Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTF1XSV1)

• DOT Name: Breast cancer type 2 susceptibility protein (BRCA2)
• Synonyms: Fanconi anemia group D1 protein
• Gene Name: BRCA2
• Related Disease:
  Breast-ovarian cancer, familial, susceptibility to, 2
  Familial prostate carcinoma
  Fanconi anemia complementation group D1
  Pancreatic cancer, susceptibility to, 2
  Sarcoma
  Fanconi's anemia
  Hereditary breast ovarian cancer syndrome
• UniProt ID: BRCA2_HUMAN
• PDB ID: 1N0W; 3EU7; 6GY2; 6HQU; 7BDX; 7LDG; 8BR9; 8C3J; 8C3N; 8PBC; 8PBD; 8R2G
• Pfam ID: PF09169 ; PF09103 ; PF09104 ; PF00634 ; PF21318 ; PF09121
• Sequence:
  MPIGSKERPTFFEIFKTRCNKADLGPISLNWFEELSSEAPPYNSEPAEESEHKNNNYEPN
  LFKTPQRKPSYNQLASTPIIFKEQGLTLPLYQSPVKELDKFKLDLGRNVPNSRHKSLRTV
  KTKMDQADDVSCPLLNSCLSESPVVLQCTHVTPQRDKSVVCGSLFHTPKFVKGRQTPKHI
  SESLGAEVDPDMSWSSSLATPPTLSSTVLIVRNEEASETVFPHDTTANVKSYFSNHDESL
  KKNDRFIASVTDSENTNQREAASHGFGKTSGNSFKVNSCKDHIGKSMPNVLEDEVYETVV
  DTSEEDSFSLCFSKCRTKNLQKVRTSKTRKKIFHEANADECEKSKNQVKEKYSFVSEVEP
  NDTDPLDSNVANQKPFESGSDKISKEVVPSLACEWSQLTLSGLNGAQMEKIPLLHISSCD
  QNISEKDLLDTENKRKKDFLTSENSLPRISSLPKSEKPLNEETVVNKRDEEQHLESHTDC
  ILAVKQAISGTSPVASSFQGIKKSIFRIRESPKETFNASFSGHMTDPNFKKETEASESGL
  EIHTVCSQKEDSLCPNLIDNGSWPATTTQNSVALKNAGLISTLKKKTNKFIYAIHDETSY
  KGKKIPKDQKSELINCSAQFEANAFEAPLTFANADSGLLHSSVKRSCSQNDSEEPTLSLT
  SSFGTILRKCSRNETCSNNTVISQDLDYKEAKCNKEKLQLFITPEADSLSCLQEGQCEND
  PKSKKVSDIKEEVLAAACHPVQHSKVEYSDTDFQSQKSLLYDHENASTLILTPTSKDVLS
  NLVMISRGKESYKMSDKLKGNNYESDVELTKNIPMEKNQDVCALNENYKNVELLPPEKYM
  RVASPSRKVQFNQNTNLRVIQKNQEETTSISKITVNPDSEELFSDNENNFVFQVANERNN
  LALGNTKELHETDLTCVNEPIFKNSTMVLYGDTGDKQATQVSIKKDLVYVLAEENKNSVK
  QHIKMTLGQDLKSDISLNIDKIPEKNNDYMNKWAGLLGPISNHSFGGSFRTASNKEIKLS
  EHNIKKSKMFFKDIEEQYPTSLACVEIVNTLALDNQKKLSKPQSINTVSAHLQSSVVVSD
  CKNSHITPQMLFSKQDFNSNHNLTPSQKAEITELSTILEESGSQFEFTQFRKPSYILQKS
  TFEVPENQMTILKTTSEECRDADLHVIMNAPSIGQVDSSKQFEGTVEIKRKFAGLLKNDC
  NKSASGYLTDENEVGFRGFYSAHGTKLNVSTEALQKAVKLFSDIENISEETSAEVHPISL
  SSSKCHDSVVSMFKIENHNDKTVSEKNNKCQLILQNNIEMTTGTFVEEITENYKRNTENE
  DNKYTAASRNSHNLEFDGSDSSKNDTVCIHKDETDLLFTDQHNICLKLSGQFMKEGNTQI
  KEDLSDLTFLEVAKAQEACHGNTSNKEQLTATKTEQNIKDFETSDTFFQTASGKNISVAK
  ESFNKIVNFFDQKPEELHNFSLNSELHSDIRKNKMDILSYEETDIVKHKILKESVPVGTG
  NQLVTFQGQPERDEKIKEPTLLGFHTASGKKVKIAKESLDKVKNLFDEKEQGTSEITSFS
  HQWAKTLKYREACKDLELACETIEITAAPKCKEMQNSLNNDKNLVSIETVVPPKLLSDNL
  CRQTENLKTSKSIFLKVKVHENVEKETAKSPATCYTNQSPYSVIENSALAFYTSCSRKTS
  VSQTSLLEAKKWLREGIFDGQPERINTADYVGNYLYENNSNSTIAENDKNHLSEKQDTYL
  SNSSMSNSYSYHSDEVYNDSGYLSKNKLDSGIEPVLKNVEDQKNTSFSKVISNVKDANAY
  PQTVNEDICVEELVTSSSPCKNKNAAIKLSISNSNNFEVGPPAFRIASGKIVCVSHETIK
  KVKDIFTDSFSKVIKENNENKSKICQTKIMAGCYEALDDSEDILHNSLDNDECSTHSHKV
  FADIQSEEILQHNQNMSGLEKVSKISPCDVSLETSDICKCSIGKLHKSVSSANTCGIFST
  ASGKSVQVSDASLQNARQVFSEIEDSTKQVFSKVLFKSNEHSDQLTREENTAIRTPEHLI
  SQKGFSYNVVNSSAFSGFSTASGKQVSILESSLHKVKGVLEEFDLIRTEHSLHYSPTSRQ
