Delving into the Latest Updates on WF-14861 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

CTSB x CTSL

Action

inhibitors

Mechanism

CTSB inhibitors(Cathepsin B inhibitors), CTSL inhibitors(Cathepsin L inhibitors)

Therapeutic Areas

Skin and Musculoskeletal Diseases

Active Indication-

Inactive Indication

Arthritis

Originator Organization

Fujisawa Pharmaceutical Co., Ltd.

Active Organization-

Inactive Organization

Fujisawa Pharmaceutical Co., Ltd.

License Organization-

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC20H30N4O6

InChIKeyGRBXFTOUISIXRP-ULQDDVLXSA-N

CAS Registry176777-37-0

AbstractA short enantioselective synthesis of the cathepsine inhibitor WF14861 (1) from the funghi Colletotrichum sp. as well as of its diasteroisomer 21 is presented. Comparison of the NMR data of the final products and, in particular, of the [α]D values of the intermediates allowed the confirmation of the formerly proposed structure 1. In addition, the so far unknown absolute configuration of all three stereogenic centres of WF14861 could be established by this synthesis.

01 Jan 1999·The Journal of AntibioticsQ4 · MEDICINE

WF14861, a New Cathepsins B and L Inhibitor Produced by Colletotrichum sp. I. Taxonomy, Production, Purification and Structure lucidation.

Q4 · MEDICINE

Article

Author: Otsuka, Takanao ; Hashimoto, Seiji ; Nakanishi, Tomoko ; Okamoto, Masanori ; Higaki, Tomoji ; Hatanaka, Hiroshi ; Takase, Shigehiro ; Muramatsu, Yuko ; Hino, Motohiro

WF14861, a novel cathepsins B and L inhibitor, was obtained from the culture mycelium of a fungus strain Colletotrichum sp. No. 14861. Spectroscopic analysis showed that WF14861 consisted of trans-epoxysuccinic acid, L-tyrosine and spermidine, WF14861 inhibited cathepsins B and L selectively.

01 Jan 1999·The Journal of AntibioticsQ4 · MEDICINE

WF14861, a New Cathepsins B and L Inhibitor Produced by Colletotrichum sp. II. Biological Properties.

Q4 · MEDICINE

Article

Author: Masanori Okamoto ; Yuko Muramatsu ; Motohiro Hino ; Seiji Hashimoto ; Kazuaki Niikura ; Takanao Otsuka

WF14861, 3-(N-(1-(N-(4-aminobutyl)-N-(3-aminopropyl)carbamoyl)-2-(4-hydroxyphenyl )ethyl)carbamoyl)oxirane-2-carboxylic acid, was obtained from the culture mycelium of Colletotrichum sp. as a novel cathepsins B and L inhibitor. WF14861 also showed inhibitory activities against bone derived crude protease and other cysteine proteases in vitro. The compound ameliorated the tissue damage and the bone destruction models of low-calcium-diet-fed mouse and adjuvant arthritis rat model.

100 Deals associated with WF-14861

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