The methods and compositions described herein relate, in part, to the generation of a synthetic degradation system in E. coli that provides tunable control of the protein level of targeted genes by using components of the Mesoplasma florum tmRNA system. Provided herein are degradation tag variants that permit independent control of both the initial level and inducible degradation rate of attached proteins.

The invention described herein pertains to processes for preparing tubulysins and derivatives thereof. The invention described herein also pertains to processes for preparing tubulysin conjugates. The invention described herein also pertains to processes for preparing intermediates for preparing tubulysin conjugates. In one step, the alpha-thiazolyl alcohol is protected with triethylsilyl chloride in the presence of imidazole in an aprotic solvent.

A family of peptides with antioxidant and brightening activities is disclosed as well as cosmetic compositions having the peptides and cosmetic uses and methods of the peptides or cosmetic compositions.

A family of peptides with antioxidant and brightening activities is disclosed as well as cosmetic compositions having the peptides and cosmetic uses and methods of the peptides or cosmetic compositions.

The invention is directed to isomeric mixtures of cyclosporine analogs that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISA.sub.TX247, and derivatives thereof. Mixtures of ISA.sub.TX247 isomers exhibit a combination of enhanced potency and reduced toxicity over the naturally occurring and presently known cyclosporins. ISA.sub.TX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of stereoselectivity. The ratio of isomers in a mixture comprises greater than about 80 percent by weight of the E-isomer and less than about 20 percent by weight of the Z-isomer, based on the total weight of the mixture.

Eph A receptor inhibitor peptides, and particularly Eph A4 receptor inhibitor peptides, are provided. The peptides comprise a sequence derived from the G-H loop of ephrin A4. Further, pharmaceutical compositions comprising said peptides and use thereof in treating, ameliorating or preventing diseases associated with memory formation are provided.

The present invention provides a stable peptide-conjugated, ascorbic acid derivative, a method for preparing the same, and a cosmetic composition comprising the same as an active ingredient. The stable peptide-conjugated ascorbic acid derivative of the present invention has both the effect of whitening the skin by inhibiting melanin production and the effect of reducing skin wrinkles by activating collagen production, and may be used in a cosmetic composition.

The present invention relates to the use of prodrugs susceptible to nitroreductase (NTR) activation. In particular, provided herein are mitochondria-targeting prodrug compounds and probes, including profluorescent near-infrared (NIR) probes and non-fluorescent prodrugs, as well as to methods of using said prodrug compounds and probes for imaging mitochondria and for mitochondria-specific delivery of therapeutic agents.

Field of application: The invention relates to medicine and pharmacy and allows to obtain new pharmaceutical compositions based on polymyxin for the treatment of severe infectious diseases, but not possessing nephrotoxic properties in therapeutic doses. Technical result: New combined dosage forms based on the antibiotic polymyxin with low nephrotoxicity and high activity.

An activity-based nanosensor composition for detecting protease activity comprising a cleavable detectable substrate and methods of use are disclosed.