C07K5/06078

Therapeutically active compounds and their methods of use

Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.

Self-assembled peptide nanostructures

Nanostructures made up from two or more types of short peptides (e.g., aromatic dipeptides), which differ from one another by the presence (or absence) of an end-capping moiety, are disclosed. The disclosed nanostructures exhibit a closed tubular structure, short average length and narrow length distribution. Also disclosed are processes of preparing the nanostructures, articles comprising the nanostructures, and use of the nanostructures in, for example, reinforcement of materials.

NMDA antagonist prodrugs

Prodrugs of an NMDA antagonist, (S)-1-phenyl-2-(pyridin-2-yl)ethanamine, useful for the treatment of depression (particularly major depressive disorder) or pain; compositions comprising them, and methods of making them.

COMPOSITION AND METHODS OF USE OF SMALL MOLECULES AS BINDING LIGANDS FOR THE MODULATION OF PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9(PCSK9) PROTEIN ACTIVITY

This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.

BIOINSPIRED HIGHLY THERMO-SUSTAINABLE PACKINGS WITH USES THEREOF
20220041651 · 2022-02-10 ·

A thermally stable composition having at least one aromatic cyclic di-peptide is provided having a thermal sustainability of up to 680 Kelvin. The thermally stable compositions can be used in high temperature applications.

Synthesis and intermediates of pyrrolobenzodiazepine derivatives for conjugation
09745303 · 2017-08-29 · ·

A method of synthesing a compound of formula (I) from a compound of formula (III). ##STR00001##

GADD45BETA/MKK7 INHIBITOR FOR THE TREATMENT OF A RESISTANT HAEMATOLOGICAL MALIGNANCY

A Gadd45β/MKK7 inhibitor for use in a method of treating a resistant haematological malignancy, combinations of said inhibitor with a further anti-cancer agent and related methods of use.

PYRROLOBENZODIAZEPINES AND CONJUGATES THEREOF

A conjugate comprising a PBD dimer linked from the tether joining the two PBD units, wherein the linker is of formula (A1): (Formula (A1)) wherein R.sup.N1 is selected from H and C.sub.1-4 alkyl; L is a linker connected to a cell binding agent; CBA is the cell binding agent; n is an integer selected in the range of 0 to 48; Q is: (Formula (Q)), where Q.sup.x is such that Q is an amino-acid residue, a dipeptide residue or a tripeptide residue.

##STR00001##

METHOD FOR ENHANCING EXTRACELLULAR VESICLE PRODUCTION
20170233766 · 2017-08-17 ·

A method for enhancing extracellular vesicle production is described. A peptide that induces polymer formation is incubated with a cell culture which results in enhanced EV production. The peptide penetrates the cells and subsequently polymerizes upon exposure to enzymes (e.g. phosphatase) within the cell. The cells that contain the newly formed polymers have an increased production of EVs. These EVs can be harvested using centrifugation techniques.

NOVEL LINKERS
20220031858 · 2022-02-03 ·

The invention relates to novel linkers which comprise two or three basic, acidic or hydrophobic natural or non-natural amino acids. The invention also relates to drug conjugates comprising said linkers, to pharmaceutical compositions comprising said drug conjugates and to the use of said drug conjugates in preventing, suppressing or treating cancer.