Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OT4GLCXW)

• DOT Name: Fibroblast growth factor receptor 1 (FGFR1)
• Synonyms: FGFR-1; EC 2.7.10.1; Basic fibroblast growth factor receptor 1; BFGFR; bFGF-R-1; Fms-like tyrosine kinase 2; FLT-2; N-sam; Proto-oncogene c-Fgr; CD antigen CD331
• Gene Name: FGFR1
• Related Disease:
  Encephalocraniocutaneous lipomatosis
  Hartsfield-Bixler-Demyer syndrome
  Hypogonadotropic hypogonadism 2 with or without anosmia
  Hypogonadotropic hypogonadism 7 with or without anosmia
  Osteoglophonic dwarfism
  Pfeiffer syndrome
  Pfeiffer syndrome type 1
  Jackson-Weiss syndrome
  Holoprosencephaly
  Hypogonadotropic hypogonadism
  Isolated trigonocephaly
  Kallmann syndrome
  Septooptic dysplasia
  Tooth agenesis
• UniProt ID: FGFR1_HUMAN
• PDB ID: 1AGW ; 1CVS ; 1EVT ; 1FGI ; 1FGK ; 1FQ9 ; 1XR0 ; 2CR3 ; 2FGI ; 3C4F ; 3DPK ; 3GQI ; 3GQL ; 3JS2 ; 3KRJ ; 3KRL ; 3KXX ; 3KY2 ; 3OJV ; 3RHX ; 3TT0 ; 4F63 ; 4F64 ; 4F65 ; 4NK9 ; 4NKA ; 4NKS ; 4RWI ; 4RWJ ; 4RWK ; 4RWL ; 4UWB ; 4UWC ; 4UWY ; 4V01 ; 4V04 ; 4V05 ; 4WUN ; 4ZSA ; 5A46 ; 5A4C ; 5AM6 ; 5AM7 ; 5B7V ; 5EW8 ; 5FLF ; 5O49 ; 5O4A ; 5UQ0 ; 5UR1 ; 5VND ; 5W21 ; 5W59 ; 5Z0S ; 5ZV2 ; 6C18 ; 6C19 ; 6C1B ; 6C1C ; 6C1O ; 6ITJ ; 6MZQ ; 6MZW ; 6NVL ; 6P68 ; 6P69 ; 7OZB ; 7OZD ; 7OZF ; 7WCL ; 7YSH
• EC Number: 2.7.10.1
• Pfam ID: PF07679 ; PF00047 ; PF07714
• Sequence:
  MWSWKCLLFWAVLVTATLCTARPSPTLPEQAQPWGAPVEVESFLVHPGDLLQLRCRLRDD
  VQSINWLRDGVQLAESNRTRITGEEVEVQDSVPADSGLYACVTSSPSGSDTTYFSVNVSD
  ALPSSEDDDDDDDSSSEEKETDNTKPNRMPVAPYWTSPEKMEKKLHAVPAAKTVKFKCPS
  SGTPNPTLRWLKNGKEFKPDHRIGGYKVRYATWSIIMDSVVPSDKGNYTCIVENEYGSIN
  HTYQLDVVERSPHRPILQAGLPANKTVALGSNVEFMCKVYSDPQPHIQWLKHIEVNGSKI
  GPDNLPYVQILKTAGVNTTDKEMEVLHLRNVSFEDAGEYTCLAGNSIGLSHHSAWLTVLE
  ALEERPAVMTSPLYLEIIIYCTGAFLISCMVGSVIVYKMKSGTKKSDFHSQMAVHKLAKS
  IPLRRQVTVSADSSASMNSGVLLVRPSRLSSSGTPMLAGVSEYELPEDPRWELPRDRLVL
  GKPLGEGCFGQVVLAEAIGLDKDKPNRVTKVAVKMLKSDATEKDLSDLISEMEMMKMIGK
  HKNIINLLGACTQDGPLYVIVEYASKGNLREYLQARRPPGLEYCYNPSHNPEEQLSSKDL
  VSCAYQVARGMEYLASKKCIHRDLAARNVLVTEDNVMKIADFGLARDIHHIDYYKKTTNG
  RLPVKWMAPEALFDRIYTHQSDVWSFGVLLWEIFTLGGSPYPGVPVEELFKLLKEGHRMD
  KPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRIVALTSNQEYLDLSMPLDQYSPSF
  PDTRSSTCSSGEDSVFSHEPLPEEPCLPRHPAQLANGGLKRR
• Function: Tyrosine-protein kinase that acts as a cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic development, cell proliferation, differentiation and migration. Required for normal mesoderm patterning and correct axial organization during embryonic development, normal skeletogenesis and normal development of the gonadotropin-releasing hormone (GnRH) neuronal system. Phosphorylates PLCG1, FRS2, GAB1 and SHB. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. Phosphorylation of FRS2 triggers recruitment of GRB2, GAB1, PIK3R1 and SOS1, and mediates activation of RAS, MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. Promotes phosphorylation of SHC1, STAT1 and PTPN11/SHP2. In the nucleus, enhances RPS6KA1 and CREB1 activity and contributes to the regulation of transcription. FGFR1 signaling is down-regulated by IL17RD/SEF, and by FGFR1 ubiquitination, internalization and degradation.
• Tissue Specificity: Detected in astrocytoma, neuroblastoma and adrenal cortex cell lines. Some isoforms are detected in foreskin fibroblast cell lines, however isoform 17, isoform 18 and isoform 19 are not detected in these cells.
• KEGG Pathway:
  MAPK sig.ling pathway (hsa04010)
  Ras sig.ling pathway (hsa04014)
  Rap1 sig.ling pathway (hsa04015)
  Calcium sig.ling pathway (hsa04020)
  PI3K-Akt sig.ling pathway (hsa04151)
  Adherens junction (hsa04520)
  Sig.ling pathways regulating pluripotency of stem cells (hsa04550)
  Thermogenesis (hsa04714)
  Regulation of actin cytoskeleton (hsa04810)
  Parathyroid hormone synthesis, secretion and action (hsa04928)
  Pathways in cancer (hsa05200)
  Proteoglycans in cancer (hsa05205)
  Prostate cancer (hsa05215)
  Melanoma (hsa05218)
  Breast cancer (hsa05224)
  Central carbon metabolism in cancer (hsa05230)
• Reactome Pathway:
  PIP3 activates AKT signaling (R-HSA-1257604)
  Signaling by FGFR1 amplification mutants (R-HSA-1839120)
  Signaling by activated point mutants of FGFR1 (R-HSA-1839122)
  Constitutive Signaling by Aberrant PI3K in Cancer (R-HSA-2219530)
  Phospholipase C-mediated cascade (R-HSA-5654219)
  Downstream signaling of activated FGFR1 (R-HSA-5654687)
  SHC-mediated cascade (R-HSA-5654688)
  PI-3K cascade (R-HSA-5654689)
  FRS-mediated FGFR1 signaling (R-HSA-5654693)
  Negative regulation of FGFR1 signaling (R-HSA-5654726)
  Signaling by FGFR1 in disease (R-HSA-5655302)
  RAF/MAP kinase cascade (R-HSA-5673001)
  PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling (R-HSA-6811558)
  Signaling by plasma membrane FGFR1 fusions (R-HSA-8853336)
  Epithelial-Mesenchymal Transition (EMT) during gastrulation (R-HSA-9758919)
  Formation of paraxial mesoderm (R-HSA-9793380)
  PI3K Cascade (R-HSA-109704)

