Protein Binding of Anticancer Drugs

Sparreboom, Alex; Loos, Walter J.

doi:10.1007/978-1-59259-734-5_12

Cited by 5 publications

(4 citation statements)

References 110 publications

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“…), and when it was 1000 nM, the value was 14.0 ± 0.60% (mean ± s.e.m.). These results agree with the values of previous studies (15–33%), 23,30,31 indicating that our method effectively measures the unbound drug concentration in human serum.…”

Section: Resultssupporting

confidence: 92%

A rapid and simple electrochemical detection of the free drug concentration in human serum using boron-doped diamond electrodes

Moriyama

Ogata

Nashimoto

et al. 2022

Analyst

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Section: Resultssupporting

confidence: 92%

A rapid and simple electrochemical detection of the free drug concentration in human serum using boron-doped diamond electrodes

Moriyama

Ogata

Nashimoto

et al. 2022

Analyst

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“…The in silico-based safety analysis of the antileukemic compounds was tested by measuring their binding affinity to albumin (PDB ID-6QS9) (Behzadi et al 2019). The affinity of cytotoxic compounds to bind to albumin has a great impact on their pharmacodynamics and pharmacokinetic properties; for example, the anticancer agent chlorambucil is 99% bound to albumin and yet has a short half-life of 1.3 ± 0.90 h (Sparreboom and Loos 2004). In accordance with this (1)…”

Section: Molecular Dockingmentioning

confidence: 95%

Phytochemical Investigation of Egyptian Spinach Leaves, a Potential Source for Antileukemic Metabolites: In Vitro and In Silico Study

Abdelgawad

Hetta

Ibrahim

et al. 2022

Rev. Bras. Farmacogn.

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Spinacia oleracea L., Amaranthaceae, leaves cultivated in Egypt demonstrated a potential antileukemic activity against the chronic myeloid leukemia, K562 cell line. Thus, the aim of this study is to carry out a phytochemical investigation of S. oleracea leaves as well as the isolation of its antileukemic phytoconstituents. Phytochemical investigation of S. oleracea leaves resulted in the isolation of seventeen known compounds. The biological study revealed that compounds hexaprenol, phytol, and 18-[(1-oxohexadecyl) oxy]-9-octadecenoic acid exhibited a remarkable antiproliferative activity against K562 cells in vitro. A mechanistic in silico study showed that hexaprenol, phytol, and 18-[(1-oxohexadecyl) oxy]-9-octadecenoic acid exhibited a strong binding affinity towards topoisomerase (docking score −12.50, −9.19, and −13.29 kcal/mol, respectively), and showed as well a strong binding affinity towards Abl kinase (docking score −11.91, −9.35, and −12.59 kcal/mol, respectively). Molecular dynamics study revealed that 18-[(1-oxohexadecyl) oxy]-9-octadecenoic acid produced stable complexes with both topoisomerase and Abl kinase with RMSD values of 1.81 and 1.85 Å, respectively. As a result of our findings, we recommend more in vivo and preclinical studies to confirm the potential benefit of spinach leaves for chronic myeloid leukemia patients. Graphical Abstract

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“…Other oligonucleotides such as siRNAs also require albumin transportation [ 176 ]. However, the plasma binding affinity of chemotherapeutics is significantly higher, ranging from >90% for carboplatin and paclitaxel to <30% for cyclophosphamide and cytarabine [ 179 ]. Thus, it is possible that oligonucleotides compete with chemotherapeutics for plasma protein binding, which may lead to reduced in vivo efficacy of the combination compared to chemotherapeutics alone [ 180 ].…”

Section: Overcoming Challenges Of Oligonucleotide Therapeuticsmentioning

confidence: 99%

Recent Advances in Oligonucleotide Therapeutics in Oncology

Xiong

Veedu

Diermeier

2021

IJMS

119

103

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Cancer is one of the leading causes of death worldwide. Conventional therapies, including surgery, radiation, and chemotherapy have achieved increased survival rates for many types of cancer over the past decades. However, cancer recurrence and/or metastasis to distant organs remain major challenges, resulting in a large, unmet clinical need. Oligonucleotide therapeutics, which include antisense oligonucleotides, small interfering RNAs, and aptamers, show promising clinical outcomes for disease indications such as Duchenne muscular dystrophy, familial amyloid neuropathies, and macular degeneration. While no approved oligonucleotide drug currently exists for any type of cancer, results obtained in preclinical studies and clinical trials are encouraging. Here, we provide an overview of recent developments in the field of oligonucleotide therapeutics in oncology, review current clinical trials, and discuss associated challenges.

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Protein Binding of Anticancer Drugs

Cited by 5 publications

References 110 publications

A rapid and simple electrochemical detection of the free drug concentration in human serum using boron-doped diamond electrodes

A rapid and simple electrochemical detection of the free drug concentration in human serum using boron-doped diamond electrodes

Phytochemical Investigation of Egyptian Spinach Leaves, a Potential Source for Antileukemic Metabolites: In Vitro and In Silico Study

Recent Advances in Oligonucleotide Therapeutics in Oncology

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