (CDK4), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.

The disclosure relates to adeno-associated (AAV) particles comprising viral genomes encoding cyclin-dependent kinase-like 5 (CDKL5) proteins and peptides, compositions comprising said AAV particles, and methods for making and delivering said AAV particles to a cell or subject. The AAV particles, compositions, and methods of the present disclosure are useful for the treatment of subjects who have, have been diagnosed with having, or are at risk of having a CDKL5 deficiency disorder (CDD), developmental and epileptic encephalopathy 2, atypical Rett syndrome, and / or other CDKL5-related disorders or at least one symptom thereof.

The present disclosure relates to combinations of cyclin-dependent kinase 7 (CDK7) inhibitors and other therapeutic treatments, in particular other anti-cancer agents, and uses of such combination(s) in the treatment of cancers.

Provided herein are bifunctional compounds that bind cyclin-dependent kinase 9 (CDK9) and / or promote targeted ubiquitination for the degradation of CDK9, a protein whose dysregulation is implicated in certain cancers. Also provided are pharmaceutical compositions comprising the bifunctional compounds, methods of treating cancer, methods of promoting the degradation of CDK9 and / or IKZF1, and methods of promoting the selective degradation of CDK9 (e.g., over IKZF1) by a compound or composition described herein.

This invention discloses an oral frameshift peptide neoantigen vaccine, its preparation method, and its application, relating to the field of biomedical technology. The preparation method includes: 1) synthesizing a sea urchin-like metal-organic framework (MOF) via a hydrothermal method using zinc ions and 3,3''-dihydroxy-2',5'-dimethyl-[1,1':4',1''-terphenyl]-4,4''-dicarboxylic acid; 2) loading the sea urchin-like MOF with a frameshift peptide and a Toll-like receptor 9 agonist via electrostatic interactions and / or van der Waals forces to prepare the oral frameshift peptide neoantigen vaccine. This vaccine not only promotes antigen endocytosis and transcytosis via intestinal microfold cells by activating cyclin 42, but also alleviates immune tolerance mediated by the goblet cell-regulatory T cell immunosuppressive axis and activates specific CD8+. + T cells help prevent the development of Lynch syndrome-related colorectal cancer.

This disclosure provides certain bifunctional compounds that induce the degradation of cyclin-dependent kinase 2 (CDK2) via the ubiquitin-proteasome pathway, and are therefore intended for the treatment of CDK2-mediated diseases. Pharmaceutical compositions containing such compounds and methods for preparing such compounds are also provided.

Disclosed is a compound as shown in formula (I) or a pharmaceutically acceptable salt, a stereoisomer, an isotope derivative or a prodrug thereof. The compound has an excellent activity as a cyclin-dependent kinase 9 (CDK9) inhibitor for treating hyperproliferative diseases. The experimental research on in vitro inhibition of cell proliferation and in vivo suppression of tumors shows that such compounds have a relatively strong inhibitory effect on MV4;11 cells and in vivo tumor models, and have a good selectivity and a low toxicity and few side effects, thereby possessing a good clinical value as novel anti-tumor drugs.

The invention relates to pharmaceutical compounds of formula (I) and pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds as inhibitors of cyclin-dependent kinase 7 (CDK7) and to their use in the treatment of diseases, e.g., cancer.