Molecular Interaction Atlas (MIA) of This DOT

14 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Encephalocraniocutaneous lipomatosis	DIST7LTP	Definitive	Somatic mosaicism	[1]
Hartsfield-Bixler-Demyer syndrome	DISS66AG	Definitive	Autosomal dominant	[2]
Hypogonadotropic hypogonadism 2 with or without anosmia	DISRVFVX	Definitive	Autosomal dominant	[3]
Hypogonadotropic hypogonadism 7 with or without anosmia	DISPBWEU	Definitive	Autosomal dominant	[4]
Osteoglophonic dwarfism	DISVSNPT	Definitive	Autosomal dominant	[5]
Pfeiffer syndrome	DISA0GA5	Definitive	Autosomal dominant	[6]
Pfeiffer syndrome type 1	DISA0WVT	Definitive	Autosomal dominant	[7]
Jackson-Weiss syndrome	DISRNZHH	Strong	Autosomal dominant	[8]
Holoprosencephaly	DISR35EC	Supportive	Autosomal recessive	[9]
Hypogonadotropic hypogonadism	DIS8JSKR	Supportive	Autosomal dominant	[10]
Isolated trigonocephaly	DISIEY3W	Supportive	Autosomal dominant	[11]
Kallmann syndrome	DISO3HDG	Supportive	Autosomal dominant	[10]
Septooptic dysplasia	DISXYR1H	Supportive	Autosomal dominant	[12]
Tooth agenesis	DIS1PWC7	Supportive	Autosomal dominant	[13]

This DOT Affected the Drug Response of 1 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Methotrexate	DM2TEOL	Approved	Fibroblast growth factor receptor 1 (FGFR1) affects the response to substance of Methotrexate.	[50]

