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 Pages 7887 - 7909 ( 23 )
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.
Azoline-based peptide, cyanobacteria, thiazoline, cytotoxicity, total synthesis, SAR, cyclodepsipeptide.
School of Pharmacy, Faculty of Medical Sciences, The University of the West Indies, St. Augustine, Trinidad & Tobago, Department of Pharmaceutical Sciences, School of Pharmacy, University of Puerto Rico, Medical Sciences Campus, San Juan, Puerto Rico, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, AIMST University, Semeling, Bedong, Kedah, School of Pharmacy, Faculty of Medical Sciences, The University of the West Indies, St. Augustine, Trinidad & Tobago, Department of Pharmaceutical Chemistry, U.S. Ostwal Institute of Pharmacy, Mangalwad, Chittorgarh, Rajasthan, School of Medicine, Faculty of Medical Sciences, The University of the West Indies, St. Augustine, Trinidad and Tobago, School of Medicine, Faculty of Medical Sciences, The University of the West Indies, St. Augustine, Trinidad and Tobago, School of Medicine, Faculty of Medical Sciences, The University of the West Indies, St. Augustine, Trinidad and Tobago, School of Medicine, Faculty of Medical Sciences, The University of the West Indies, St. Augustine, Trinidad and Tobago, School of Medicine, Faculty of Medical Sciences, The University of the West Indies, St. Augustine, Trinidad and Tobago, School of Medicine, Faculty of Medical Sciences, The University of the West Indies, St. Augustine, Trinidad and Tobago, School of Medicine, Faculty of Medical Sciences, The University of the West Indies, St. Augustine, Trinidad and Tobago, Department of Pharmaceutical Chemistry, Faculty of Pharmacy, AIMST University, Semeling, Bedong, Kedah