Interaction of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (NSC 79037) with nucleic acids and proteins in vivo and in vitro.

Paper

Interaction of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (NSC 79037) with nucleic acids and proteins in vivo and in vitro.

Published 1972 · C. J. Cheng, Shinji Fujimura, Dezider Grunberger

Cancer research

Q1 SJR score

130

Citations

1

Influential Citations

Semantic Scholar

Abstract

The macromolecular binding of radioactivity from 1-(2-chlorethyl)-3-cyclohexyl-1-nitrosourea, labeled with 14C in either the cyclohexyl moiety or the ethylene residue, was studied in the L1210 leukemia-bearing mice, in a suspension of L1210 leukemia cells, and during in vitro incubation with isolated nucleic acids and proteins. In all three systems, radioactivity from cyclohexyl-14C-labeled 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea was extensively bound to proteins, and there was negligible binding to nucleic acids. Radioactivity from the ethylene-14C-labeled drug was bound to both nucleic acids and proteins, but the binding was only a fraction of the observed protein binding of the cyclohexyl label. Of the various macromolecules examined for in vitro binding, poly-l-lysine and albumin were the most active in binding the cyclohexyl-labeled material; polyguanylic acid, polycytidylic acid, and tRNA were the most active in binding the ethylene-14C-labeled material. The possibility that the carcinostatic activity of this drug reflects a dual capacity, namely, modification of cellular proteins via cyclohexylcarbamoylation and of nucleic acids via alkylation, is discussed.

In Vitro Study

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Study Snapshot

The carcinostatic activity of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea may be due to its dual capacity to modify proteins and nucleic acids, potentially affecting cancer cell growth.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Interaction of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (NSC 79037) with nucleic acids and proteins in vivo and in vitro.

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References

Clinical studies with 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea (NSC 79037).

1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea shows potential as an effective and well-tolerated treatment for advanced cancers, with potential responses in various cancer types and neurological improvement in glioblastoma multiforme patients.

The uptake, distribution, and antitumor activity of 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea in the murine glioma.

CCNU shows antitumor activity in murine gliomas, with its effectiveness being independent of preferential uptake or distribution between normal and tumor tissue.

The absorption, distribution, excretion, and biotransformation of the carcinostatic 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea in animals.

The carcinostatic 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea rapidly degrades in mouse and dog plasma, is primarily excreted by kidneys, and is primarily bound to cyclohexyl proteins, with inactive cata

Interaction of N-methyl-N'-nitro-N-nitrosoguanidine with ascites hepatoma cells in vitro.

N-methyl-N'-nitro-N-nitrosoguanidine (NG) interacts with ascites hepatoma cells in vitro, potentially impacting biological materials and affecting cancer progression.

Reaction of N-methyl-N'-nitro-N-nitrosoguanidine with protein: formation of nitroguanido derivatives.

Serum albumin exposure to N-methyl-N′-nitro-N-nitrosoguanidine leads to the formation of nitroguanido derivatives, increasing protein extinction coefficient and electrophoretic mobility, while reducing lysine content.

BCNU (1,3), BIS(B‐chloroethyl)‐1‐nitrosourea. Effects on advanced Hodgkin's disease and other neoplasia

BCNU shows promise as a rapid and effective treatment for advanced Hodgkin's disease, with potential for use in lymphosarcoma and reticulum cell sarcoma patients.

Pigmentation due to a new antitumor agent. Effects of topical application of BCNU [1,3-bis(2-chloroethyl)-1-nitrosourea].

Topical application of BCNU, a potential antitumor agent, may cause skin hyperpigmentation as a postinflammatory event.

Citations

Glioblastoma Treatment Modalities besides Surgery

Novel treatments for glioblastoma, such as BNCT and immunotherapy, show promising preclinical results but clinical results are uncertain or discouraging.

Nanoparticle based strategies for the treatment of Glioblastoma

A high dose nanoparticle formulation of the cytotoxic drug lomustine using a self-assembling chitosan amphiphile, quaternary ammonium palmitoyl glycol chitosan, led to improved survival outcomes without a commensurate increase in toxic effects in

Nitrosoureas inhibit the stathmin-mediated migration and invasion of malignant glioma cells.

Inhibiting stathmin expression and function may help limit the spread of malignant gliomas within the brain, offering potential therapeutic benefits in addition to their antiproliferative effects.

Covalent modification of stathmin by CCNU determined by FTMS analysis of modified proteins and tryptic peptides.

Reversed-phase protein chromatography and FT-ICR mass spectrometry effectively determine the stoichiometry and sites of CCNU modification in stathmin, revealing differential reactivity of several lysyl residues.

The 1p-encoded protein stathmin and resistance of malignant gliomas to nitrosoureas.

Decreased stathmin expression in malignant gliomas is associated with increased recurrence-free survival and resistance to nitrosourea treatments.