Abstract
Legumain (LGMN; EC: 3.4.22.34), an asparaginyl endopeptidase (AEP) or asparaginyl carboxypeptidase (ACP), is a member of the C13 family of cysteine proteases. Elevated expression of LGMN is reported not only in the tumor cells of breast, prostate, and liver but also in the macrophages of the tumor microenvironment. Hence, LGMN is considered as a key protein involved in the regulation of tumor angiogenesis, invasion, and metastasis. Targeting LGMN using siRNA or pharmacological agents and peptides was reported to reduce cancer cell proliferation in vitro and shrink tumor size in vivo. Moreover, expression of LGMN is significantly low in normal cells compared to tumor cells or tumor-associated macrophages (TAMs); hence, legumain can be used as a marker for tumor recognition and targeting. Therefore, approaches inhibiting LGMN expression or activity are more viable, less toxic, and help in developing the targeted therapeutics. However, to date, LGMN targeting strategies have not been well reported. In this review, an attempt was made to summarize articles pertaining to LGMN (a) structure and activity; (b) oncogenic nature; (c) pharmacological inhibitors; and (d) targeting approaches that inhibit tumor growth. Furthermore, a list of existing gaps in LGMN research is highlighted, which needs additional studies.
Keywords: Legumain, cancers, TAMs, metastasis, targeted therapies, DNA vaccines, miRNAs.
Current Pharmaceutical Design
Title:An Overview of Targeting Legumain for Inhibiting Cancers
Volume: 27 Issue: 31
Author(s): Bandi D. Reddy, Narasimha M. Beeraka, CH. M. Kumari Chitturi and SubbaRao V. Madhunapantula*
Affiliation:
- Center of Excellence in Molecular Biology and Regenerative Medicine, Department of Biochemistry, (A DST-FIST Sponsored Department), JSS Medical College, JSS Academy of Higher Education & Research, Mysore - 570 015, Karnataka,India
Keywords: Legumain, cancers, TAMs, metastasis, targeted therapies, DNA vaccines, miRNAs.
Abstract: Legumain (LGMN; EC: 3.4.22.34), an asparaginyl endopeptidase (AEP) or asparaginyl carboxypeptidase (ACP), is a member of the C13 family of cysteine proteases. Elevated expression of LGMN is reported not only in the tumor cells of breast, prostate, and liver but also in the macrophages of the tumor microenvironment. Hence, LGMN is considered as a key protein involved in the regulation of tumor angiogenesis, invasion, and metastasis. Targeting LGMN using siRNA or pharmacological agents and peptides was reported to reduce cancer cell proliferation in vitro and shrink tumor size in vivo. Moreover, expression of LGMN is significantly low in normal cells compared to tumor cells or tumor-associated macrophages (TAMs); hence, legumain can be used as a marker for tumor recognition and targeting. Therefore, approaches inhibiting LGMN expression or activity are more viable, less toxic, and help in developing the targeted therapeutics. However, to date, LGMN targeting strategies have not been well reported. In this review, an attempt was made to summarize articles pertaining to LGMN (a) structure and activity; (b) oncogenic nature; (c) pharmacological inhibitors; and (d) targeting approaches that inhibit tumor growth. Furthermore, a list of existing gaps in LGMN research is highlighted, which needs additional studies.
