Abstract: Provided herein is a dolastatin 10 analog, useful for preparing conjugates thereof with targeting, diagnostic, imaging and other moieties. Also provided are the conjugates and uses thereof.

Abstract: Provided herein is a drug delivery (DD) system for ratiometric luminescence determination of drug release degree in drug delivery monitoring, which includes a drug, a switchable reporter and non-switchable reporter providing two distinguishable signals for detection; or a single switchable reporter providing two distinguishable signals for detection, and a cleavable linker connecting a drug to a switchable reporter, as well as a method for ratiometric luminescence determination of drug release in a target (in vivo or in vitro), which is effected by administering the DD system provided herein that is capable of releasing a drug from the DD system, measuring two luminescent signals provided by the switchable reporter and the non-switchable reporter, or the single switchable reporter, determining the ratio between these two luminescence signals, and determining the drug release degree through the ratio between the two luminescence signals.

Abstract: A molecular structure comprising a single-stranded hyaluronic acid moiety, and a plurality of releasable cannabidiol moieties attached thereto is provided herein, as well as uses and methods of treating a skin conditions using the same.

Abstract: A molecular structure comprising a targeting moiety, a multi-functional peptide platform and a plurality of controllably released bioactive agents attached thereto is provided herein.

Abstract: Provided herein is a class of anti-cancer conjugates designed to cross the blood-brain barrier (BBB) and thereby deliver a methylation agent into cancerous tumor cells, wherein the conjugate comprises a BBB-shuttle moiety that allows the conjugate to cross the BBB, and at least two methylation moieties of the methyltriazene type attached thereto for effecting DNA methylation in the cancerous cells. Also provided are uses of the conjugates in the treatment of brain cancer.

Abstract: Provided herein is a conjugate comprising two residues of structurally and/or mechanistically different anticancer bioactive agents, coupled to one another by a biocleavable linking moiety, as well as methods of treating cancer using the same and pharmaceutical compositions comprising the same.

Abstract: A molecular structure comprising a targeting moiety, a multi-functional peptide platform and a plurality of controllably released bioactive agents attached thereto is provided herein.

Abstract: A molecular structure comprising a targeting moiety, a multi-functional peptide platform and a plurality of controllably released bioactive agents attached thereto is provided herein.

Abstract: Provided herein is a conjugate comprising two residues of structurally and/or mechanistically different anticancer bioactive agents, coupled to one another by a biocleavable linking moiety, as well as methods of treating cancer using the same and pharmaceutical compositions comprising the same.

Abstract: A multifunctional molecular platform is provided, for covalent binding of two or more therapeutic or diagnostic agents, and for their sequential release in a biological environment near desired target sites. The platform is used in the preparation of pharmaceutical compositions for treating abnormal cell proliferation, infections, and inflammation.

Abstract: A molecular structure comprising a targeting moiety, a multi-functional peptide platform and a plurality of controllably released bioactive agents attached thereto is provided herein.

Abstract: A multifunctional molecular platform is provided, for covalent binding of two or more therapeutic or diagnostic agents, and for their sequential release in a biological environment near desired target sites. The platform is used in the preparation of pharmaceutical compositions for treating abnormal cell proliferation, infections, and inflammation.

Abstract: N-substituted 9-aminoacridine and bis-acridino derivatives containing electron-withdrawing groups (EWG) or electron-donating groups (EDG), including amino acid residues, and one-pot methods for their synthesis are disclosed. The derivatives are potential candidates for cancer treatment.

Abstract: Disclosed are heterocyclic scaffolds useful, for example, for solid-phase organic synthesis of combinatorial libraries and methods for the preparation thereof. Also disclosed are libraries, including combinatorial libraries, and methods for preparation thereof.

Abstract: A multifunctional molecular platform is provided, for covalent binding of two or more therapeutic or diagnostic agents, and for their sequential release in a biological environment near desired target sites. The platform is used in the preparation of pharmaceutical compositions for treating abnormal cell proliferation, infections, and inflammation.

Abstract: Methods of use of pharmaceutical compositions and novel peptides which are conformationally constrained backbone cyclized somatostatin analogs, having somatostatin receptor subtype selectivity, are disclosed. These patterns or receptor subtype selectivity provide compounds having improved therapeutic utility. Methods for synthesizing the somatostatin analogs and for screening of the somatostatin analogs are also disclosed. Furthermore, pharmaceutical compositions comprising somatostatin analogs are disclosed.

Abstract: Novel peptides which are conformationally constrained backbone cyclized somatostatin analogs, having somatostatin receptor subtype selectivity are disclosed. These patterns or receptor subtype selectivity provide compounds having improved therapeutic utility. Methods for synthesizing the somatostatin analogs and for screening of the somatostatin analogs are also disclosed. Furthermore, pharmaceutical compositions comprising somatostatin analogs, and methods of using such compositions are disclosed.

Abstract: Methods of use of pharmaceutical compositions and novel peptides which are conformationally constrained backbone cyclized somatostatin analogs, having somatostatin receptor subtype selectivity, are disclosed. These patterns or receptor subtype selectivity provide compounds having improved therapeutic utility. Methods for synthesizing the somatostatin analogs and for screening of the somatostatin analogs are also disclosed. Furthermore, pharmaceutical compositions comprising somatostatin analogs are disclosed.

Abstract: Novel peptides which are conformationally constrained backbone cyclized somatostatin analogs, having somatostatin receptor subtype selectivity are disclosed. These patterns or receptor subtype selectivity provide compounds having improved therapeutic utility. Methods for synthesizing the somatostatin analogs and for screening of the somatostatin analogs are also disclosed. Furthermore, pharmaceutical compositions comprising somatostatin analogs, and methods of using such compositions are disclosed.

Abstract: Novel peptides which are conformationally constrained backbone cyclized somatostatin analogs. Methods for synthesizing the somatostatin analogs and for producing libraries of the somatostatin analogs are also disclosed. Furthermore, pharmaceutical compositions comprising somatostatin analogs, and methods of using such compositions are disclosed.