Target Information

Target General Infomation
Target ID
T11822
Former ID
TTDS00072
Target Name
Retinoic acid receptor
Target Type
Successful
Disease Acute promyelocytic leukemia [ICD9: 205; ICD10: C92.4]
Acne vulgaris [ICD9: 706.1; ICD10: L70.0]
Breast cancer [ICD9: 174, 175; ICD10: C50]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Glioma [ICD9: 191; ICD10: C71]
Hepatocellular carcinoma [ICD9: 155; ICD10: C22.0]
Macular degeneration [ICD9: 362.5; ICD10: H35.3]
Night blindness [ICD9: 368.6; ICD10: H53.6]
Psoriasis [ICD9: 696; ICD10: L40]
Rosacea [ICD10: L71]
BioChemical Class
Zinc-finger
Target Validation
T11822
Drugs and Mode of Action
Drug(s) Adapalene Drug Info Approved Acne vulgaris [536911], [540832]
Isotretinoin Drug Info Approved Acne vulgaris [536361], [542589]
Tretinoin Drug Info Approved Acne vulgaris [536361], [539710]
Vitamin A Drug Info Approved Night blindness [537623], [540652]
13-cis-retinoic acid, UCSD Drug Info Phase 3 Glioma [525348]
Fenretinide Drug Info Phase 3 Macular degeneration [521449]
Peretinoin Drug Info Phase 3 Hepatocellular carcinoma [523972]
Velac Gel Drug Info Phase 3 Acne vulgaris [525348]
Amsilarotene Drug Info Phase 2 Cancer [522335]
Tretinoin Drug Info Phase 2 Acute promyelocytic leukemia [525348], [539710]
LAS-41001 Drug Info Discontinued in Preregistration Rosacea [548717]
IRX-4310 Drug Info Discontinued in Phase 3 Psoriasis [546671]
BMY-30123 Drug Info Discontinued in Phase 2 Acne vulgaris [545453]
LG-1550 Drug Info Discontinued in Phase 2 Cancer [539785], [546388]
MX-781 Drug Info Terminated Breast cancer [546931]
Modulator 13-cis-retinoic acid, UCSD Drug Info [525851], [551871]
BMY-30123 Drug Info [526777], [551871]
Fenretinide Drug Info [550397]
LAS-41001 Drug Info [548718]
LG-1550 Drug Info [550887]
MX-781 Drug Info [527172]
Peretinoin Drug Info [532310]
Binder Adapalene Drug Info [535694], [536877]
Tretinoin Drug Info [535273]
Vitamin A Drug Info [537623]
Antagonist Amsilarotene Drug Info [526402]
IRX-4310 Drug Info [527142]
Agonist Isotretinoin Drug Info [535834]
Inhibitor Velac Gel Drug Info [525349]
References
Ref 521449ClinicalTrials.gov (NCT00003075) Fenretinide in Treating Patients With Cervical Neoplasia. U.S. National Institutes of Health.
Ref 522335ClinicalTrials.gov (NCT00687596) Study of TAC-101 as Second Line Treatment in Patients With Advanced Hepatocellular Carcinoma Who Received Sorafenib as First Line Therapy. U.S. National Institutes ofHealth.
Ref 523972ClinicalTrials.gov (NCT01640808) Study of Peretinoin for Suppressing Recurrence of HCV-positive HCC. U.S. National Institutes of Health.
Ref 525348Chromosomal translocation t(15;17) in human acute promyelocytic leukemia fuses RAR alpha with a novel putative transcription factor, PML. Cell. 1991 Aug 23;66(4):663-74.
Ref 536361Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20.
Ref 536911Topical retinoids in acne vulgaris: update on efficacy and safety. Am J Clin Dermatol. 2008;9(6):369-81. doi: 10.2165/0128071-200809060-00003.
Ref 537623Vitamins and cofactors: highlights of ESBOC 2009. Nat Chem Biol. 2009 Aug;5(8):530-3.
Ref 539710(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2644).
Ref 539785(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2740).
Ref 540652(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4053).
Ref 540832(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5429).
Ref 542589(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7600).
Ref 545453Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003321)
Ref 546388Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007857)
Ref 546671Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009573)
Ref 546931Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011240)
Ref 548717Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027956)
Ref 525349Chromosomal translocation t(15;17) in human acute promyelocytic leukemia fuses RAR alpha with a novel putative transcription factor, PML. Cell. 1991 Aug 23;66(4):663-74.
Ref 52585113-cis retinoic acid exerts its specific activity on human sebocytes through selective intracellular isomerization to all-trans retinoic acid and binding to retinoid acid receptors. J Invest Dermatol. 2000 Aug;115(2):321-7.
Ref 526402Initial clinical trial of oral TAC-101, a novel retinoic acid receptor-alpha selective retinoid, in patients with advanced cancer. J Clin Oncol. 2002 Aug 15;20(16):3522-32.
Ref 526777The pharmacology of a novel topical retinoid, BMY 30123: comparison with tretinoin. J Pharm Pharmacol. 1992 May;44(5):379-86.
Ref 527142An antagonist of retinoic acid receptors more effectively inhibits growth of human prostate cancer cells than normal prostate epithelium. Br J Cancer. 2004 Aug 2;91(3):580-8.
Ref 527172The retinoid antagonist MX781 induces clusterin expression in prostate cancer cells via heat shock factor-1 and activator protein-1 transcription factors. Cancer Res. 2004 Aug 15;64(16):5905-12.
Ref 532310Peretinoin, an acyclic retinoid, improves the hepatic gene signature of chronic hepatitis C following curative therapy of hepatocellular carcinoma. BMC Cancer. 2013 Apr 15;13:191.
Ref 535273Retinoids--which dermatological indications will benefit in the near future? Skin Pharmacol Appl Skin Physiol. 2001 Sep-Oct;14(5):303-15.
Ref 535694Topical treatment in acne: current status and future aspects. Dermatology. 2003;206(1):29-36.
Ref 535834Retinoid agonist isotretinoin ameliorates obstructive renal injury. J Urol. 2003 Oct;170(4 Pt 1):1398-402.
Ref 536877A review of adapalene in the treatment of acne vulgaris. J Adolesc Health. 2008 Nov;43(5):421-4.
Ref 537623Vitamins and cofactors: highlights of ESBOC 2009. Nat Chem Biol. 2009 Aug;5(8):530-3.
Ref 548718Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027956)
Ref 550397National Cancer Institute Drug Dictionary (drug id 39582).
Ref 550887US patent application no. 2005,0014,729, Method for the treatment or prevention of dermatological disorders with a cyclooxygenase-2 inhibitor alone and in combination with a dermatological treatment agent and compositions therewith.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

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