Abstract: The present invention provides means and methods for functionalizing a polypeptide of interest at its C-terminus with an amino acid derivative.

Abstract: Sulfonamide-containing linkage systems for release of payload compounds from an attached targeting moiety in drug conjugates. The conjugates have the formula of [(P)-(L)]m-(T), wherein (P) is a payload compound, (L) is a linker, (T) is a targeting moiety and m is an integer from 1- to 10. Also provided are pharmaceutical compositions comprising such conjugates and there use in treating cancer.

Abstract: Described herein are antibody conjugates and methods of making antibody conjugates.

Abstract: The subject matter described herein is directed to methods of preparing certain antibody-drug conjugates (ADCs) wherein the antibody is linked to the drug through a linker, wherein the drug contains a heteroaryl group having a secondary nitrogen, and the linker is attached to the drug via the secondary nitrogen. The resulting conjugates are useful in treating various diseases and conditions.

Abstract: The invention relates to compounds of general structure (1): Q-(L1)n-(L2)o-(L3)p-(L4)q-D (1), wherein Q is a click probe; D is a cytotoxin containing an enediyne moiety; L1, L2, L3 and L4 are each individually linkers that together link Q to D; n, o, p and q are each individually 0 or 1, provided that n+o+p+q=1, 2, 3 or 4, wherein D comprises a functional moiety (21): wherein R12?C1-3-alkyl, the wavy line indicates the connection to the remainder of the cytotoxin, and wherein D is conjugated to (L4)q by replacing the amine H atom, and to conjugates obtainable by reacting the compound according to the invention with a protein comprising a click probe F capable of reacting with click probe Q in a click reaction. The invention further relates to a bioconjugate according to general structure (2): Pr-[(L6)-Z-(L1)n-(L2)o-(L3)p-(L4)q-D]xx (2), wherein Z is a connecting group that is formed in a click reaction, L6 is a linker that links Z to Pr and Pr is a (glyco)protein.

Abstract: Provided herein are poly-1-hydroxymethylethylene hydroxymethyl formal (PHF)-based drug delivery systems. Also disclosed are methods of making antibody-drug conjugates and methods of treatment using these conjugates.

Abstract: The addition of a selective, fast-acting, short half-life CDK 4/6 inhibitor in a very specific dosage regimen to the combination of chemotherapy with a checkpoint inhibitor provides superior results in the treatment of a tumor or cancer. The unexpected discovery is that the short pulsatile specifically-timed administration of a selective, fast-acting, short half-life CDK 4/6 inhibitor during administration of the chemotherapy portion of the triple combination therapy has a profound effect on the immune cells in the cancer microenvironment.

Abstract: Anti-CD8 antibodies, radiolabeled anti-CD8 antibodies, fluorescently labeled anti-CD8 antibodies and their use in imaging are provided herein. Included are methods of detecting the presence of CD8 proteins in a subject or sample.

Abstract: Provided herein are extracellular vesicle (EV) (a.k.a. exosome) compositions for specifically targeting the delivery of a therapeutic agent to particular cells and/or tissues in a subject, as well as methods of making and methods of using said compositions. The compositions and methods disclosed herein are useful for targeted drug delivery in the treatment of diseases in which a cell surface receptor is overexpressed, such as, for example, cancer.

Abstract: The present invention relates to a Fab fragment based switchable antibody system for generating site-specific antibody conjugates. Methods are described for the attachment of molecules to specific sites the Fab fragment and for the attachment of the Fab fragment to a target molecule (e.g., an antibody) directed against any desired target antigen (tumor, bacterial, fungal, viral, parasitic etc.) The attachment is via binding of the Fab fragment to an epitope linked to the target molecule.

