Patent classifications
C07K5/123
Proteasome inhibitors
Unique compounds useful for inhibiting a proteasome in a cell, pharmaceutical compositions and methods of their use are provided herein.
Cyclic RGD peptide and method for preparing the same
A method for preparing a cyclopeptide and a cyclopeptide preparing by the method are disclosed. The method includes the following steps: (A) providing compounds represented by the following formulas (I-1) and (I-2): ##STR00001## wherein, G, R.sub.a, R.sub.b, R.sub.c, R.sub.d, and R.sub.e are defined in the specification; (B) performing a reaction between the compounds of formulas (I-1) and (I-2) to obtain a compound represented by the following formula (I-3): ##STR00002##
and (C) performing a cyclization reaction of the compound of formula (I-3) with a catalyst of formula (II) and deprotection to obtain a compound represented by the following formula (III): ##STR00003## wherein, G′, Q, M, L.sup.1, L.sup.2, m, y, and z are defined in the specification.
CONTROLLED-RELEASE FERTILIZER COMPRISING OXIDIZED GLUTATHIONE
A controlled-release fertilizer includes oxidized glutathione and a release control agent, and a method produces the controlled-release fertilizer.
SOLID PHASE SYNTHESIS OF CYCLIC AMINO ACID MOLECULES
The present invention relates to cyclic amino acid molecules and methods of preparing the same, and in particular the macrocyclization of amino acids or linear peptides bound to a solid support.
SYNTHETIC CYCLIC PEPTIDES AND METHODS OF PREPARATION AND USE THEREOF
The present invention relates, in part, to novel compounds comprising 4-imidazolidinone-fused cyclic peptides and compositions thereof. The present invention also relates to methods of generating said compounds and compositions thereof as well as methods of inhibiting protein-protein interaction using said compounds or compositions thereof. In another aspect, the present invention relates, in part, to methods of treating or preventing a various diseases or disorders using said compounds or compositions thereof.
Method of monomerisation of recombinant antibody molecules
The present invention provides method of increasing the percentage of monomer in a composition of recombinantly expressed antibody molecules characterised in that the antibody molecule comprises at least one Fv with specificity for an antigen of interest comprising one VH and one VL wherein said VH and VL are connected directly or indirectly via one or more linkers and are stabilised by a disulfide bond therebetween, said method comprises: a) a conversion step of treating the composition with a denaturant selected from urea and/or Guanidine hydrochloride; b) wherein step a) is performed in the presence of a reducing agent or after treatment with a reducing agent.
PROTEASOME INHIBITORS
Unique compounds useful for inhibiting a proteasome in a cell, pharmaceutical compositions and methods of their use are provided herein.
CYCLOPEPTIDE AND METHOD FOR PREPARING THE SAME
A method for preparing a cyclopeptide and a cyclopeptide preparing by the method are disclosed. The method includes the following steps: (a) providing compounds represented by formulas (I-1) and (I-4); (b) performing a reaction between the compounds of formulas (I-1) and (I-4) to obtain a compound represented by formula (I-5); (c) performing a reaction between the compound of formula (I-5) and the compound represented by formula (I-6) to obtain a compound represented by formula (I-7); (d) performing a cyclization reaction of the compound of formula (I-7) with a catalyst of formula (II) and deprotection to obtain a compound represented by formula (III), wherein the compounds of formulas (I-1), (I-4) to (I-7), (III) and the catalyst of formula (II) are as defined in the specification.
Multifunction cyclic peptide polymer nanomaterials
Disclosed herein is a cyclic peptide polymer. R.sup.1, R.sup.2, and R.sup.3 are organic groups. Each R.sup.4 is a covalent bond, methylene, ethylene, n-propylene, or n-butylene. Each X is —NH—, —O—, or —O—CO—. The values m and n are nonnegative integers having a sum of at least 1. The value p is an integer greater than 1. The cyclic peptide polymer may be made by providing a first cyclic peptide monomer having a protecting group on the X group, covalently binding the —CO—OH group of the first cyclic peptide monomer to a solid support having a carboxylic acid-reactive group, converting the protecting group to —XH, reacting the —XH group with the —CO—OH group of an additional cyclic peptide monomer, optionally repeating the converting and reacting steps with further additional cyclic peptide monomers, and cleaving the cyclic peptide polymer from the solid support. ##STR00001##
PROTEASOME INHIBITORS
Unique compounds useful for inhibiting a proteasome in a cell, pharmaceutical compositions and methods of their use are provided herein.