Peptidomimetics in cancer targeting

Abstract

The low efficiency of treatment strategies is one of the main obstacles to developing cancer inhibitors. Up to now, various classes of therapeutics have been developed to inhibit cancer progression. Peptides due to their small size and easy production compared to proteins are highly regarded in designing cancer vaccines and oncogenic pathway inhibitors. Although peptides seem to be a suitable therapeutic option, their short lifespan, instability, and low binding affinity for their target have not been widely applicable against malignant tumors. Given the peptides’ disadvantages, a new class of agents called peptidomimetic has been introduced. With advances in physical chemistry and biochemistry, as well as increased knowledge about biomolecule structures, it is now possible to chemically modify peptides to develop efficient peptidomimetics. In recent years, numerous studies have been performed to the evaluation of the effectiveness of peptidomimetics in inhibiting metastasis, angiogenesis, and cancerous cell growth. Here, we offer a comprehensive review of designed peptidomimetics to diagnose and treat cancer.

Advances in MRI: Peptide and peptidomimetic‐based contrast agents

“…40 Peptidomimetics can be described as mimic of peptides with improved properties such as metabolic stability and high selectivity facilitating the cancer diagnosis. 41 A new family of RGD (arginine-glycineaspartic acid) peptidomimetics having a bifunctional diketopiperazine (DKP) scaffold with integrin affinity has caught the interest of different research groups. 42 Integrins are a family of transmembrane glycoproteins belonging to a group of cell adhesion molecules playing an important role in tumor and metastasis.…”

“…Many research groups have created integrin ligands based on linear or cyclic peptidomimetics to enhance MRI for cancer diagnosis 40 . Peptidomimetics can be described as mimic of peptides with improved properties such as metabolic stability and high selectivity facilitating the cancer diagnosis 41 . A new family of RGD (arginine–glycine–aspartic acid) peptidomimetics having a bifunctional diketopiperazine (DKP) scaffold with integrin affinity has caught the interest of different research groups 42 …”

AGuIX nanoparticle-nanobody bioconjugates to target immune checkpoint receptors

“…However, they often exhibit low affinity for the target compared to antibodies. 10 Conversely, antibodies have demonstrated remarkable efficacy as targeting molecules, but their larger size hampers tissue penetration and prevents access to certain areas in tumoral tissues. 11 For these reasons, our work focuses on bioconjugates based on nanobodies, otherwise known as variable heavy domain of heavy chain (VHH).…”

Peptides as Therapeutic Agents: Challenges and Opportunities in the Green Transition Era

“…Accordingly, both peptide analogues and peptidomimetics have flourished over the past years and stand out for their own importance as a well-defined category of therapeutics; hence, their discussion is beyond the scope of the present work. For an in-depth discussion on this topic, several excellent publications can be found in the recent literature [14][15][16][17][18][19][20].…”