Patent classifications
A61K49/0043
Methods to spatially profile protease activity in tissue and sections
Aspects of the disclosure relate to methods and compositions useful for in vivo and/or in vitro enzyme profiling. In some embodiments, the disclosure provides methods of in vivo enzymatic processing of exogenous molecules followed by detection of signature molecules as representative of the presence of active enzymes associated with diseases or conditions. In some embodiments, the disclosure provides compositions and in vitro methods for localization of enzymatic activity in a tissue sample.
SPECIFIC CONJUGATION LINKERS, SPECIFIC IMMUNOCONJUGATES THEREOF, METHODS OF MAKING AND USES SUCH CONJUGATES THEREOF
The present invention relates to novel linkers containing a 2,3-disubstituted succinic group, or 2-monosubstituted, or 2,3-disubstituted fumaric or maleic (trans (E)- or cis (Z)-butenedioic), or acetylenedicarboxyl group for conjugation of a cytotoxic agent, and/or one or more different functional molecules per linker to a cell-binding molecule, through bridge linking pairs of thiols on the cell-binding molecule specifically. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.
METAL-BINDING PEPTIDE, AND USE THEREOF
The present invention is intended to provide a peptide that selectively binds to a metal surface. Specifically, the present invention relates to a peptide consisting of an amino acid sequence as set forth in SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 5, SEQ ID NO: 6, SEQ ID NO: 7, or SEQ ID NO: 8, or a peptide substantially identical to the aforementioned peptide, and a method for detecting a metal surface of a medical device, using these peptides.
IN SITU SOLIDIFYING SOLUTIONS AND METHODS OF MAKING AND USING THEREOF
Described herein are fluid complex coacervates that produce solid adhesives in situ. Oppositely charged polyelectrolytes were designed to form fluid adhesive complex coacervates at ionic strengths higher than the ionic strength of the application site, but an insoluble adhesive solid or gel at the application site. When the fluid, high ionic strength adhesive complex coacervates are introduced into the lower ionic strength application site, the fluid complex coacervate is converted to a an adhesive solid or gel as the salt concentration in the complex coacervate equilibrates to the application site salt concentration. In one embodiment, the fluid complex coacervates are designed to solidify in situ at physiological ionic strength and have numerous medical applications. In other aspects, the fluid complex coacervates can be used in aqueous environment for non-medical applications.
RENAL TARGETING-TYPE DRUG DELIVERY CARRIER HAVING EXCELLENT BIODEGRABILITY
The present invention aims to provide a carrier for drug delivery that selectively accumulates in the kidney in the body, and shows high biodegradability and drug releasability in the kidney. The present invention relates to a compound in which a carbonyl group of serine is linked directly or via a linker to terminal amino group of linear polylysine, compound carrier for delivery, and a medicament for the diagnosis, prophylaxis, or treatment of a renal disease, containing the carrier for drug delivery, and a drug bound to the carrier directly or via a linker or encapsulated therein.
MESOPOROUS POLYMERIC PARTICULATE MATERIAL
A particulate material comprising porous polymeric particles is described. The porous polymeric particles have an average pore diameter of from 2 to 50 nm and a volume mean particle diameter D[4,3] of less than 100 μm. The material is obtained or obtainable by spray-drying a polymer solution. The particles find use as a solubility-enhancing carrier for active pharmaceutical compounds. Methods of manufacturing the particulate material and pharmaceutical compositions including the particulate material loaded with one or more active pharmaceutical compounds are also described.
FIBROBLAST ACTIVATION PROTEIN (FAP) TARGETED IMAGING AND THERAPY IN FIBROSIS
Excessive deposition of extracellular matrix is a hallmark of Idiopathic pulmonary fibrosis (IPF), it is advantageous to target the cells and the mechanisms associated with this process. By targeting myofibroblasts (specialized contractile fibroblasts) that are key for the development of IPF with drugs conjugated with fibroblast activation protein (FAP). this technology helps minimize the production of extracellular matrix in the lungs and provides a new treatment option for patients diagnosed with IPF.
Compositions for inhibiting 3′ repair exonuclease 2 and methods of screening for such compositions
Provided here are therapeutically effective pharmaceutical compositions containing one or more TREX2 inhibitors, and more specifically methods of administering TREX2 inhibitors to increase the effectiveness of a chemotherapeutic agent. Also provided here are methods of identifying agents that inhibit the exonuclease activity of TREX2.
NORRIN REGULATION OF PLASMALEMMA VESICLE-ASSOCIATED PROTEIN AND USE TO TREAT MACULAR DEGENERATION
A method is provided to limit inter-cellular leakage between cells in retinal or choroidal vasculature. As a result, an ocular disorder in which ocular or choroidal edema occurs based on leakage of the Adherens Junctions or Tight Junctions is readily treated. The method is particularly well-suited for usage in response to the blood-retinal barrier (BRB) compromise. A method is also provided for the reduction of plasmalemma vesicle-associated protein (PLVAP), which causes transcytosis and pinicytotic leakage. In a particular application, fluid collection under retinal pigment epithelial cells in wet macular degeneration is reduced; a condition currently without effective clinical treatments.
In situ solidifying solutions and methods of making and using thereof
Described herein are fluid complex coacervates that produce solid adhesives in situ. Oppositely charged polyelectrolytes were designed to form fluid adhesive complex coacervates at ionic strengths higher than the ionic strength of the application site, but an insoluble adhesive solid or gel at the application site. When the fluid, high ionic strength adhesive complex coacervates are introduced into the lower ionic strength application site, the fluid complex coacervate is converted to a an adhesive solid or gel as the salt concentration in the complex coacervate equilibrates to the application site salt concentration. In one embodiment, the fluid complex coacervates are designed to solidify in situ at physiological ionic strength and have numerous medical applications. In other aspects, the fluid complex coacervates can be used in aqueous environment for non-medical applications.