Keynote
Peptide-based drug discovery: Current status and recent advances

https://doi.org/10.1016/j.drudis.2022.103464Get rights and content

Highlights

  • A comprehensive compilation and analysis of FDA approved and under clinical trials peptide-based therapeutics.

  • Clinical trial peptides pipeline analysis reveals emerging areas and drug targets.

  • Recent advancements in the synthesis and diversification of peptides using unnatural amino acids, late-stage and Csingle bondH functionalization, and ligation techniques.

  • New advancements in peptide discovery through emphasis on emerging technologies such as DNA-encoded library and display techniques.

The progressive development of peptides from reaction vessels to life-saving drugs via rigorous preclinical and clinical assessments is fascinating. Peptide therapeutics have gained momentum with the evolution of techniques in peptide chemistry, such as microwave irradiation in solid- and solution-phase synthesis, ligation chemistry, recombinant synthesis, and amalgamation with synthetic tools, including metal catalysis. Diverse emerging technologies, such as DNA-encoded libraries (DELs) and display techniques, are changing the status quo in the discovery of peptide therapeutics. In this review, we analyzed US Food and Drug Administration (FDA)-approved peptide drugs and those in clinical trials, highlighting recent advances in peptide-based drug discovery.

Keywords

peptide therapeutics
peptide drug discovery
peptide synthesis
display technology
clinical trial
FDA-approved drug

Data availability

No data was used for the research described in the article.

Cited by (0)

Komal Sharma was awarded an MS Pharm from the National Institute of Pharmaceutical Education and Research (NIPER), Mohali, India while working in the area of carbohydrate chemistry. She then completed a PhD with Rahul Jain, working on the synthesis and biological and mechanistic investigation of short antimicrobial peptides. She recently joined Stanford University to further pursue her passion for research. Her research interests include the design and development of peptide-based therapeutics and biomaterial chemistry.

Krishna K. Sharma Krishna K. Sharma was awarded an MS Pharm and PhD from NIPER, Mohali, India under the supervision of Rahul Jain while working on the functionalization of heterocycles, amino acids, peptides, and their utilization in therapeutics. He conducted postdoctoral research in the School of Pharmacy of The University of Kansas (2017–2019) and College of Pharmacy, Ohio State University (2019–2021). He is currently working in the Department of Chemistry at Iowa State University. His research interests include peptide-based medicinal chemistry approaches in various therapeutic areas.

Rahul Jain Rahul Jain moved to UT Southwestern Medical Center after completing a PhD in medicinal chemistry at CDRI, Lucknow, India. He returned to India after working at National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, and Tulane University, and joined the Department of Medicinal Chemistry at NIPER, where he is professor of medicinal chemistry. His research interests vary from heterocycle-based antimalarials and antituberculosis agents to ultra-short peptide/mimetic-based central nervous system drugs and antimicrobials, as well as new structural classes of synthetic amino acid.

1

Present address: Department of Chemistry, Iowa State University, Ames, IA 50011, USA.

2

These authors contributed equally.

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