  NVSKILPRVDKRNPEHCVNSEMEKTCSKEFKLSNNLNVEGGSSENNHSIKVSPYLSQFQQ
  DKQQLVLGTKVSLVENIHVLGKEQASPKNVKMEIGKTETFSDVPVKTNIEVCSTYSKDSE
  NYFETEAVEIAKAFMEDDELTDSKLPSHATHSLFTCPENEEMVLSNSRIGKRRGEPLILV
  GEPSIKRNLLNEFDRIIENQEKSLKASKSTPDGTIKDRRLFMHHVSLEPITCVPFRTTKE
  RQEIQNPNFTAPGQEFLSKSHLYEHLTLEKSSSNLAVSGHPFYQVSATRNEKMRHLITTG
  RPTKVFVPPFKTKSHFHRVEQCVRNINLEENRQKQNIDGHGSDDSKNKINDNEIHQFNKN
  NSNQAVAVTFTKCEEEPLDLITSLQNARDIQDMRIKKKQRQRVFPQPGSLYLAKTSTLPR
  ISLKAAVGGQVPSACSHKQLYTYGVSKHCIKINSKNAESFQFHTEDYFGKESLWTGKGIQ
  LADGGWLIPSNDGKAGKEEFYRALCDTPGVDPKLISRIWVYNHYRWIIWKLAAMECAFPK
  EFANRCLSPERVLLQLKYRYDTEIDRSRRSAIKKIMERDDTAAKTLVLCVSDIISLSANI
  SETSSNKTSSADTQKVAIIELTDGWYAVKAQLDPPLLAVLKNGRLTVGQKIILHGAELVG
  SPDACTPLEAPESLMLKISANSTRPARWYTKLGFFPDPRPFPLPLSSLFSDGGNVGCVDV
  IIQRAYPIQWMEKTSSGLYIFRNEREEEKEAAKYVEAQQKRLEALFTKIQEEFEEHEENT
  TKPYLPSRALTRQQVRALQDGAELYEAVKNAADPAYLEGYFSEEQLRALNNHRQMLNDKK
  QAQIQLEIRKAMESAEQKEQGLSRDVTTVWKLRIVSYSKKEKDSVILSIWRPSSDLYSLL
  TEGKRYRIYHLATSKSKSKSERANIQLAATKKTQYQQLPVSDEILFQIYQPREPLHFSKF
  LDPDFQPSCSEVDLIGFVVSVVKKTGLAPFVYLSDECYNLLAIKFWIDLNEDIIKPHMLI
  AASNLQWRPESKSGLLTLFAGDFSVFSASPKEGHFQETFNKMKNTVENIDILCNEAENKL
  MHILHANDPKWSTPTKDCTSGPYTAQIIPGTGNKLLMSSPNCEIYYQSPLSLCMAKRKSV
  STPVSAQMTSKSCKGEKEIDDQKNCKKRRALDFLSRLPLPPPVSPICTFVSPAAQKAFQP
  PRSCGTKYETPIKKKELNSPQMTPFKKFNEISLLESNSIADEELALINTQALLSGSTGEK
  QFISVSESTRTAPTSSEDYLRLKRRCTTSLIKEQESSQASTEECEKNKQDTITTKKYI
• Function: Involved in double-strand break repair and/or homologous recombination. Binds RAD51 and potentiates recombinational DNA repair by promoting assembly of RAD51 onto single-stranded DNA (ssDNA). Acts by targeting RAD51 to ssDNA over double-stranded DNA, enabling RAD51 to displace replication protein-A (RPA) from ssDNA and stabilizing RAD51-ssDNA filaments by blocking ATP hydrolysis. Part of a PALB2-scaffolded HR complex containing RAD51C and which is thought to play a role in DNA repair by HR. May participate in S phase checkpoint activation. Binds selectively to ssDNA, and to ssDNA in tailed duplexes and replication fork structures. May play a role in the extension step after strand invasion at replication-dependent DNA double-strand breaks; together with PALB2 is involved in both POLH localization at collapsed replication forks and DNA polymerization activity. In concert with NPM1, regulates centrosome duplication. Interacts with the TREX-2 complex (transcription and export complex 2) subunits PCID2 and SEM1, and is required to prevent R-loop-associated DNA damage and thus transcription-associated genomic instability. Silencing of BRCA2 promotes R-loop accumulation at actively transcribed genes in replicating and non-replicating cells, suggesting that BRCA2 mediates the control of R-loop associated genomic instability, independently of its known role in homologous recombination.
• Tissue Specificity: Highest levels of expression in breast and thymus, with slightly lower levels in lung, ovary and spleen.
