Patent classifications
A61K47/557
Antibodies and Fc fusion protein modifications with enhanced persistence or pharmacokinetic stability in vivo and methods of use thereof
In certain embodiments, this present invention provides antibodies and Fc fusion proteins with enhanced pharmacokinetics, such as biotinylated antibodies or biotinylated Fc fusion polypeptides.
Covalent modification of biological macromolecules
The present disclosure provides a method of covalently modifying a biological macromolecule, the method comprising subjecting a reaction mixture comprising: (a) a biological macromolecule comprising one or more thiol groups; and (b) a molecule comprising one or more olefin or alkyne moieties to a radical reaction under conditions sufficient to produce the covalently modified biological macromolecule. The present disclosure also provides a method of covalently modifying a biological macromolecule, the method comprising subjecting a reaction mixture comprising: (a) a molecule comprising one or more thiol groups; and (b) a biological macromolecule comprising one or more olefin or alkyne moieties to a radical reaction under conditions sufficient to produce the covalently modified biological macromolecule. The present disclosure further provides a covalently modified biological macromolecule prepared by any of the disclosed methods. The covalently modified biological macromolecules may be further crosslinked to form a scaffold.
Binding compound and uses thereof
Described are compounds for targeting proteases, e.g. serine proteases and their use in the diagnostic methods and methods for treatment of respiratory diseases such as cystic fibrosis. The compounds have the structure [H]—[B]-[A]; wherein [H] is a hydrophilic group, [B] is a subsite recognition group and [A] is a binding group; wherein A has the formula: —C(0)—CH.sub.2—NR.sup.1—COOR.sup.2 and wherein [B] has the structure: (i) —[CO—CH.sub.2—NR.sup.3]m-, or (ii) -[AA1-AA2]- or (iii) -(AA1-C0-CH.sub.2NR.sup.3)— or (iv) —(CO—CH.sub.2—NR.sup.3-AA1)- or (v) —(C0—CH.sub.2—NR.sup.4-AA1-AA3)-.
Polyoxazoline antibody drug conjugates
In the present disclosure, polymer conjugates, including polymer-antibody-drug conjugates (polymer ADCs) are described, as well as the use of such conjugates to treat human disease. The polymer conjugates can contain a large number of polymer-bound agents, thus effectively increasing the drug antibody ration (DAR) of the antibody significantly beyond the currently available technology. This may be of particular importance when antibodies to low density antigens are used as target antibodies. The described polymer-ADCs have improved pharmacokinetics and solubility relative to traditional ADCs. The linker between agent and the polymer can be tailored to provide release of toxin at the desired site and under the desired conditions within the tumor. An additional feature of the polymer-ADCs of the current disclosure is that a purification moiety can be attached to the polymer backbone to provide ease of purification of the polymer-ADCs.
COMPOSITIONS FOR RADIOTHERAPY AND USES THEREOF
Provided herein are kits, compositions, and methods for treatment of a disease, disorder, or condition, such as a proliferative disease, disorder, or condition. One aspect provides a composition including a radioisotope, a gelatin matrix and bovine collagen or a thixotropic gel. Another aspect provides methods for treating a disease, disorder, or condition.
AZIDE INSULIN ANALOGUES
The present invention relates to insulin analogues and processes of making such insulin analogues by direct conversion of a free amine to an azide via diazo-transfer with an azotransfer agent.
CATIONIC NANOSTRUCTURES FOR INTRA-CARTILAGE DELIVERY OF THERAPEUTICS AND CONTRAST AGENTS
The present invention provides a platform for the delivery of small molecule drugs or contrast agents to joints and other soft tissues. The platform enables penetration of the drug through the full thickness of cartilage and long intra-cartilage residence time by leveraging electrostatic interactions between the cationic platform and the anionic cartilage matrix. Described herein are compounds and complexes that fit this platform. Also provided are methods of treating a joint disease with the compounds and complexes of the invention, and methods of imaging joints and other soft tissue.
COMPOSITIONS AND METHODS FOR INHIBITING CARP-1 BINDING TO NEMO
Described herein are compositions and methods for treating cancer in a subject. The compositions include selective NF-κB inhibitor inhibitors. The methods include inhibiting the binding of CARP-1 with NEMO.
COMPOSITION FOR TARGETING CANCER CELL, COMPRISING STRAIN EXPRESSING MONOMERIC STREPTAVIDIN, AND BIOTINYLATED COMPOUND
The present invention relates to host cells expressing monomeric streptavidin. The host cells according to the present invention may express streptavidin in vivo, making it possible to visualize and monitor in real time the biodistribution of cancer tissue, pre-targeted by the host cell, with a biotinylated diagnostic agent, as well as to increase the cancer-targeting efficiency of biotinylated anticancer drugs.
BISPECIFIC ANTI-HAPTEN/ANTI-BLOOD BRAIN BARRIER RECEPTOR ANTIBODIES, COMPLEXES THEREOF AND THEIR USE AS BLOOD BRAIN BARRIER SHUTTLES
Herein is reported a bispecific antibody comprising a first binding specificity that specifically binds to a haptenylated payload and a second binding specificity that specifically binds to a blood brain barrier receptor.