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Selective high affinity retinoic acid receptor alpha or beta-gamma ligands.
Two complementary assays are set up, an in vitro binding assay to determine the Kd values of retinoids for RAR alpha, RAR beta, and RAR gamma and a functional assay in cultured cells to evaluate the potential of Retinoids to transactivate, through their binding to one type of RAR, a reporter gene. Expand
p53 independent G0/G1 arrest and apoptosis induced by a novel retinoid in human breast cancer cells.
AHPN represents a novel retinoid that induces G0/G1 arrest and apoptosis via a unique pathway which appears to involve activation of known downstream effectors of p53 in a p53-independent manner. Expand
Identification of synthetic retinoids with selectivity for human nuclear retinoic acid receptor gamma.
- B. Bernard, J. Bernardon, +7 authors B. Shroot
- Biology, Medicine
- Biochemical and biophysical research…
- 31 July 1992
Using in vitro binding studies and a functional transactivation assay, this work has identified three compounds with high RAR gamma selectivity that could provide therapeutic entities with a higher therapeutic index at lower teratogenic risk. Expand
The role of retinoic acid receptors in neurite outgrowth from different populations of embryonic mouse dorsal root ganglia.
Results suggest a role for RA acting via RAR(beta)(2) in the outgrowth of neurites in NGF, NT-3 and BDNF dependent neurons isolated from embryonic day (E)13.5 mouse DRG. Expand
Molecular Determinants of AHPN (CD437)-Induced Growth Arrest and Apoptosis in Human Lung Cancer Cell Lines
The results reveal a novel pathway for retinoid-induced apoptosis and suggest that AHPN/CD437 or analogs may have a better therapeutic efficacy against lung cancer. Expand
Retinoid induced apoptosis in leukemia cells through a retinoic acid nuclear receptor-independent pathway.
A novel retinoid 6-[3-adamantyl)-4-hydroxyphenyl]-2-naphthalene carboxylic acid (AHPN; CD437) is described that not only totally inhibits the proliferation of RA-resistant leukemic cell lines HL-60R and K562 but also induces apoptosis in these cells. Expand
Differential effects of synthetic nuclear retinoid receptor-selective retinoids on the growth of human non-small cell lung carcinoma cells.
There appeared to be no simple correlation among the histological type of the NSCLC, the levels of nuclear receptors or CRABPs, and the response of the cells to the growth-inhibitory effects of retinoids, but results suggest that several synthetic retinoid do exhibit inhibitory activity against NSCLCs, and some of them may be useful clinically. Expand
Pharmacology and chemistry of adapalene.
Adapalene is a stable naphthoic acid derivative with potent retinoid pharmacology, controlling cell proliferation and differentiation, and has significant antiinflammatory action. Expand
Cellular senescence mechanisms in chronic wound healing
The majority of chronic wounds respond well to conventional treatments; however, in a small population of chronic wound patients (estimated to be anywhere from 15 to 20% of all chronic wound sufferers) healing does not occur despite the best care. Expand
Site-Specific Drug Delivery to Pilosebaceous Structures Using Polymeric Microspheres
- A. Rolland, N. Wagner, A. Chatelus, B. Shroot, H. Schaefer
- Chemistry, Medicine
- Pharmaceutical Research
- 1 December 1993
The view that follicular drug targeting using 5-µm polymeric microspheres may represent a promising therapeutic approach for the treatment of pathologies associated with pilosebaceous units is supported. Expand