An aromatic amine androgen receptor (AR) and BET targeting protein degradation chimera compound is represented by formula I. Experimental results show that the compound can target and degrade both AR and BRD4, and down-regulate the expression of AR and BRD4 proteins; the compound can inhibit the proliferation of a variety of prostate cancer cells; the compound can inhibit the proliferation of a prostate cancer cell line LNCaP/AR, which overexpresses the AR, and can achieve a good inhibition effect on a prostate cancer cell line 22RV1, which is resistant to a marketed prostate cancer drug (enzalutamide). The compound also shows good metabolic stability, and has a good application prospect in the preparation of an AR and/or BET protein degradation targeting chimera, and a drug for the treatment of related diseases regulated by the AR and BET.

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The present disclosure provides antibody-drug conjugate structures, which include a cleavable linker that links the antibody to the drug and has a first enzymatically cleavable moiety and a second enzymatically cleavable moiety which includes a glycoside selected from a galactoside, a glucoside, a mannoside, a fucoside, O-GlcNAc, and O-GalNAc. The disclosure also encompasses compounds and methods for production of such conjugates, as well as methods of using the conjugates.

The present disclosure relates to certain molecules, pharmaceutical compositions containing them, and methods of using them to treat viral infections.

A compound of formula (I) wherein R.sup.L is a linker for connection to a cell binding agent.

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Provided herein are deuterated compounds and compositions useful in increasing PPARδ activity. The compounds have a formula ##STR00001##
where L.sup.5 comprises at least one deuterium. Exemplary species include ##STR00002##
The compounds and compositions provided herein are useful for the treatment of PPARδ related diseases (e.g., muscular diseases, vascular disease, demyelinating disease, and metabolic diseases).

Disclosed are protein arginine methyltransferase 5 (PRMT5) degradation/disruption compounds including a PRMT5 ligand, a degradation/disruption tag and a linker, and methods for use of such compounds in the treatment of PRMT5-mediated diseases. The PRMT5 degraders disclosed herein offer a novel mechanism for treating PRMT5-mediated diseases compared to small molecule inhibitors of PRMT5 activity.

Provided are a compound superior in a cytotoxic action on cancer cells, an action inducing degradation of BET protein in cancer cells, and an inhibitory action on the binding of BET protein and acetylated histone, and useful as an anticancer agent, a BET protein degradation inducer or a BET protein inhibitor. A compound represented by the following formula (I)

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wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof

Disclosed are proteasome inhibitors, fibroblast activation protein (FAP)-activated prodrugs of proteasome inhibitors, and pharmaceutically acceptable salts of the inhibitors and prodrugs. Also disclosed are related pharmaceutical compositions, and methods of using the inhibitors and prodrugs and compositions thereof, for example, in treating cancer or other cell proliferative diseases. In vitro and in vivo methods of quantifying the expression of FAP in a biopsy sample and a mammal, respectively, are also disclosed.

Provided herein are tripeptide epoxy ketone protease inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula (X): ##STR00001##
and pharmaceutically acceptable salts and compositions including the same. The compounds and compositions provided herein may be used, for example, in the treatment of diseases including inflammation and neurodegenerative disease.

The invention features methods and compositions for (i) controlling the amount of peptide bound to calcium phosphate particles; and (ii) for tightly binding peptide to the surface of calcium phosphate particles. The methods and compositions can be useful for preparing implants useful for promoting bone deposition at the site of implantation, and for repairing a variety of orthopedic conditions.