Journal ArticleDOI
Preclinical pharmacokinetics, metabolism, and toxicity of azurin-p28 (NSC745104) a peptide inhibitor of p53 ubiquitination
Lee Jia,Gregory S. Gorman,Lori Coward,Patricia E. Noker,David L. McCormick,Thomas L. Horn,J. Brooks Harder,Miguel Muzzio,Bellur S. Prabhakar,Balaji B. Ganesh,Tapas K. Das Gupta,Craig W. Beattie +11 more
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TLDR
p28 does not exhibit preclinical immunogenicity or toxicity, has a similar metabolic profile among species, and is therapeutic in xenograft models.Abstract:
Purpose
Characterize the preclinical pharmacokinetics, metabolic profile, multi-species toxicology, and antitumor efficacy of azurin-p28 (NSC 745104), an amphipathic, 28 amino acid fragment (aa 50–77) of the copper containing redox protein azurin that preferentially enters cancer cells and is currently under development for treatment of p53-positive solid tumors.read more
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Cell-Penetrating Peptides: From Basic Research to Clinics
TL;DR: In this article, cell-penetrating peptides (CPPs) have been used to increase medicament concentrations in areas that are difficult to access, which can transport into the cell a wide variety of biologically active conjugates.
Journal ArticleDOI
Cell Penetrating Peptides as Molecular Carriers for Anti-Cancer Agents.
TL;DR: This review describes the several types of CPPs, the chemical modifications to improve their cellular uptake, the different mechanisms to cross cell membranes and their biological properties upon conjugation with specific molecules.
Journal ArticleDOI
Recent Advances in Cell Penetrating Peptide-Based Anticancer Therapies.
Justine Habault,Jean-Luc Poyet +1 more
TL;DR: Recent advances in the potential usage of CPPs in the context of cancer therapy are focused on, with a particular interest in CPP-mediated delivery of anti-tumoral proteins.
Journal ArticleDOI
A first-in-class, first-in-human, phase i trial of p28, a non-HDM2-mediated peptide inhibitor of p53 ubiquitination in patients with advanced solid tumours
Michael A. Warso,Jon M. Richards,D. Mehta,Konstantin Christov,C. M. Schaeffer,L Rae Bressler,Taketo Yamada,Dibyen Majumdar,Scott Kennedy,Craig W. Beattie,T. K. Das Gupta +10 more
TL;DR: Evidence of anti-tumour activity indicates a highly favourable therapeutic index and demonstrates proof of concept for this new class of non-HDM2-mediated peptide inhibitors of p53 ubiquitination.
Journal ArticleDOI
Pharmaceutical development, composition and quantitative analysis of phthalocyanine as the photosensitizer for cancer photodynamic therapy.
TL;DR: Mechanisms of action of Pc used for photodynamic therapy, its pharmaceutical development and molecular modification to enhance its drugability and improve its intracellular localization are reviewed.
References
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Journal ArticleDOI
The conduct of drug metabolism studies considered good practice (II): in vitro experiments.
Lee Jia,Xiaodong Liu +1 more
TL;DR: This publication aims at providing a general framework to guide designs and protocols of the in vitro drug metabolism studies considered good practice in an efficient manner such that it would help researchers avoid common pitfalls and misleading results.
Journal ArticleDOI
Bacterial cupredoxin azurin as an inducer of apoptosis and regression in human breast cancer
Vasu Punj,Suchita Bhattacharyya,Djenann Saint-Dic,Chenthamarakshan Vasu,Elizabeth A Cunningham,J. M. Graves,Tohru Yamada,Andreas I. Constantinou,Konstantin Christov,Bethany E. Perez White,Gang Li,Dibyen Majumdar,Ananda M. Chakrabarty,Tapas K. Das Gupta +13 more
TL;DR: In conclusion, azurin blocks breast cancer cell proliferation and induces apoptosis through the mitochondrial pathway both in vitro and in vivo, thereby suggesting a potential chemotherapeutic application of this bacterial cupredoxin for the treatment of breast cancer.
Journal ArticleDOI
Noncationic peptides obtained from azurin preferentially enter cancer cells.
Brad N. Taylor,Rajeshwari R. Mehta,Tohru Yamada,Fatima Lekmine,Konstantin Christov,Ananda M. Chakrabarty,Albert Green,Laura Bratescu,Anne Shilkaitis,Craig W. Beattie,Tapas K. Das Gupta +10 more
TL;DR: Observations suggest the azurin fragments, p18 and p28, account for the preferential entry of Azurin into human cancer cells and a significant amount of the antiproliferative activity of azurIn on human cancer Cells, respectively.
Journal ArticleDOI
Internalization of bacterial redox protein azurin in mammalian cells: entry domain and specificity.
Tohru Yamada,Arsenio M. Fialho,Vasu Punj,Laura Bratescu,Tapas K. Das Gupta,Ananda M. Chakrabarty +5 more
TL;DR: It is demonstrated that azurin is internalized in J774 or cancer cells in a temperature‐dependent manner and shows preferential entry into cancer compared with normal cells.
Journal ArticleDOI
Apoptosis or growth arrest: Modulation of tumor suppressor p53's specificity by bacterial redox protein azurin.
Tohru Yamada,Yoshinori Hiraoka,Masateru Ikehata,Kazuhide Kimbara,Benjamin S. Avner,Tapas K. Das Gupta,Ananda M. Chakrabarty +6 more
TL;DR: It is reported that purified M44KM64E mutant azurin protein can enter both J774 cells as well as the human breast cancer MCF-7 cells, demonstrating the role of a single bacterial protein and its hydrophobic patch in modulating two important functions of p53.