3 Drug(s) Affected the Post-Translational Modifications of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate increases the methylation of Fibroblast growth factor receptor 1 (FGFR1).	[14]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the methylation of Fibroblast growth factor receptor 1 (FGFR1).	[38]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the methylation of Fibroblast growth factor receptor 1 (FGFR1).	[42]

39 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Ciclosporin	DMAZJFX	Approved	Ciclosporin decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[15]
Tretinoin	DM49DUI	Approved	Tretinoin decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[16]
Acetaminophen	DMUIE76	Approved	Acetaminophen increases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[17]
Doxorubicin	DMVP5YE	Approved	Doxorubicin decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[18]
Cisplatin	DMRHGI9	Approved	Cisplatin decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[19]
Estradiol	DMUNTE3	Approved	Estradiol decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[20]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[21]
Hydrogen peroxide	DM1NG5W	Approved	Hydrogen peroxide decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[22]
Calcitriol	DM8ZVJ7	Approved	Calcitriol decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[23]
Vorinostat	DMWMPD4	Approved	Vorinostat decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[24]
Carbamazepine	DMZOLBI	Approved	Carbamazepine affects the expression of Fibroblast growth factor receptor 1 (FGFR1).	[25]
Decitabine	DMQL8XJ	Approved	Decitabine decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[26]
Folic acid	DMEMBJC	Approved	Folic acid decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[27]
Isotretinoin	DM4QTBN	Approved	Isotretinoin increases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[28]
Diclofenac	DMPIHLS	Approved	Diclofenac affects the expression of Fibroblast growth factor receptor 1 (FGFR1).	[25]
Malathion	DMXZ84M	Approved	Malathion increases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[29]
Thalidomide	DM70BU5	Approved	Thalidomide affects the expression of Fibroblast growth factor receptor 1 (FGFR1).	[30]
Pomalidomide	DMTGBAX	Approved	Pomalidomide decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[30]
Lenalidomide	DM6Q7U4	Approved	Lenalidomide affects the expression of Fibroblast growth factor receptor 1 (FGFR1).	[30]
Urea	DMUK75B	Approved	Urea decreases the activity of Fibroblast growth factor receptor 1 (FGFR1).	[32]
Urethane	DM7NSI0	Phase 4	Urethane increases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[33]
HIF-1alpha	DM4OQRD	Phase 4	HIF-1alpha decreases the activity of Fibroblast growth factor receptor 1 (FGFR1).	[34]
SNDX-275	DMH7W9X	Phase 3	SNDX-275 increases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[24]
Resveratrol	DM3RWXL	Phase 3	Resveratrol increases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[35]
Tamibarotene	DM3G74J	Phase 3	Tamibarotene decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[16]
Chlorpromazine	DMBGZI3	Phase 3 Trial	Chlorpromazine decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[36]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[39]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[40]
PMID25656651-Compound-5	DMAI95U	Patented	PMID25656651-Compound-5 decreases the activity of Fibroblast growth factor receptor 1 (FGFR1).	[41]
Formaldehyde	DM7Q6M0	Investigative	Formaldehyde increases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[43]
Coumestrol	DM40TBU	Investigative	Coumestrol decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[20]
4-hydroxy-2-nonenal	DM2LJFZ	Investigative	4-hydroxy-2-nonenal decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[22]
Forskolin	DM6ITNG	Investigative	Forskolin increases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[44]
ELLAGIC ACID	DMX8BS5	Investigative	ELLAGIC ACID decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[35]
Paraoxon	DMN4ZKC	Investigative	Paraoxon decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[45]
Taurine	DMVW7N3	Investigative	Taurine decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[46]
Z-Pro-Prolinal	DM43O2U	Investigative	Z-Pro-Prolinal decreases the expression of Fibroblast growth factor receptor 1 (FGFR1).	[47]
SU5402	DM9JON3	Investigative	SU5402 decreases the activity of Fibroblast growth factor receptor 1 (FGFR1).	[48]
PD173074	DMP0N4U	Investigative	PD173074 decreases the activity of Fibroblast growth factor receptor 1 (FGFR1).	[49]

2 Drug(s) Affected the Protein Interaction/Cellular Processes of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Ardeparin	DMYRX8B	Approved	Ardeparin affects the binding of Fibroblast growth factor receptor 1 (FGFR1).	[31]
PIPERINE	DMYEAB1	Phase 1/2	PIPERINE affects the binding of Fibroblast growth factor receptor 1 (FGFR1).	[37]

References

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