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Review
. 2024 Jun 13;25(12):6523.
doi: 10.3390/ijms25126523.

The Versatility of Collagen in Pharmacology: Targeting Collagen, Targeting with Collagen

Francisco Revert-Ros  1 , Ignacio Ventura  1 , Jesús A Prieto-Ruiz  1 , José Miguel Hernández-Andreu  1 , Fernando Revert  1
Affiliations
Review

The Versatility of Collagen in Pharmacology: Targeting Collagen, Targeting with Collagen

Francisco Revert-Ros et al. Int J Mol Sci. .

Abstract

Collagen, a versatile family of proteins with 28 members and 44 genes, is pivotal in maintaining tissue integrity and function. It plays a crucial role in physiological processes like wound healing, hemostasis, and pathological conditions such as fibrosis and cancer. Collagen is a target in these processes. Direct methods for collagen modulation include enzymatic breakdown and molecular binding approaches. For instance, Clostridium histolyticum collagenase is effective in treating localized fibrosis. Polypeptides like collagen-binding domains offer promising avenues for tumor-specific immunotherapy and drug delivery. Indirect targeting of collagen involves regulating cellular processes essential for its synthesis and maturation, such as translation regulation and microRNA activity. Enzymes involved in collagen modification, such as prolyl-hydroxylases or lysyl-oxidases, are also indirect therapeutic targets. From another perspective, collagen is also a natural source of drugs. Enzymatic degradation of collagen generates bioactive fragments known as matrikines and matricryptins, which exhibit diverse pharmacological activities. Overall, collagen-derived peptides present significant therapeutic potential beyond tissue repair, offering various strategies for treating fibrosis, cancer, and genetic disorders. Continued research into specific collagen targeting and the application of collagen and its derivatives may lead to the development of novel treatments for a range of pathological conditions.

Keywords: cancer; collagen; drug; fibrosis.

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Conflict of interest statement

The authors declare no conflicts of interest.

Figures

Figure 1
Figure 1
Phylogeny of collagen. Collagen IV is the earliest form of collagen and is normally associated with epithelial differentiation. Collagen I emerged in more advanced organisms and serves as a key component of the mesenchymal extracellular matrix. This illustration is inspired by the findings, schemes, and conclusions of Billy G. Hudson’s laboratory [12].
Figure 2
Figure 2
Direct and indirect targeting of collagen. Schematic representation of relevant cellular processes and drugs targeting collagen expression, cleavage, assembly, and degradation in the extracellular matrix. The different targetable processes are indicated with cursive bold lettering, and the drugs listed below with the corresponding target in parentheses. In red are the drugs assayed in clinical trials registered in ClinicalTrials.org. A question mark (?) denotes that a not fully demonstrated drug target.
See this image and copyright information in PMC

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