Recent updates on Wnt signaling modulators: a patent review (2014-2020)

被引：25
作者：
Goswami, Vishalgiri G. [1 ]
Patel, Bhumika D. [1 ]
机构：
[1] Nirma Univ, Inst Pharm, Dept Pharmaceut Chem, Ahmadabad 382481, Gujarat, India
来源：
EXPERT OPINION ON THERAPEUTIC PATENTS | 2021年 / 31卷 / 11期
关键词：
Beta-catenin; cancer; osteoarthritis; porcupine; Wnt modulators; Wnt signaling; CANCER STEM-CELLS; BETA-CATENIN; OXIDATIVE STRESS; MUTATIONS; PATHWAY; ACTIVATION; DISEASE; GROWTH; MECHANISMS; EXPRESSION;
D O I：
10.1080/13543776.2021.1940138
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Introduction: Wnt signaling is a signal transduction pathway that plays a vital role in embryonic development and normal tissue preservation. Dysfunction of it gives rise to various diseases like cancer, Alzheimer's, metabolic and skeletal disorders, kidney and liver disease, etc. Thus, targeting Wnt pathway can be a potential approach to design and develop novel therapeutic classes. Areas covered: Authors provided an overview of Wnt modulators from 2014 to 2020. Different heterocyclic scaffolds and their pharmacology from a total of 104 PCT applications have been summarized. Expert opinion: The scientific community is working extensively to bring first in the class molecule to the market which targets Wnt pathway. Lorecivivint, Wnt inhibitor, for the treatment of knee Osteoarthritis and SM-04554, Wnt activator, for the treatment of androgenetic alopecia are currently under Phase III. Other molecules, LGK-974, RXC-004, ETC-159, CGX-1321, PRI-724, CWP-232291 and BC-2059 are also under different stages of clinical development for the treatment of cancer. Antibody based Wnt modulator, OTSA101-DTPA-90Y is currently under Phase I for the treatment of Relapsed or Refractory Synovial Sarcoma while OMP-18R5 is under Phase I for Metastatic Breast Cancer. Ongoing preclinical/clinical trials will define the role of the Wnt pathway in different therapeutic areas and open new opportunities.
引用
收藏
页码：1009 / 1043
页数：35
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