Abstract
Increasing evidence demonstrates that three classes of molecules originally derived from all-trans-retinoic acid and its synthetic analogues, which function by interacting with the retinoid nuclear receptors, exert their anticancer activities through alternative signaling pathways. Thus, the methylene-linked analogues (4-HBR, 4-HPRCG, and 4-HBRCG) of N-(4-hydroxyphenyl) retinamide (4-HPR) and its O-glucuronide metabolite (4-HPROG), the cinnamic acid analogues (3- Cl-AHPC and AHPC/ST1926) of 6-[3-(1-adamantyl)-4-hydroxyphenyl)]-2-naphthalenecarboxylic acid, and N-(2,3- dihydro-2,2,4,4-tetramethyl-6-benzothiopyranyl),N-(4-nitrophenyl)thiourea (SHetA2) induce cancer cell-cycle arrest and apoptosis mediated most likely through mitochondrial and/or endoplasmic reticulum stress responses. Structure – activity relationships and potential for clinical translation as anticancer therapeutics are presented.
Keywords: 3-Cl-AHPC, 4-HPR, AHPC, AHPN, apoptosis, cell-cycle arrest, retinoid-related molecule, SHetA2, ST1926
Mini-Reviews in Medicinal Chemistry
Title: The Peptidomimetic, 1-Adamantyl-Substituted, and Flex-Het Classes of Retinoid-Derived Molecules: Their Structure-Activity Relationships and Retinoid Receptor-Independent Anticancer Activities
Volume: 10 Issue: 6
Author(s): M.I. Dawson and J.A. Fontana
Affiliation:
Keywords: 3-Cl-AHPC, 4-HPR, AHPC, AHPN, apoptosis, cell-cycle arrest, retinoid-related molecule, SHetA2, ST1926
Abstract: Increasing evidence demonstrates that three classes of molecules originally derived from all-trans-retinoic acid and its synthetic analogues, which function by interacting with the retinoid nuclear receptors, exert their anticancer activities through alternative signaling pathways. Thus, the methylene-linked analogues (4-HBR, 4-HPRCG, and 4-HBRCG) of N-(4-hydroxyphenyl) retinamide (4-HPR) and its O-glucuronide metabolite (4-HPROG), the cinnamic acid analogues (3- Cl-AHPC and AHPC/ST1926) of 6-[3-(1-adamantyl)-4-hydroxyphenyl)]-2-naphthalenecarboxylic acid, and N-(2,3- dihydro-2,2,4,4-tetramethyl-6-benzothiopyranyl),N-(4-nitrophenyl)thiourea (SHetA2) induce cancer cell-cycle arrest and apoptosis mediated most likely through mitochondrial and/or endoplasmic reticulum stress responses. Structure – activity relationships and potential for clinical translation as anticancer therapeutics are presented.
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Cite this article as:
Dawson M.I. and Fontana J.A., The Peptidomimetic, 1-Adamantyl-Substituted, and Flex-Het Classes of Retinoid-Derived Molecules: Their Structure-Activity Relationships and Retinoid Receptor-Independent Anticancer Activities, Mini-Reviews in Medicinal Chemistry 2010; 10 (6) . https://dx.doi.org/10.2174/138955710791384045
DOI https://dx.doi.org/10.2174/138955710791384045 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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