Title:Natural Thiazoline-Based Cyclodepsipeptides from Marine Cyanobacteria: Chemistry, Bioefficiency and Clinical Aspects
Volume: 28
Issue: 38
Author(s): Rajiv Dahiya*, Sunita Dahiya, Neeraj Kumar Fuloria, Satish Jankie, Alka Agarwal, Vernon Davis, Vijaya Sahadeo, Vishal Radhay, Yashoda Ramsubhag, Wellecia Mullings, Zachary Langford, Zekiel Bedassie and Shivkanya Fuloria
Affiliation:
- School of Pharmacy, Faculty of Medical Sciences, The University of the West Indies, St. Augustine, Trinidad & Tobago,West Indies
Keywords:
Azoline-based peptide, cyanobacteria, thiazoline, cytotoxicity, total synthesis, SAR, cyclodepsipeptide.
Abstract:
Background: Peptides and peptide-based therapeutics are biomolecules that
demarcate a significant chemical space to bridge small molecules with biological therapeutics,
such as antibodies, recombinant proteins, and protein domains.
Introduction: Cyclooligopeptides and depsipeptides, particularly cyanobacteria-derived
thiazoline-based polypeptides (CTBCs), exhibit a wide array of pharmacological activities
due to their unique structural features and interesting bioactions, which furnish them
as promising leads for drug discovery.
Methods: In the present study, we comprehensively review the natural sources, distinguishing
chemistries, and pertinent bioprofiles of CTBCs. We analyze their structural peculiarities
counting the mode of actions for biological portrayals which render CTBCs as
indispensable sources for emergence of prospective peptide-based therapeutics. In this
milieu, metal organic frameworks and their biomedical applications are also briefly discussed.
To boot, the challenges, approaches, and clinical status of peptide-based therapeutics
are conferred.
Results: Based on these analyses, CTBCs can be appraised as ideal drug targets that have
always remained a challenge for traditional small molecules, like those involved in protein-
protein interactions or to be developed as potential cancer-targeting nanomaterials.
Cyclization-induced reduced conformational freedom of these cyclooligopeptides contribute
to improved metabolic stability and binding affinity to their molecular targets.
Clinical success of several cyclic peptides provokes the large library-screening and synthesis
of natural product-like cyclic peptides to address the unmet medical needs.
Conclusion: CTBCs can be considered as the most promising lead compounds for drug
discovery. Adopting the amalgamation of advanced biological and biopharmaceutical
strategies might endure these cyclopeptides to be prospective biomolecules for futuristic
therapeutic applications in the coming times.