Export Options
About this article
Cite this article as:
Reddy D. Bandi , Beeraka M. Narasimha, Chitturi Kumari CH. M. and Madhunapantula V. SubbaRao*, An Overview of Targeting Legumain for Inhibiting Cancers, Current Pharmaceutical Design 2021; 27 (31) . https://dx.doi.org/10.2174/1381612826666201125111625
DOI https://dx.doi.org/10.2174/1381612826666201125111625 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
Call for Papers in Thematic Issues
"Tuberculosis Prevention, Diagnosis and Drug Discovery"
The Nobel Prize-winning discoveries of Mycobacterium tuberculosis and streptomycin have enabled an appropriate diagnosis and an effective treatment of tuberculosis (TB). Since then, many newer diagnosis methods and drugs have been saving millions of lives. Despite advances in the past, TB is still a leading cause of infectious disease mortality ...read more
Current Pharmaceutical challenges in the treatment and diagnosis of neurological dysfunctions
Neurological dysfunctions (MND, ALS, MS, PD, AD, HD, ALS, Autism, OCD etc..) present significant challenges in both diagnosis and treatment, often necessitating innovative approaches and therapeutic interventions. This thematic issue aims to explore the current pharmaceutical landscape surrounding neurological disorders, shedding light on the challenges faced by researchers, clinicians, and ...read more
Emerging and re-emerging diseases
Faced with a possible endemic situation of COVID-19, the world has experienced two important phenomena, the emergence of new infectious diseases and/or the resurgence of previously eradicated infectious diseases. Furthermore, the geographic distribution of such diseases has also undergone changes. This context, in turn, may have a strong relationship with ...read more
Melanoma and Non-Melanoma Skin Cancer Treatment: Standard of Care and Recent Advances
In this thematic issue, we aim to provide a standard of care of the diagnosis and treatment of melanoma and non-melanoma skin cancer. The editor will invite authors from different countries who will write review articles of melanoma and non-melanoma skin cancers. The Diagnosis, Staging, Surgical Treatment, Non-Surgical Treatment all ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Reprofiling of Troglitazone Towards More Active and Less Toxic Derivatives: A New Hope for Cancer Treatment?
Current Topics in Medicinal Chemistry Utility and Limitations of SP600125, an Inhibitor of Stress-Responsive c-Jun N-Terminal Kinase
Current Enzyme Inhibition Lessons from the Drug Discovery of Lapatinib, a Dual ErbB1/2 Tyrosine Kinase Inhibitor
Current Topics in Medicinal Chemistry Green Chemistry Approach as a Versatile Platform for Nanoparticles with Biomedical Applications
Nanoscience & Nanotechnology-Asia Intestinal Immunomodulation. Role of Regulative Peptides and Promising Pharmacological Activities
Current Pharmaceutical Design GABA System as a Target for New Drugs
Current Medicinal Chemistry Clinical Use of Therapies Targeting Tumor Vasculature and Stroma
Current Cancer Drug Targets Regulation and Function of DNA and Histone Methylations
Current Pharmaceutical Design Versatility of Cancer Associated Fibroblasts: Commendable Targets for Anti-tumor Therapy
Current Drug Targets Mining the Dark Matter of the Cancer Proteome for Novel Biomarkers
Current Cancer Therapy Reviews GCPII Imaging and Cancer
Current Medicinal Chemistry KRAS Mutation Testing of Colorectal Cancer for Anti-EGFR Therapy: Dogmas Versus Evidence
Current Cancer Drug Targets Current Status and Future Prospects of Small–molecule Protein–protein Interaction (PPI) Inhibitors of Tumor Necrosis Factor (TNF) and Receptor Activator of NF-κB Ligand (RANKL)
Current Topics in Medicinal Chemistry Meet Our Editorial Board Member
Current Medicinal Chemistry Ecto-Nucleotidase Inhibitors: Recent Developments in Drug Discovery
Mini-Reviews in Medicinal Chemistry Fyn Kinase in Brain Diseases and Cancer: The Search for Inhibitors
Current Medicinal Chemistry DTCM-glutarimide Delays Growth and Radiosensitizes Glioblastoma
Anti-Cancer Agents in Medicinal Chemistry Chemistry in the Bioactivity of Chlorophylls: An Overview
Current Medicinal Chemistry Liposomal-All-trans-Retinoic Acid in the Treatment of Acute Promyelocytic Leukemia
Current Cancer Therapy Reviews Targeting Stem Cells-Clinical Implications for Cancer Therapy
Current Stem Cell Research & Therapy