Patent classifications
C07K9/003
SITE-SPECIFIC ANTIBODY CONJUGATES AND THE METHODS FOR PREPARATION OF THE SAME
The present disclosure provides a site-specific protein conjugate and the method for preparation of the same. The protein conjugate comprising a protein and an oligosaccharide, wherein said oligosaccharide comprises
##STR00001##
wherein: said GlcNAc is directly or indirectly linked to an amino acid of said protein; said Gal is a galactose; said (Fuc) is a fucose, b is 0 or 1; said Fuc* comprises a fucose or a fucose derivative linked to a molecule of interest (MOI), said protein comprises an antigen binding fragment and/or a Fc fragment.
Supramolecular glycosaminoglycans
Provided herein are glycosylated peptide amphiphiles (GPAs), supramolecular glyconanostructures assembled therefrom, and methods of use thereof. In particular, provided herein are glycosaminoglycan (GAG) mimetic peptide amphiphiles (PAs) and supramolecular GAG mimetic nanostructures assembled therefrom that mimic the biological activities of GAGs, such as heparin, heparan sulfate, hyaluronic acid etc.
CHIP SURFACE LINKER AND PREPARATION METHOD AND USE THEREFOR
The present invention relates to the field of biochips, and provides a chip surface linker and a preparation method and a use therefor. The chip surface linker is obtained by means of applying a direct current voltage to an aromatic amine bonding molecule in the presence of an acid and a nitrite to cause a reaction with a chip surface to form a bonding molecular group connected the chip surface, and then using a functional molecular for reaction and modification to add a functional molecular group containing a hydroxyl group and an ester group. The chip surface linker obtained in the present invention is able to bond more stably with a chip surface, being stable in hot water and basic conditions, and features relatively good electrical conductivity, stability during energization, and resistance to organic solvents required for nucleic acid synthesis, and is thus very advantageous for subsequent nucleic acid synthesis and other uses.
THIRD GENERATION TUBULYSIN ANALOGUES AND PROCESS OF PREPARATION THEREOF
The present disclosure relates to a third generation tubulysin analogues and process of preparation thereof. The present disclosure also relates to a method of using these third generation tubulysin analogues for treatment of various diseases including cancer.
Peptides with anti-cancer activity
The peptides of the invention are of formula (I) or (IV). The peptides of the invention are useful in the treatment of cancer.
TARGETED DEGRADATION OF THE ONCOGENIC MICRORNA 17-92 CLUSTER BY STRUCTURE-TARGETING LIGANDS
Embodiments of methods are disclosed for inhibiting, regulating and/or otherwise affecting or managing the pri-miR-17-92 cluster, and certain pre-miRNA's embedded in the cluster as well as the pre-miRNA's themselves as isolated forms, as members of a library, present in oncogenic and/or polycystic cell lines and/or that are present in breast cancer, prostate cancer and/or polycystic kidney disease in animals or humans, or present in any other disease in which the pri-miR-17-92 cluster and the certain pre-miRNAs within in it cause or contribute to disease. The methods utilize compounds that target the structural feature or features of the pri-miR-17-92 cluster and/or the certain pre-miRNA's. The pre-miRNA's are members of the pre-miRNA-X group which includes one or more of pre-miR-17, pre-miR-18a, pre-miR-19a, pre-miR-19b-1, pre-miR-20a, and pre-miR-92a-1 or any combination thereof. The compounds incorporate a dimeric formula of a binding moiety for the certain pre-miRNA-X's. The binding moiety can bind or complex with structural feature(s) of the certain pre-miRNA-X's without specificity for the particular nucleotide sequence of the structural features. The binding moiety nevertheless is selective for the certain structural feature(s) so that it does not bind with other pre-miRNA's not having the certain structural feature(s).
Third generation tubulysin analogues and process of preparation thereof
The present disclosure relates to a third generation tubulysin analogues and process of preparation thereof. The present disclosure also relates to a method of using these third generation tubulysin analogues for treatment of various diseases including cancer.
HEMIASTERLIN DERIVATIVES FOR CONJUGATION AND THERAPY
Provided herein are hemiasterlin derivatives, conjugates thereof, compositions comprising the derivatives or conjugates thereof, methods of producing the derivatives and conjugates thereof, and methods of using the derivatives, conjugates, and compositions for the treatment of cell proliferation. The derivatives, conjugates, and compositions are useful in methods of treatment and prevention of cell proliferation and cancer, methods of detection of cell proliferation and cancer, and methods of diagnosis of cell proliferation and cancer. In an embodiment, the hemiasterlin derivatives are according to Formula 1000:
##STR00001##
or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein Ar, L, W.sup.1, W.sup.4, W.sup.5, SG, and R are as described herein.
Molecular rotor-based D-amino acids as tools for imaging peptidoglycan biosynthesis
Disclosed herein are compositions for assessing peptidoglycan (PG) biosynthesis in bacteria using modified D-amino acids covalently attached to a molecular rotor and visualizing the labeled PG in bacteria based upon the enhanced fluorescence of the molecular rotor incorporated in the PG. The resultant, labeled peptidoglycan structures are amenable for identification by microscopic visualization, flow cytometry or other suitable methods.
HEMIASTERLIN DERIVATIVES FOR CONJUGATION AND THERAPY
Provided herein are hemiasterlin derivatives, conjugates thereof, compositions comprising the derivatives or conjugates thereof, methods of producing the derivatives and conjugates thereof, and methods of using the derivatives, conjugates, and compositions for the treatment of cell proliferation. The derivatives, conjugates, and compositions are useful in methods of treatment and prevention of cell proliferation and cancer, methods of detection of cell proliferation and cancer, and methods of diagnosis of cell proliferation and cancer. In an embodiment, the hemiasterlin derivatives are according to Formula 1000:
##STR00001##
or a pharmaceutically acceptable salt, solvate, or tautomer thereof, wherein Ar, L, W.sup.1, W.sup.4, W.sup.5, SG, and R are as described herein.