Aza-peptide aldehydes and ketones: synthesis and evaluation as human 20S proteasome inhibitors

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This is a Experimental Study study.

Thomas S. Corrigan; Sarah E. Border; Leilani Lotti Díaz; Kayla Q. Kasper; Abigail R. Miller; RababM Amer; Kayla S. Kucway; Moyer S. Fleisher; Joseph Fernandez; Alex R. Lovins; Ana K. Serrano; Conor R. Caffrey; Anthony J. O’Donoghue; Don M. Benson; Christopher M. Hadad; Özlem Doǧan Ekici

doi:10.1080/17568919.2025.2561542

October 16, 2025Future Medicinal ChemistryOpen Access

Aza-peptide aldehydes and ketones: synthesis and evaluation as human 20S proteasome inhibitors

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Key Points

Aza-peptide aldehydes and ketones effectively inhibited the human 20S proteasome, offering potential treatment for multiple myeloma.
The research demonstrates a promising new class of proteasome inhibitors focusing on cancer treatment, particularly for multiple myeloma.
The compounds were synthesized and rigorously evaluated for their inhibitory effects on the constitutive 20S proteasome activity.
These findings indicate the potential of aza-peptide analogues as alternative therapeutics in managing multiple myeloma.

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Implication

Aza-peptide aldehydes and ketones inhibit the human 20S proteasome in multiple myeloma, suggesting new therapeutic avenues.

Abstract

Aims Aza-peptide aldehydes and ketones were developed as a new class of peptidyl analogues to inhibit the human constitutive (c)20S proteasome as alternative therapeutics to treat multiple myeloma (MM).

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Cite This Study

Corrigan et al. (2025) studied this question.

synapsesocial.com/papers/68f3eb011cfc5ad53f2906d6 https://doi.org/10.1080/17568919.2025.2561542

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Aza-peptide aldehydes and ketones: synthesis and evaluation as human 20S proteasome inhibitors

Key Points

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Abstract

Discussion

Cite This Study

Aza-peptide aldehydes and ketones: synthesis and evaluation as human 20S proteasome inhibitors

Key Points

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Implication

Abstract

Discussion

Cite This Study

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