Novel retinoids with receptor selectivity and functional selectivity

British Journal of Dermatology, Supplement

Volumn 140, Issue 54, 1999, Pages 12-17

  Johnson, A ^a   Chandraratna, R A S ^a  

^a ALLERGAN INC   (United States)

Author keywords

Agonist; Antagonist; Cancer; Psoriasis; Receptor; Retinoic acid; Retinoid

Indexed keywords

4 [2 (5,6,7,8 TETRAHYDRO 5,5,8,8 TETRAMETHYL 2 NAPHTHYL) 1 PROPENYL]BENZOIC ACID; 4 [2 [5,6 DIHYDRO 5,5 DIMETHYL 8 (4 METHYLPHENYL) 2 NAPHTHYL]ETHYNYL]BENZOIC ACID; AGN 192599; ALITRETINOIN; ALRT 1150; BEXAROTENE; RETINOIC ACID; RETINOIC ACID RECEPTOR; RETINOID; RETINOID X RECEPTOR; TAZAROTENE; UNCLASSIFIED DRUG;

ACNE; CANCER INHIBITION; CONFERENCE PAPER; DERMATOLOGY; DRUG DESIGN; DRUG EFFICACY; DRUG POTENCY; DRUG RECEPTOR BINDING; PRIORITY JOURNAL; PSORIASIS; RECEPTOR AFFINITY; TRANSCRIPTION REGULATION;

EID: 0032902636     PISSN: 0366077X     EISSN: None     Source Type: Journal    
DOI: 10.1046/j.1365-2133.1999.140s54012.x     Document Type: Conference Paper

References (20)

1. Zhang L, Nadzan AM, Heyman RA et al. Discovery of novel retinoic acid receptor agonists having potent antiproliferative activity in cervical cancer cells. J Med Chem 1996; 39: 2659-63.
2. Nagpal S, Chandraratna RAS. Retinoids as anti-cancer agents. Curr Pharmaceut Design 1996; 2: 295-316.
3. Pfahl M. Nuclear retinoid receptors as central regulators of retinoid response pathways. In; Dermatology Progress and Perspectives (Burgdorf WHC, Katz SI, eds.). New York; Parthenon Publishing Group, 1993; 155-9.
4. Mangelsdorf DJ, Umesono K, Evans RM. The retinoid receptors. In: The Retinoids; Biology, Chemistry, and Medicine (Sporn MB, Roberts AB, Goodman DS, eds.). New York; Raven Press, 1994; 319-49.
5. Klein ES, Pino ME, Johnson AT et al. Identification and functional separation of retinoic acid receptor neutral antagonists and inverse agonists. J Biol Chem 1996; 271: 22692-6.
6. Esgleyes-Ribot T, Chandraratna RA, Lew-Kaya DA, Sefton J, Duvic M. Response of psoriasis to a new topical retinoid. AGN 190168. J Am Acad Dermatol 1994; 30: 581-90.
7. Weinstein GD, Krueger GC, Lowe NJ et al. Tazarotene gel, a new retinoid, for topical therapy of psoriasis; vehicle-controlled study of safety, efficacy, and duration of therapeutic effect. J Am Acad Dermatol 1997; 37: 85-92.
8. Thiboutot DM, Acne. An overview of clinical research findings. Derm Clin 1997; 15: 97-109.
9. Shalita A, Chalker D, Griffith R et al. Double-blind study of AGN 190168, a new retinoid gel, in the topical treatment of acne vulgaris; a multicenter trial. J Invest Dermatol 1993; 100: 542. Abstract 325.
10. Standeven AM, Johnson AT, Escobar M, Chandraratna RAS. Specific antagonist of retinoid toxicity in mice. Toxicol Appl Pharmacol 1996; 138: 169-75.
11. Nagpal S, Thacher SM, Patel S et al. Negative regulation of two hyperproliferative keratinocyte differentiation markers by a retinoic acid receptor-specific retinoid: insight into the mechanism of retinoid action in psoriasis. Cell Growth Differentiation 1996; 7: 1783-91.
12. Shalinsky DR, Bischoff ED, Lamph WW et al. A novel retinoic acid receptor-selective retinoid. ALRT1550, has potent antitumor activity against human oral squamous carcinoma xenografts in nude mice. Cancer Res 1997; 57: 162-8.
13. Anzano MA, Byers SW, Smith JM et al. Prevention of breast cancer in the rat with 9-cis-retinoic acid as a single agent and in combination with tamoxifen. Cancer Res 1994; 54: 4614-17.
14. Gottardis MM, Bischoff ED, Shirley MA et al. Chemoprevention of mammary carcinoma by LGD1069 (Targretin): an RXR-selective ligand. Cancer Res 1996; 56: 5566-70.
15. Nagpal S, Cai J, Zheng T et al. Retinoid antagonism of NF-IL6: insight into the mechanism of antiproliferative effects of retinoids in Kaposi's sarcoma. Mol Cell Biol 1997; 17: 4159-68.
16. Huang ME, Ye YC, Chen SR et al. Use of all-trans retinoic acid in the treatment of acute promyelocytic leukemia. Blood 1988; 72: 567-72.
17. Han QX, Allegretto EA, Shao ZM et al. Elevated expression of retinoic acid receptor-alpha (RAR alpha) in estrogen-receptor-positive breast carcinomas as detected by immunohistochemistry. Diagn Mol Path 1997; 6: 42-8.
18. Fitzgerald P, Teng M, Chandraratna RAS, Heyman RA, Allegretto EA. Retinoic acid receptor alpha expression correlates with retinoid-induced growth inhibition of human breast cancer cells regardless of estrogen receptor status. Cancer Res 1997; 57: 2642-50.
19. Mukherjee R, Davies PJA, Crombie DL et al. Sensitization of diabetic and obese mice to insulin by retinoid X receptor agonists. Nature 1997; 386: 407-10.
20. Agarwal C, Chandraratna RAS, Johnson AT et al. AGN193109 is a highly effective antagonist of retinoid action in human ectocervical epithelial cells. J Biol Chem 1996; 24: 12209-12.