Melanin and Tyrosinase Association in Normal and Pathological Skin Pigmentation

Traub, Eugene F.; Spoor, Herbert J.

doi:10.1016/b978-1-4832-2904-1.50019-3

Cited by 5 publications

(3 citation statements)

References 10 publications

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“…The interactions of DM-CHOC-PEN and DOPA induced the formation of melanina high-energy component/storage that results in an increase in ΔF and a decrease in ΔS, with the development of cells in a new, resting high-energy state -the beta state (Figure 3). The latter cells are well-differentiated and die (30).…”

Section: Table I Half-maximal Inhibitory Concentration (Ic 50 ) Of Di...mentioning

confidence: 99%

Preclinical Activity of 4-Demethyl-4-cholesteryloxycarbonylpenclomedine in Melanoma

Friedlander¹,

Morgan²,

Benes³

et al. 2023

Anticancer Res

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Background/Aim: Temozolomide plays a role in treating melanoma refractory to immunomodulatory and mitogen-activated protein kinase-targeted approaches, but its efficacy is limited. 4-Demethyl-4-cholesteryloxycarbonylpenclomedine (DM-CHOC-PEN) is a polychlorinated pyridine cholesteryl carbonate. Its mechanism of action is considered to be via alkylation/adduct formation with N 7 -guanine. It demonstrated activity in intracranial implanted human glioma and breast cancer xenograft mouse models. The activity of DM-CHOC-PEN in melanoma models was assessed. Material and Methods: B-16 melanoma cells were exposed to DM-CHOC-PEN at different concentrations to assess proliferation and survival. B-16 cells were implanted subcutaneously into the flank of adult female C57BL mice which were then were treated with 200 mg/kg DM-CHOC-PEN intraperitoneally daily for 5 days in the setting of palpable subcutaneous tumor. Survival was compared to mice treated with temozolomide or saline. Five mice were treated per group. Results: In vitro, the respective half-maximal inhibitory concentrations of DM-CHOC-PEN and temozolomide were 0.5 and ≥3.0 μg/ml. Floating, heavily melanotic cells formed and these cells were separated, analyzed, and contained 10-90 ng DM-CHOC-PEN per 10 5 cells. The improvement in survival of mice treated with DM-CHOC-PEN or temozolomide relative to saline controls was 142% and 78%, respectively. Conclusion: Longer survival was seen with DM-CHOC-PEN in a C57BL murine model relative to temozolomide and saline-treated controls, supporting the development of clinical trials assessing the efficacy of DM-CHOC-PEN as treatment for metastatic melanoma.

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Section: Table I Half-maximal Inhibitory Concentration (Ic 50 ) Of Di...mentioning

confidence: 99%

Preclinical Activity of 4-Demethyl-4-cholesteryloxycarbonylpenclomedine in Melanoma

Friedlander¹,

Morgan²,

Benes³

et al. 2023

Anticancer Res

View full text Add to dashboard Cite

show abstract

“…Melanin is far from being an end-product of oxidation [34][35][36][37]. At a glance the existence of energy bands are obvious from the highly conjugated heterocyclic indole quinone structure for melanin (Fig.…”

Section: Evolution Of the Molecular Biology Of Brain Tumors And The Tmentioning

confidence: 99%

“…Clusters of melanin laden cells contained significantly elevated concentrations of DM-CHOC-PEN, as compared to the amelanotic variant; a possible storage site for the drug [31]. The initial DOPA → DOPA quinone transformation is catalyzed by tyrosinase (DOPA oxidase) intracellular [32][33][34][35]. However, the red-ox potential for DM-CHOC-PEN is sufficient to catalyze the conversion with excess melanin formation per the Rapier Scheme below [32].…”

Section: Evolution Of the Molecular Biology Of Brain Tumors And The Tmentioning

confidence: 99%

A Rational for Novel Anti-NeuroOncology Drugs

Morgan¹

2013

Evolution of the Molecular Biology of Brain Tumors and the Therapeutic Implications

Melanin and Tyrosinase Association in Normal and Pathological Skin Pigmentation

Cited by 5 publications

References 10 publications

Preclinical Activity of 4-Demethyl-4-cholesteryloxycarbonylpenclomedine in Melanoma

Preclinical Activity of 4-Demethyl-4-cholesteryloxycarbonylpenclomedine in Melanoma

A Rational for Novel Anti-NeuroOncology Drugs

Zur Diagnostik und Therapie der Melanocytoblastome

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