Peptide-based drug discovery: Current status and recent advances

Sharma, Komal; Sharma, Krishna K.; Sharma, Anku; Jain, Rahul

doi:10.1016/j.drudis.2022.103464

Cited by 95 publications

(87 citation statements)

References 113 publications

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“…As different synthetic strategies continue to be developed, such as studies on oxytocin in 1953 [ 2 ] and vasopressin in 1958 [ 3 ] which were performed by solution phase peptide synthesis strategies, synthetic human insulin was obtained by recombinant technology in 1982, leuprolide in 1985, and goserin in 1989. Various synthetic strategies for complex peptides were developed as an effective, efficient, and harmless alternative to small molecule drugs [ 4 ]. On the other side, the local application and short residence time of free AMPs are affected by environmental sensitivities such as hydrolysis, oxidation, enzymatic hydrolysis, photolysis, and pH.…”

Section: Introductionmentioning

confidence: 99%

Actinomycin-X2-Immobilized Silk Fibroin Film with Enhanced Antimicrobial and Wound Healing Activities

Zhou

Xie

et al. 2023

IJMS

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Actinomycin is a family of chromogenic lactone peptides that differ in their peptide portions of the molecule. An antimicrobial peptide, actinomycin X2 (Ac.X2), was produced through the fermentation of a Streptomyces cyaneofuscatus strain. Immobilization of Ac.X2 onto a prepared silk fibroin (SF) film was done through a carbodiimide reaction. The physical properties of immobilized Ac.X2 (antimicrobial films, AMFs) were analyzed by ATR-FTIR, SEM, AFM, and WCA. The findings from an in vitro study showed that AMFs had a more broad-spectrum antibacterial activity against both S. aureus and E. coli compared with free Ac.X2, which showed no apparent strong effect against E. coli. These AMFs showed a suitable degradation rate, good hemocompatibility, and reduced cytotoxicity in the biocompatibility assay. The results of in vivo bacterially infected wound healing experiments indicated that wound inflammation was prevented by AMFs, which promoted wound repair and improved the wound microenvironment. This study revealed that Ac.X2 transformation is a potential candidate for skin wound healing.

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Section: Introductionmentioning

confidence: 99%

Actinomycin-X2-Immobilized Silk Fibroin Film with Enhanced Antimicrobial and Wound Healing Activities

Zhou

Xie

et al. 2023

IJMS

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“…Along with the above mentioned applications, peptide drugs also play a significant role in biomaterial science and drug delivery and also possess widespread applications in the medicinal domain. In this context, peptide-installed therapeutics have great priority in the pharmaceutical field [ 54 , 55 ]. Moreover, in order to treat various diseases, different kinds of peptides are doing rounds in the market, namely chelated peptides (7%), cyclic peptides (25%), linear peptides (45%) and conjugated peptides (23%) ( Figure 6 ).…”

Section: Introductionmentioning

confidence: 99%

Conjugation as a Tool in Therapeutics: Role of Amino Acids/Peptides-Bioactive (Including Heterocycles) Hybrid Molecules in Treating Infectious Diseases

et al. 2023

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Peptide-based drugs are gaining significant momentum in the modern drug discovery, which is witnessed by the approval of new drugs by the FDA in recent years. On the other hand, small molecules-based drugs are an integral part of drug development since the past several decades. Peptide-containing drugs are placed between small molecules and the biologics. Both the peptides as well as the small molecules (mainly heterocycles) pose several drawbacks as therapeutics despite their success in curing many diseases. This gap may be bridged by utilising the so called ‘conjugation chemistry’, in which both the partners are linked to one another through a stable chemical bond, and the resulting conjugates are found to possess attracting benefits, thus eliminating the stigma associated with the individual partners. Over the past decades, the field of molecular hybridisation has emerged to afford us new and efficient molecular architectures that have shown high promise in medicinal chemistry. Taking advantage of this and also considering our experience in this field, we present herein a review concerning the molecules obtained by the conjugation of peptides (amino acids) to small molecules (heterocycles as well as bioactive compounds). More than 125 examples of the conjugates citing nearly 100 references published during the period 2000 to 2022 having therapeutic applications in curing infectious diseases have been covered.

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“…15 Proteins are often natural drug targets, therefore, identifying key residues ("hot spots") that can be used for functionalization 16 for lead identification in drug discovery. 17 amino acids that are considered as "weakly" reactive, including Trp, Tyr, Phe, and His, would lead to a plethora of new chemistries. Peptide-based therapeutics often exhibit high potency than small molecule drugs, and further synthetic peptide modification can improve pharmacokinetic features such as drug stability, cell penetration, and oral bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Exploring Chemical Modifications of Aromatic Amino Acid Residues in Peptides

et al. 2023

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The chemical diversification of biomolecules set forth a significant area that constitutes an important intersection between chemistry and biology. Amino acids and peptides, are the fundamental building blocks of proteins, play an ubiquitous role in all living organisms. While significant efforts have been geared to the chemical modifications of amino acid residues, particularly the functionalization of reactive functional groups such as Lysine-NH2 and Cysteine –SH, the exploration of aromatic amino acid residues of Tryptophan, Tyrosine, Phenylalanine, and Histidine has been relatively limited. Therefore, this review highlights on the strategies for side chain functionalization of these four aromatic amino acids in peptides, with a focus on elucidating the underlying mechanisms. We have also illustrated the usage of these chemical modifications in the chemical and biological realm.

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Peptide-based drug discovery: Current status and recent advances

Cited by 95 publications

References 113 publications

Actinomycin-X2-Immobilized Silk Fibroin Film with Enhanced Antimicrobial and Wound Healing Activities

Actinomycin-X2-Immobilized Silk Fibroin Film with Enhanced Antimicrobial and Wound Healing Activities

Conjugation as a Tool in Therapeutics: Role of Amino Acids/Peptides-Bioactive (Including Heterocycles) Hybrid Molecules in Treating Infectious Diseases

Exploring Chemical Modifications of Aromatic Amino Acid Residues in Peptides

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