• KEGG Pathway:
  Homologous recombi.tion (hsa03440)
  Fanconi anemia pathway (hsa03460)
  Pathways in cancer (hsa05200)
  Pancreatic cancer (hsa05212)
  Breast cancer (hsa05224)
• Reactome Pathway:
  HDR through Homologous Recombination (HRR) (R-HSA-5685942)
  Resolution of D-loop Structures through Synthesis-Dependent Strand Annealing (SDSA) (R-HSA-5693554)
  Resolution of D-loop Structures through Holliday Junction Intermediates (R-HSA-5693568)
  Homologous DNA Pairing and Strand Exchange (R-HSA-5693579)
  Presynaptic phase of homologous DNA pairing and strand exchange (R-HSA-5693616)
  Meiotic recombination (R-HSA-912446)
  Defective homologous recombination repair (HRR) due to BRCA1 loss of function (R-HSA-9701192)
  Defective HDR through Homologous Recombination Repair (HRR) due to PALB2 loss of BRCA1 binding function (R-HSA-9704331)
  Defective HDR through Homologous Recombination Repair (HRR) due to PALB2 loss of BRCA2/RAD51/RAD51C binding function (R-HSA-9704646)
  Impaired BRCA2 translocation to the nucleus (R-HSA-9709275)
  Impaired BRCA2 binding to RAD51 (R-HSA-9709570)
  Impaired BRCA2 binding to PALB2 (R-HSA-9709603)
  Impaired BRCA2 binding to SEM1 (DSS1) (R-HSA-9763198)
  HDR through MMEJ (alt-NHEJ) (R-HSA-5685939)

Molecular Interaction Atlas (MIA) of This DOT

7 Disease(s) Related to This DOT

Disease Name	Disease ID	Evidence Level	Mode of Inheritance	REF
Breast-ovarian cancer, familial, susceptibility to, 2	DIS78HM9	Definitive	Autosomal dominant	[1]
Familial prostate carcinoma	DISL9KNO	Definitive	Autosomal dominant	[2]
Fanconi anemia complementation group D1	DIS9247K	Definitive	Autosomal recessive	[1]
Pancreatic cancer, susceptibility to, 2	DIS850J4	Strong	Autosomal dominant	[3]
Sarcoma	DISZDG3U	Moderate	Autosomal dominant	[4]
Fanconi's anemia	DISGW6Q8	Supportive	Autosomal recessive	[5]
Hereditary breast ovarian cancer syndrome	DISWDUGU	Supportive	Autosomal dominant	[6]

This DOT Affected the Drug Response of 3 Drug(s)

Drug Name	Drug ID	Highest Status	Interaction	REF
Temozolomide	DMKECZD	Approved	Breast cancer type 2 susceptibility protein (BRCA2) decreases the response to substance of Temozolomide.	[43]
Olaparib	DM8QB1D	Approved	Breast cancer type 2 susceptibility protein (BRCA2) affects the response to substance of Olaparib.	[44]
	DM9CEI5		Breast cancer type 2 susceptibility protein (BRCA2) decreases the response to substance of .	[43]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Valproate	DMCFE9I	Approved	Valproate decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[7]
Ciclosporin	DMAZJFX	Approved	Ciclosporin decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[8]
Tretinoin	DM49DUI	Approved	Tretinoin decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[9]
Acetaminophen	DMUIE76	Approved	Acetaminophen increases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[10]
