C07K5/0215

Gamma glutamyl-valine synthase, and method for producing gamma glutamyl-valyl-glycine
10508295 · 2019-12-17 · ·

-Glu-Val synthetase suitable for generating -Glu-Val, and a method for producing -Glu-Val-Gly using the same are provided. By using -Glu-Val synthetase showing a ratio of -glutamylvaline synthetase activity to -glutamylglycine synthetase activity of 2.0 or higher, such as -Glu-Val synthetase of Kocuria rosea (AJ3132), -Glu-Val-Gly is produced from Glu, Val, and Gly as raw materials.

COMPOUND TARGETING PROSTATE SPECIFIC MEMBRANE ANTIGEN, AND PREPARATION METHOD AND APPLICATION THEREOF
20240091389 · 2024-03-21 ·

The present disclosure provides a compound targeting prostate specific membrane antigen (PSMA), wherein the compound has the following structure shown in Formula (I); R.sub.1 is a compound structure targeting prostate specific membrane antigen; L.sub.1 is (X).sub.n(CH.sub.2).sub.m(Y).sub.q, X and Y are independently selected from lysine, glutamic acid or a derivative structure containing lysine and glutamic acid, n is an integer from 0 to 12, m is an integer from 0 to 60, q is an integer from 0 to 12, and each CH.sub.2 may be individually substituted with O, NH(CO), or (CO)NH; L.sub.2 is (CH.sub.2).sub.p, p is an integer from 0 to 30, and each CH.sub.2 may be individually substituted with O, NH(CO), or (CO)NH; and R.sub.2 is a nuclide chelating group. The present disclosure also provides a radiolabeled complex based on the structure of the compound. The compound and the radiolabeled complex have appropriate blood circulation time, high uptake in tumors and long retention time, and are suitable for nuclide therapy and imaging of tumors with high expression of PSMA.

##STR00001##

Peptide having antioxidant activity and composition containing same

The present invention provides a functional peptide having excellent antioxidant activity, the peptide having excellent biocompatibility and significantly better antioxidant activity than conventional GSHs in order to overcome the limitation of the weak antioxidant activity of existing peptides. The peptide of the present invention can promote antioxidant activity or effectively repair biological tissue or cell damage caused by reactive oxygen species generated due to oxidative stress. Therefore, the peptide having such antioxidant activity effectively acts on cell damage caused by oxidative stress, and can thus be used to prevent and repair cell damage.

MACROCYCLIC COMPOUNDS AS PROTEASOME INHIBITORS

The compounds of the present invention are represented by the following compounds having Formula I and Formula (I):

##STR00001##

where the substituents R.sup.1, R.sup.2, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R, R, X, Y, and Z are as defined herein and

##STR00002##

where the substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R, R, X, Y, and Z are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.

Prodrugs of NRF2 Activating Compounds and Uses Thereof
20190367472 · 2019-12-05 ·

Aspects of the present disclosure include prodrugs of compounds that activate Nrf2. Such prodrugs find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these prodrugs, methods of using these prodrugs in the treatment of various diseases and disorders, processes for preparing these prodrugs and intermediates useful in these processes.

METHODS AND COMPOSITIONS FOR MODULATING TRANSPORT OF A DRUG
20190336564 · 2019-11-07 ·

Methods and pharmaceutical compositions for inhibiting or decreasing transport of a drug by a transporter of multidrug resistance-associated protein are provided.

Compound targeting prostate specific membrane antigen, and preparation method and application thereof

The present disclosure provides a compound targeting prostate specific membrane antigen (PSMA), wherein the compound has the following structure shown in Formula (I); R.sub.1 is a compound structure targeting prostate specific membrane antigen; L.sub.1 is -(X).sub.n-(CH.sub.2).sub.m-(Y).sub.q-, X and Y are independently selected from lysine, glutamic acid or a derivative structure containing lysine and glutamic acid, n is an integer from 0 to 12, m is an integer from 0 to 60, q is an integer from 0 to 12, and each CH.sub.2 may be individually substituted with O, NH(CO), or (CO)NH; L.sub.2 is -(CH.sub.2).sub.p-, p is an integer from 0 to 30, and each CH.sub.2 may be individually substituted with O, NH(CO), or (CO)NH; and R.sub.2 is a nuclide chelating group. The present disclosure also provides a radiolabeled complex based on the structure of the compound. The compound and the radiolabeled complex have appropriate blood circulation time, high uptake in tumors and long retention time, and are suitable for nuclide therapy and imaging of tumors with high expression of PSMA. ##STR00001##

GLUTAMINASE INHIBITORS
20190309017 · 2019-10-10 · ·

Disclosed are newly identified chemotherapeutic agents. These inhibitors are particularly useful in the treatment of cancers such as leukemic cells and pancreatic cancers.

DIPEPTIDE PIPERIDINE DERIVATIVES

The disclosure relates to pharmaceutical compositions, to methods of preparing such compositions, and to methods for using such compositions for treating or preventing a disease or condition associated with arginase activity.

Method for producing alpha-form crystal of reduced glutathione, and method for storing said crystal

The invention provides a method of efficiently and stably producing -form crystal of reduced glutathione, and a preservation method thereof. According to the invention, development of -form crystal and/or transition to -form crystal of reduced glutathione are suppressed by the coexistence of at least one kind of compound selected from the group of aliphatic amino acid, sulfur-containing amino acid, aromatic amino acid, an analogous compound and dipeptide, as a habit modifier, during production and preservation of an aqueous solution or -form crystal of reduced glutathione.