Patent classifications
A61K47/645
Peptidyl inhibitors of calcineurin-NFAT interaction
Described are peptides and peptide conjugates comprising CN binding motifs (CNBM) which inhibit the CN-NFAT interaction. In some embodiments, the peptides comprise: (i) CNBM; (ii) a hydrophobic, non-peptidic moiety (RH) which interacts with the hydrophobic pocket on a CN protein; (iii) a sequence -AAU1-AAU2-AAU3-AAU4-AAU5-AAU6-, wherein each of AAU2, AAU3, AAU4, AAU5, and AAU6, is, independently, optional, and each of AAU1, AAU2, AAU3, AAU4, AAU5, and AAU6 when present is independently an amino acid as defined herein; or (iv) combinations thereof. In some embodiments, RH is conjugated to the N- or C-terminus of the CNBM. In some embodiments, the sequence -AAU1-AAU2-AAU3-AAU4-AAU5-AAU6- is conjugated to the N- or C terminus of the CNBM. In some embodiments, the peptides comprise: CNBM and RH. In some embodiments. In some embodiments, the peptides comprise: CNBM and AAU1-AAU2-AAU3-AAU4-AAU5-AAU6-. In some embodiments, the peptides of the disclosure CNBM and RH.
CANCER IMMUNOTHERAPY
Methods, compounds, compositions and kits for the treatment and/or prevention of cancer are provided. In particular, methods for the treatment of cancer comprising the administration of a TLR2 agonist, such as a conjugate of dipalmitoyl-S-glyceryl-cysteine (Pam2Cys) and polyethylene glycol (PEG), more particularly a Pam2Cys-Ser-PEG compound, and an immunostimulant such as an anti-PD-1, anti-PDL-1, anti-PL-1, or anti-CTLA-4 immunotherapeutic, are provided.
Mitochondria-Targeted Polypeptide, Preparation Method thereof, and Use thereof
Disclosed are a type of mitochondria-targeted polypeptides, the preparation method and the uses thereof. The polypeptide is abbreviated as MTP. The synthesis method of the present disclosure is simple, and the mitochondria-targeted polypeptide prepared by the method can specifically target the mitochondria of cells and are basically non-toxic to cells. In addition, these synthesized polypeptides demonstrate good cell-membrane-penetrating properties, and can conveniently undergo further multi-functional derivation and modification, thereby providing a potential delivery tool for the preparation of a mitochondria-targeted medicament.
P-boronophenylalanine derivative and composition containing same, and kit for producing said derivative and composition
The present invention pertains to: a p-boronophenylalanine derivative that comprises a polymer to which a group represented by formula (I) is linked directly or via a linker; a composition containing same; and a kit for producing said derivative and composition.
Peptide compositions and methods of use thereof for disrupting TEAD interactions
Described herein are peptides and variants and mutants thereof capable of interacting with TEAD, disrupting the HIPPO pathway, or modulating the activity or function of TEAD interactions in a cell. Pharmaceutical compositions and uses of peptides, as well as methods of designing and manufacturing such peptides, to treat cancer, tumor, or any other disease/condition associated with a dysregulated HIPPO pathway or uncontrolled cell growth are also described herein.
SELECTIVE HIGH-AFFINITY POLYDENTATE LIGANDS AND METHODS OF MAKING SUCH
This invention provides novel polydentate selective high affinity ligands (SHALs) that can be used in a variety of applications in a manner analogous to the use of antibodies. SHALs typically comprise a multiplicity of ligands that each bind different region son the target molecule. The ligands are joined directly or through a linker thereby forming a polydentate moiety that typically binds the target molecule with high selectivity and avidity.
USE OF PLL FOR IMPROVING THE STABILITY OF MOLECULES IN SOLUTION
The invention relates to a molecular complex comprising at least one polylysine conjugate (PLL), comprising a main PLL straight chain and at least one molecule F having an average molecular weight of between 50 daltons and 1000 daltons that is covalently bonded to said main chain, and at least one molecule M that is unstable in solution, the conjugate(s) and the molecule(s) M being bonded by means of a non-covalent bond. The invention also relates to a composition comprising a complex of this kind, to a method for obtaining said composition and use thereof, and to the use of one or more PLL-based conjugates for improving the hydrophilicity, the effectiveness, and the activity of a molecule that is unstable in solution, over a time period that is compatible with the use of said molecule. The invention also relates to a method for identifying a PLL-based conjugate or a combination of a plurality of PLL-based conjugates that makes it possible to improve the hydrophilicity, the effectiveness, and the activity of a molecule that is unstable in solution, and to a kit for implementing said method.
Kidney-Targeted Drug Delivery Systems
A composition including an elastin-like polypeptide (ELP) coupled to a kidney targeting peptide and. a therapeutic agent is provided. A method of delivering a therapeutic agent to a subject in need thereof comprising: administering to the subject an effective amount of a composition comprising: an elastin-like polypeptide (ELP), a kidney targeting agent coupled to the ELP and a targeting agent and/or a drug binding domain coupled to the ELP, wherein the ELP includes an amino acid sequence having at least about repeats of the amino acid sequence GVPGX (SEQ ID NO: 1), and wherein the composition enhances the deposition and retention of the therapeutic agent in the kidney relative to the non-conjugated therapeutic.
Ligand capable of multivalently binding to glutamine transporter, and composition comprising same
The present invention pertains to a ligand that contains a plurality of groups represented by formula (1) and is capable of multivalently binding to a glutamine transporter expressed in excess in a cancer cell compared to a normal cell.
SILICON BASED DRUG CONJUGATES AND METHODS OF USING SAME
Described herein are silicon based conjugates capable of delivering one or more payload moieties to a target cell or tissue. Contemplated conjugates may include a silicon-heteroatom core, one or more optional catalytic moieties, a targeting moiety that permits accumulation of the conjugate within a target cell or tissue, one or more payload moieties (e.g., a therapeutic agent or imaging agent), and two or more non-interfering moieties covalently bound to the silicon-heteroatom core.