Abstract: An antibody or antigen-binding portion thereof which binds to PSMA and comprises a heavy chain variable domain comprising the sequence given in SEQ ID NO:33, wherein SEQ ID NO:33 is: EVQLVQSGX9E X11KKPGASVKV SCKX24SGYTFT EYTIHWVX38QA X41 GKGLEWIGN INPNX55GGTTY NOKFEDRX68TX70 TVDKSTSTAY MELSSLRSED TAVYYCAAGW NFDYWGOGTT VTVSS wherein: X9 is A or P X11 is V or L X24 is A or T X38 is R or K X41 is P or H X55 is N or Q X68 is V or A; and X70 is I or L whereby the heavy chain variable domain comprises up to 3 amino acid sequence modification(s) between positions 1-30, 36-49, 67-98 and 105-115 of SEQ ID NO: 33. The invention also provides compounds that include the antibody or antigen-binding portion thereof, such as conjugates, and their use in the treatment or diagnosis of diseases, in particular cancers, particularly prostate cancer.

Abstract: The present invention provides compounds of Formula (I): a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, a solvate thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.

Abstract: Disclosed is use of NK3R antagonists for the therapeutic treatment leptin-related disease.

Abstract: Provided are conjugates including a targeting moiety that binds to a cell surface molecule of a target cell and a target cell surface-editing enzyme. Also provided are compositions and kits that include the conjugates, as well as methods of using the conjugates. Methods of making conjugates are also provided.

Abstract: The invention relates to a conjugate comprising (a) an amatoxin comprising (i) an amino acid 4 with a 6?-deoxy position; and (ii) an amino acid 8 with an S-deoxy position; (b) a BCMA-binding moiety comprising (i) the variable domains of humanized antibody J22.9-ISY, and (ii) a heavy chain constant region comprising a D265C mutation; and (c) a protease-cleavable linker linking said amatoxin and said target-binding moiety. The invention furthermore relates to a pharmaceutical composition comprising such conjugate, particularly for use in the treatment of multiple myeloma.

Abstract: The present invention relates to benzimidazole derivatives having the general formula I, wherein n is 0 or 1; X1 and X2 are independently, at each occurrence, CR5 or N; Y is C1-C6 alkylene, wherein alkylene is optionally substituted with one to two C1-C3 alkyl groups; R1 is selected from the group consisting of hydrogen, halogen, C1-C6 alkoxy, —NH2, —NHR6, —NR7R8 and —NH—(R9)n—R10, n being 0 or 1; R2 is selected from the group consisting of hydrogen, halogen, C1-C6 alkyl, —NH2, —NHR6, —NR7R8 and —NH—(R9)n—R10; R3 is selected from the group consisting of hydrogen, hydroxyl, OR11, —NR7R8, C1-C6 alkoxy, C1-C6 alkyl, C3-C10 cycloalkyl, C1-C3 haloalkyl, —C(O)NHR11, aryl, heteroaryl and heterocyclyl, wherein each of said cycloalkyl, aryl, heteroaryl and heterocyclyl is optionally and independently substituted with one to four Ra groups; and R4 is selected from the group consisting of —NH2, —N(R12)(V)pR13, —NH(V)p—OR14, —NHC(O)R15, and groups of formula 1a shown below, and their use in the treatment of diseases, in

Abstract: Provided herein is are methods of using 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-1-yl)-3-fluorobenzonitrile, or an enantiomer, a mixture of enantiomers, a tautomer, or a pharmaceutically acceptable salt thereof and a bispecific antibody specifically binding to human B cell maturation antigen (BCMA) and to human CD3? (CD3) provided herein, in treating, preventing or managing multiple myeloma.

Abstract: This disclosure provides cell surface anchoring antigen conjugates, formulations comprising cell surface anchoring antigen conjugates, and methods of using the same for treating cancer.

Abstract: The present application relates to antibodies that bind to small molecules such as cyclophosphamide, ifosfamide, and analogs thereof, and immunological assays for determining the presence and/or quantifying the amount of cyclophosphamide and/or ifosfamide in a sample. By way of example, such immunological assays can be used for environmental testing.

Abstract: A crystalline form I of a compound represented by Formula (VII-1): having characteristic peaks appearing at lattice spacing (d) of 7.34, 5.66, 5.53, 5.30, 5.02, 4.66, 4.37, 4.28, 4.06, 3.68, 3.62, 3.47, 3.36, 3.30, 3.16, 3.11, 3.03, 2.99 and 2.50 ? in the powder X-ray diffraction pattern.