摘要:
The present disclosure provides compounds of Formula I and a process of preparing the compounds of Formula I. The present disclosure further provides a compound of Formula II, Formula III, and Formula IV. The present disclosure provides compounds of Formula I that are capable of modifying cell-cell interactions, cell-pathogen interactions, or cell-extracellular matrix interactions, and methods thereof.
摘要:
The present invention related to microRNA (miR) signatures also called DNA damage sensitive miRs (DDSMs) which responds to the levels of DNA damage. The present invention provides method for identification of DDSMs which are upregulated by a common transcription factor (CDX2). Further, the present invention also provides miR inhibitors along with nanoparticle or hydrogel or adenoviral based delivery system for administering the same and kits comprising the same. The microRNA (miR) signature of the present invention can be used as biological markers to detect earliest stages of cancers particularly colon cancers. The present invention also provides a method of treatment of other types of cancer and related diseases.
摘要:
The present invention provides a novel compound of formula I, its derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for modulating GSK3 level (e.g., GSK3 (e.g., GSK3a/GSK3b or GSK3P) or CK1) hence, activity.
摘要:
The present invention describes methods and compositions for treating viral diseases through novel combinational therapy of one or more anti-viral and anti-kinase drugs. The composition and method of the present invention are aimed at targeting a NiRAN domain of RNA dependent RNA polymerase (RdRp) as RdRp is key enzyme for virus replication of the viral pathogens. The compositions of the present invention comprise one or more kinase inhibitors in combination with one or more anti-viral agents. The combination therapy of these agents was found to exhibit synergistic effecta in inhibiting viral activity against several lethal viruses including but not limited to SARS-CoV-2.
摘要:
A supramolecular insulin assembly and supramolecular exendin-4 assembly, which is useful as a protein therapeutic agent for the treatment of metabolic disorders particularly diabetes. The supramolecular assemblies disclosed in the present invention consists of insoluble and aggregated oligomers the protein. The invention also provides pharmaceutical compositions comprising the supramolecular assembly.
摘要:
The present invention provides a novel method of generating knock down models by electroporation of shRNA construct into the testis. The present invention provides an ethically superior, non-surgical, user friendly rapid method for the generation of permanent lines of shRNA knock down non human vertebrates. This invention is ethically superior as it does not involve any loss of animal life and drastically minimizes the production time and use of animals. Current techniques for making knockout models are cumbersome, require trained personnel, costly infrastructure and require hundreds of eggs collected after killing several females. In contrast, this method neither involves any costly infrastructure nor requires trained personnel. The invention also relates to the quick incorporation of shRNA gene construct into the germline of a species so that shRNA is inheritable. The present invention also generates in a single go a variety of knock down models differentially expressing gene specific shRNA, depending on differential shRNA gene incorporation in native genome of various male germ cells, so that there is no restriction in the choice of the gene knock down.
摘要:
Transthyretin (TTR), a tetrameric thyroxine (T4) carrier protein, is associated with a variety of amyloid diseases. Derivative of biphenyl ethers (BPE), which are shown to interact with a high affinity to its T4 binding site thereby preventing its aggregation and fibrillogenesis. They prevent fibrillogenesis by stabilizing the tetrameric ground state of transthyretin. Two compounds (2-(5-mercapto-[1,3,4]oxadiazol-2-yl)-phenol and 2,3,6-trichloro-N-(4H-[1,2,4]triazol-3-yl) exhibit the ability to arrest TTR amyloidosis. The dissociation constants for the binding of BPEs and compound 11 and 12 to TTR correlate with their efficacies of inhibiting amyloidosis. They also have the ability to inhibit the elongation of intermediate fibrils as well as show nearly complete (>90%) disruption of the preformed fibrils. Biphenyl ethers and compounds 11 and 12 as very potent inhibitors of TTR fibrillization and inducible cytotoxicity.
摘要:
The present disclosure relates to a novel enzymatic approach according to the invention using an unprecedented sortase-catalyzed transpeptidation reaction between a substrate comprising LPXTG peptide motif and biomolecules such as aminosugars, hydroxyamino acids, hydroxyamino acid esters, aminolipids, polyamines; nucleic acids or derivatives thereof, or any molecule having such moieties; or any compound having such moieties to obtain a bioconjugates useful for target delivery of a compound. The present disclosure provides bioconjugates obtained by the novel sortase catalysed transpeptidedation reaction.
摘要:
The present invention relates to synthetic catalytic DNA molecules or DNAzymes which specifically cleave the RNA sequences of the Japanese Encephalitis Viral genome and is useful in treating Japanese Encephalitis infection. The DNAzyme comprises of a chemical modification, a catalytic domain and two hybridizing arms. The DNAzymes are 29-45 nucleotides in length. The 3′ end of the DNAzyme is tethered to a poly-(G)10 tail (SEQ ID NO: 46) and the molecule comprises of at least one chemical modification. The chemical modifications are in the form of sugar modification, nucleic acid base modification, and/or phosphate backbone modification. The catalytic DNA molecule inhibits JEV replication in vitro in cultured cells and in vivo in the mouse brain. The present invention also relates to the method of treatment of Japanese encephalitis comprising the steps of introducing the catalytic DNA molecule or DNAzyme into the infected cells under conditions suitable for cleavage and reduction of viral titres.
摘要翻译:本发明涉及特异性切割日本脑炎病毒基因组的RNA序列的合成催化DNA分子或DNA酶,可用于治疗日本脑炎感染。 DNAzyme由化学修饰,催化结构域和两个杂交臂组成。 DNA酶长度为29-45个核苷酸。 DNA酶的3'端连接到聚(G)10尾(SEQ ID NO:46),并且分子包含至少一种化学修饰。 化学修饰是糖修饰,核酸碱基修饰和/或磷酸酯骨架修饰的形式。 催化DNA分子在培养细胞中体外抑制JEV复制,并在小鼠脑中体内抑制。 本发明还涉及治疗日本脑炎的方法,包括以下步骤:在适合于切割和还原病毒滴度的条件下将催化DNA分子或DNA酶引入感染的细胞中。
摘要:
This invention relates to a method of combatting cancer which cancer releases chorionic gonadotropin or a subunit thereof present in a mammal which method comprises administering to said animal an anti-cancer effective amount of a birth-control vaccine or an antibody to said chorionic gonadotropin or subunit thereof. Birth-control vaccines which are polyvalent vaccines and birth-control vaccines which employ recombinant organisms incorporating sequences coding for reproductive hormones are of particular interest as well as polyclonal and monoclonal antibodies to the chorionic gonadotropin.