Drug intelligence / Profile preview

ferrocenyl-cyclo-(gly-l-pro)

Development stage
Preclinical
Modality
Peptide-Drug Conjugates → Peptide Conjugates → Peptides, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
01

Overview

Ferrocenyl-cyclo-(Gly-l-Pro) is an organometallic hybrid compound comprised of a ferrocene moiety linked to a cyclic dipeptide scaffold (cyclo-(Gly-L-Pro)). These hybrids are novel inhibitors of ABC transporter proteins, specifically ABCB1 (P-glycoprotein) and ABCG2, which are involved in multidrug resistance (MDR) in cancer. The compounds are virtually nontoxic to both colon cancer cells (including MDR variants) and normal fibroblasts, but when used in combination with chemotherapeutics such as vincristine, mitoxantrone, and doxorubicin, they significantly sensitize MDR cells and lower the IC50 values for these drugs. The hybrids act as substrates and inhibitors of ABC transporters, increasing intracellular drug retention and showing synergistic effects with standard chemotherapy agents. Their mechanism appears to be direct inhibition of drug efflux by ABCB1 and ABCG2, overcoming MDR phenotypes[1][3][6][7][8][9][10].

Other names
ferrocenyl–cyclo-(gly-l-pro) hybrids
02

Targets

ABCB1 (P-glycoprotein)ABCG2 (Breast cancer resistance protein)

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