Target Information

Target General Information

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Target ID

T11822 (Former ID: TTDS00072)

Target Name

Retinoic acid receptor (RAR)

Synonyms

Retinoic acid receptor

Click to Show/Hide

Gene Name

NO-GeName

Target Type

Successful target

[1]

Disease

[+] 3 Target-related Diseases

Acne vulgaris [ICD-11: ED80]

Acute myeloid leukaemia [ICD-11: 2A60]

Light sensitivity impairment [ICD-11: 9D45]

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Approved Drug(s)

[+] 4 Approved Drugs

Adapalene

Drug Info

Approved

Acne vulgaris

[2], [3]

Isotretinoin

Drug Info

Approved

Acne vulgaris

[4], [5]

Tretinoin

Drug Info

Approved

Acne vulgaris

[5], [6]

Vitamin A

Drug Info

Approved

Night blindness

[7], [8]

Clinical Trial Drug(s)

[+] 5 Clinical Trial Drugs

13-cis-retinoic acid

Drug Info

Phase 3

Glioma

[9]

Fenretinide

Drug Info

Phase 3

Macular degeneration

[10]

Peretinoin

Drug Info

Phase 3

Hepatocellular carcinoma

[11]

Velac Gel

Drug Info

Phase 3

Acne vulgaris

[9]

Amsilarotene

Drug Info

Phase 2

Solid tumour/cancer

[12]

Discontinued Drug(s)

[+] 5 Discontinued Drugs

LAS-41001

Drug Info

Discontinued in Preregistration

Rosacea

[13]

IRX-4310

Drug Info

Discontinued in Phase 3

Psoriasis vulgaris

[14]

BMY-30123

Drug Info

Discontinued in Phase 2

Acne vulgaris

[15]

LG-1550

Drug Info

Discontinued in Phase 2

Solid tumour/cancer

[16], [17]

MX-781

Drug Info

Terminated

Breast cancer

[18]

Mode of Action

[+] 5 Modes of Action

Binder

[+] 3 Binder drugs

Adapalene

Drug Info

[19], [20]

Tretinoin

Drug Info

[21]

Vitamin A

Drug Info

[8]

Agonist

[+] 1 Agonist drugs

Isotretinoin

Drug Info

[1]

Modulator

[+] 7 Modulator drugs

13-cis-retinoic acid

Drug Info

[22], [23]

Fenretinide

Drug Info

[24]

Peretinoin

Drug Info

[25]

LAS-41001

Drug Info

[28]

BMY-30123

Drug Info

[23], [30]

LG-1550

Drug Info

[31]

MX-781

Drug Info

[32]

Inhibitor

[+] 1 Inhibitor drugs

Velac Gel

Drug Info

[26]

Antagonist

[+] 2 Antagonist drugs

Amsilarotene

Drug Info

[27]

IRX-4310

Drug Info

[29]

Drug Property Profile of Target

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(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

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Co-Targets

Co-Targets Info

Target-Related Models and Studies

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Target Validation

Target Validation Info

References

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REF 1

Retinoid agonist isotretinoin ameliorates obstructive renal injury. J Urol. 2003 Oct;170(4 Pt 1):1398-402.

REF 2

URL: 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 3

Topical retinoids in acne vulgaris: update on efficacy and safety. Am J Clin Dermatol. 2008;9(6):369-81.

REF 4

REF 5

Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77.

REF 6

REF 7

REF 8

Vitamins and cofactors: highlights of ESBOC 2009. Nat Chem Biol. 2009 Aug;5(8):530-3.

REF 9

Chromosomal 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 10

ClinicalTrials.gov (NCT00003075) Fenretinide in Treating Patients With Cervical Neoplasia. U.S. National Institutes of Health.

REF 11

ClinicalTrials.gov (NCT01640808) Study of Peretinoin for Suppressing Recurrence of HCV-positive HCC. U.S. National Institutes of Health.

REF 12

ClinicalTrials.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 13

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027956)

REF 14

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009573)

REF 15

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003321)

REF 16

REF 17

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007857)

REF 18

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011240)

REF 19

A review of adapalene in the treatment of acne vulgaris. J Adolesc Health. 2008 Nov;43(5):421-4.

REF 20

Topical treatment in acne: current status and future aspects. Dermatology. 2003;206(1):29-36.

REF 21

Retinoids--which dermatological indications will benefit in the near future Skin Pharmacol Appl Skin Physiol. 2001 Sep-Oct;14(5):303-15.

REF 22

13-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 23

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 24

National Cancer Institute Drug Dictionary (drug id 39582).

REF 25

Peretinoin, 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 26

Chromosomal 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 27

Initial 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 28

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027956)

REF 29

An 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 30

The pharmacology of a novel topical retinoid, BMY 30123: comparison with tretinoin. J Pharm Pharmacol. 1992 May;44(5):379-86.

REF 31

US 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 32

The 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.

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