PEGylated peptide to TIP1 is a novel targeting agent that binds specifically to various cancers in vivo

Kapoor, Vaishali; Singh, Abhay K.; Rogers, Buck E.; Thotala, Dinesh; Hallahan, Dennis E.

doi:10.1016/j.jconrel.2019.02.008

Cited by 13 publications

(6 citation statements)

References 36 publications

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“…To improve the pharmacological properties of peptide-based drugs, a wide range of chemical and structural modifications have been proposed in the past. It includes PEGylated peptides (Kapoor et al, 2019), peptide lipidation (Menacho-Melgar et al, 2019), peptide acetylation and amidation (da Silva et al, 2014), incorporation of unnatural D-amino acids (Khara et al, 2016), and N-methylation (Chatterjee et al, 2008), etc. The overall goal of chemical/structural modification in the peptide is to improve solubility (Mahajan et al), membrane permeation and decrease hemolysis (Lee and Lee, 2008) without tempering the therapeutic activity.…”

Section: Introductionmentioning

confidence: 99%

A Method for Predicting Hemolytic Potency of Chemically Modified Peptides From Its Structure

Kumar

Agrawal

et al. 2020

Front. Pharmacol.

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In the present study, a systematic effort has been made to predict the hemolytic potency of chemically modified peptides. All models have been trained, tested, and evaluated on a dataset that contains 583 modified hemolytic peptides and a balanced number of nonhemolytic peptides. Machine learning techniques have been used to build the classification models using an immense range of peptide features that include 2D, 3D descriptors, fingerprints, atom, and diatom compositions. Random Forest based model developed using fingerprints as an input feature achieved maximum accuracy of 78.33% with AUC of 0.86 on the main dataset and accuracy of 78.29% with AUC of 0.85 on the validation dataset. Models developed in this study have been incorporated in a web server "HemoPImod" to facilitate the scientific community (http://webs.iiitd.edu.in/raghava/ hemopimod/).

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Section: Introductionmentioning

confidence: 99%

A Method for Predicting Hemolytic Potency of Chemically Modified Peptides From Its Structure

Kumar

Agrawal

et al. 2020

Front. Pharmacol.

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“…These multivalent interactions, which arise from synergistic binding of ligands, can enhance the binding affinity of ligands [ 42 , 43 ]. Another strategy is the insertion of a longer PEG as a linker, which could delay the blood clearance rate and increase tumor uptake of the radiotracer [ 44 , 45 ].…”

Section: Discussionmentioning

confidence: 99%

Development of Radiogallium-Labeled Peptides for Platelet-Derived Growth Factor Receptor β (PDGFRβ) Imaging: Influence of Different Linkers

et al. 2020

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The purpose of this study is to develop peptide-based platelet-derived growth factor receptor β (PDGFRβ) imaging probes and examine the effects of several linkers, namely un-natural amino acids (D-alanine and β-alanine) and ethylene-glycol (EG), on the properties of Ga-DOTA-(linker)-IPLPPPRRPFFK peptides. Seven radiotracers, 67Ga-DOTA-(linker)-IPLPPPRRPFFK peptides, were designed, synthesized, and evaluated. The stability and cell uptake in PDGFRβ positive peptide cells were evaluated in vitro. The biodistribution of [67Ga]Ga-DOTA-EG2-IPLPPPRRPFFK ([67Ga]27) and [67Ga]Ga-DOTA-EG4-IPLPPPRRPFFK ([67Ga]28), which were selected based on in vitro stability in murine plasma and cell uptake rates, were determined in BxPC3-luc-bearing nu/nu mice. Seven 67Ga-labeled peptides were successfully synthesized with high radiochemical yields (>85%) and purities (>99%). All evaluated radiotracers were stable in PBS (pH 7.4) at 37 °C. However, only [67Ga]27 and [67Ga]28 remained more than 75% after incubation in murine plasma at 37 °C for 1 h. [67Ga]27 exhibited the highest BxPC3-luc cell uptake among the prepared radiolabeled peptides. As regards the results of the biodistribution experiments, the tumor-to-blood ratios of [67Ga]27 and [67Ga]28 at 1 h post-injection were 2.61 ± 0.75 and 2.05 ± 0.77, respectively. Co-injection of [67Ga]27 and an excess amount of IPLPPPRRPFFK peptide as a blocking agent can significantly decrease this ratio. However, tumor accumulation was not considered sufficient. Therefore, further probe modification is required to assess tumor accumulation for in vivo imaging.

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“…In recent years, various strategies have been developed to overcome the diverse limitations of therapeutic peptides and their administration. − …”

Section: Strategies To Tackle the Limitations Of Therapeutic Peptide ...mentioning

confidence: 99%

Recent Advances in Formulations for Long-Acting Delivery of Therapeutic Peptides

Zangabad

Rezvani

Tong

et al. 2023

ACS Appl. Bio Mater.

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Recent preclinical and clinical studies have focused on the active area of therapeutic peptides due to their high potency, selectivity, and specificity in treating a broad range of diseases. However, therapeutic peptides suffer from multiple disadvantages, such as limited oral bioavailability, short half-life, rapid clearance from the body, and susceptibility to physiological conditions (e.g., acidic pH and enzymolysis). Therefore, high peptide dosages and dose frequencies are required for effective patient treatment. Recent innovations in pharmaceutical formulations have substantially improved therapeutic peptide administration by providing the following advantages: long-acting delivery, precise dose administration, retention of biological activity, and improvement of patient compliance. This review discusses therapeutic peptides and challenges in their delivery and explores recent peptide delivery formulations, including micro/nanoparticles (based on lipids, polymers, porous silicon, silica, and stimuli-responsive materials), (stimuli-responsive) hydrogels, particle/hydrogel composites, and (natural or synthetic) scaffolds. This review further covers the applications of these formulations for prolonged delivery and sustained release of therapeutic peptides and their impact on peptide bioactivity, loading efficiency, and (in vitro/in vivo) release parameters.

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PEGylated peptide to TIP1 is a novel targeting agent that binds specifically to various cancers in vivo

Cited by 13 publications

References 36 publications

A Method for Predicting Hemolytic Potency of Chemically Modified Peptides From Its Structure

A Method for Predicting Hemolytic Potency of Chemically Modified Peptides From Its Structure

Development of Radiogallium-Labeled Peptides for Platelet-Derived Growth Factor Receptor β (PDGFRβ) Imaging: Influence of Different Linkers

Recent Advances in Formulations for Long-Acting Delivery of Therapeutic Peptides

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