Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTK59TV)

• DTT Name: Vitamin D3 receptor (VDR)
• Synonyms: Vitamin D(3) receptor; Nuclear vitamin D receptor; Nuclear receptor subfamily 1 group I member 1; NR1I1; 1,25-dihydroxyvitamin D3 receptor
• Gene Name: VDR
• DTT Type: Successful target; [1]
• BioChemical Class: Nuclear hormone receptor
• UniProt ID: VDR_HUMAN
• TTD ID: T34234
• Sequence:
  MEAMAASTSLPDPGDFDRNVPRICGVCGDRATGFHFNAMTCEGCKGFFRRSMKRKALFTC
  PFNGDCRITKDNRRHCQACRLKRCVDIGMMKEFILTDEEVQRKREMILKRKEEEALKDSL
  RPKLSEEQQRIIAILLDAHHKTYDPTYSDFCQFRPPVRVNDGGGSHPSRPNSRHTPSFSG
  DSSSSCSDHCITSSDMMDSSSFSNLDLSEEDSDDPSVTLELSQLSMLPHLADLVSYSIQK
  VIGFAKMIPGFRDLTSEDQIVLLKSSAIEVIMLRSNESFTMDDMSWTCGNQDYKYRVSDV
  TKAGHSLELIEPLIKFQVGLKKLNLHEEEHVLLMAICIVSPDRPGVQDAALIEAIQDRLS
  NTLQTYIRCRHPPPGSHLLYAKMIQKLADLRSLNEEHSKQYRCLSFQPECSMKLTPLVLE
  VFGNEIS
• Function: Enters the nucleus upon vitamin D3 binding where it forms heterodimers with the retinoid X receptor/RXR. The VDR-RXR heterodimers bind to specific response elements on DNA and activate the transcription of vitamin D3-responsive target genes. Plays a central role in calcium homeostasis. Nuclear receptor for calcitriol, the active form of vitamin D3 which mediates the action of this vitamin on cells.
• KEGG Pathway:
  Endocrine and other factor-regulated calcium reabsorption (hsa04961)
  Mineral absorption (hsa04978)
  Tuberculosis (hsa05152)
• Reactome Pathway: Nuclear Receptor transcription pathway (R-HSA-383280)

Molecular Interaction Atlas (MIA) of This DTT

9 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Calcidiol	DMN4CV5	Hypophosphatemia		Approved	[1]
Calcipotriol	DM03CP7	Psoriasis	EA90	Approved	[2]
Calcitriol	DM8ZVJ7	Congenital alopecia	LC30	Approved	[3]
Cholecalciferol	DMGU74E	Adult acute monocytic leukemia		Approved	[4]
Dihydrotachysterol	DMFB97P	Hypocalcemia	5B5K.1	Approved	[5]
Doxercalciferol	DM6FG1P	Chronic kidney disease	GB61	Approved	[6]
Ergocalciferol	DMHO0AR	Hypoparathyroidism	5A50	Approved	[1]
Falecalcitrol	DMBI9ZJ	Hyperparathyroidism	5A51	Approved	[7]
Paricalcitol	DMYBV3G	Hyperparathyroidism	5A51	Approved	[8]

5 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
S-06911	DMAYTIH	Osteoporosis	FB83.0	Phase 3	[9]
Seocalcitol	DMKL9QO	Rickets	5B57	Phase 3	[10]
Inecalcitol oral	DMU5SZP	Acute myeloid leukaemia	2A60	Phase 2	[11]
CTAP-201	DMHBK6L	Hyperparathyroidism	5A51	Phase 1	[12]
RO-23-7553	DM9PQ2N	Prostate disease	GA91	Phase 1	[13]

12 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID27454349-Compound-100	DM5LOST	N. A.	N. A.	Patented	[14]
PMID27454349-Compound-101	DMQIYM6	N. A.	N. A.	Patented	[14]
PMID27454349-Compound-102	DMEGRMX	N. A.	N. A.	Patented	[14]
PMID27454349-Compound-91	DMAN7CG	N. A.	N. A.	Patented	[14]
PMID27454349-Compound-92	DMOEYVT	N. A.	N. A.	Patented	[14]
PMID27454349-Compound-93	DMCTMB1	N. A.	N. A.	Patented	[14]
PMID27454349-Compound-94	DMK0SIM	N. A.	N. A.	Patented	[14]
PMID27454349-Compound-95	DM17KL2	N. A.	N. A.	Patented	[14]
PMID27454349-Compound-96	DMW0TM1	N. A.	N. A.	Patented	[14]
PMID27454349-Compound-97	DMEXV6L	N. A.	N. A.	Patented	[14]
PMID27454349-Compound-98	DMZKYMI	N. A.	N. A.	Patented	[14]
PMID27454349-Compound-99	DMH0CQU	N. A.	N. A.	Patented	[14]

8 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Atocalcitol	DM7OE9F	Psoriasis vulgaris	EA90	Discontinued in Phase 2	[15]
Lexacalcitol	DMJ3ZT8	Solid tumour/cancer	2A00-2F9Z	Discontinued in Phase 2	[16]
RO-26-9228	DMPB80O	Urinary incontinence	MF50.2	Discontinued in Phase 2	[9]
Tisocalcitate	DMGF35T	Psoriasis vulgaris	EA90	Discontinued in Phase 2	[17]
BXL-746	DMUD6IK	Inflammation	1A00-CA43.1	Discontinued in Phase 1	[18]
CB-1267	DM75KBM	Prostate cancer	2C82.0	Terminated	[19]
CEP-4186	DMZE0SJ	Acute myeloid leukaemia	2A60	Terminated	[20]
Ecalcidene	DMUR1FK	Acne vulgaris	ED80	Terminated	[21]

10 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2MD	DMPJT1C	Discovery agent	N.A.	Investigative	[22]
3-keto-lithocholic acid	DM5LUED	Discovery agent	N.A.	Investigative	[23]
calcitriol-26,23-lactone	DMZ45M6	Discovery agent	N.A.	Investigative	[24]
gemini	DMETRIS	Discovery agent	N.A.	Investigative	[25]
KSP-BCS-1-alpha-CHF2-1624F2-2	DMXBITO	Discovery agent	N.A.	Investigative	[26]
KSP-BCS-1-alpha-CHF2-20-epi-22-oxabishomo-26-OH	DMJV3R7	Discovery agent	N.A.	Investigative	[26]
LG190178	DMO1FCU	Discovery agent	N.A.	Investigative	[27]
MC-1301	DM5RVO0	Discovery agent	N.A.	Investigative	[28]
TEI-9647	DMLDAR4	Discovery agent	N.A.	Investigative	[29]
ZK159222	DMYRHK6	Discovery agent	N.A.	Investigative	[30]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Psoriasis	EA90	Skin	1.08E-01	-0.22	-0.5
Prostate cancer	2C82	Prostate	1.69E-02	-0.23	-0.66
Osteoporosis	FA20	Bone marrow	2.78E-01	0.26	0.81
Acute myelocytic leukaemia	2C82	Bone marrow	1.80E-03	-0.18	-0.42

References

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