Doxorubicin	DMVP5YE	Approved	Doxorubicin decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[11]
Cisplatin	DMRHGI9	Approved	Cisplatin increases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[12]
Estradiol	DMUNTE3	Approved	Estradiol increases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[13]
Quercetin	DM3NC4M	Approved	Quercetin decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[14]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[15]
Calcitriol	DM8ZVJ7	Approved	Calcitriol decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[16]
Vorinostat	DMWMPD4	Approved	Vorinostat increases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[17]
Testosterone	DM7HUNW	Approved	Testosterone decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[16]
Marinol	DM70IK5	Approved	Marinol increases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[18]
Zoledronate	DMIXC7G	Approved	Zoledronate increases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[19]
Folic acid	DMEMBJC	Approved	Folic acid decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[20]
Demecolcine	DMCZQGK	Approved	Demecolcine decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[21]
Cannabidiol	DM0659E	Approved	Cannabidiol decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[22]
Bortezomib	DMNO38U	Approved	Bortezomib decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[23]
Azathioprine	DMMZSXQ	Approved	Azathioprine decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[24]
Cytarabine	DMZD5QR	Approved	Cytarabine increases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[25]
Dasatinib	DMJV2EK	Approved	Dasatinib decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[26]
Lucanthone	DMZLBUO	Approved	Lucanthone decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[27]
Resveratrol	DM3RWXL	Phase 3	Resveratrol decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[28]
Tamibarotene	DM3G74J	Phase 3	Tamibarotene decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[9]
Fenretinide	DMRD5SP	Phase 3	Fenretinide decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[29]
Camptothecin	DM6CHNJ	Phase 3	Camptothecin decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[11]
I3C	DMIGFOR	Phase 3	I3C increases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[30]
Abexinostat	DM91LGU	Phase 3	Abexinostat decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[31]
Genistein	DM0JETC	Phase 2/3	Genistein increases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[30]
PEITC	DMOMN31	Phase 2	PEITC decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[32]
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene increases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[33]
(+)-JQ1	DM1CZSJ	Phase 1	(+)-JQ1 decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[34]
PMID28460551-Compound-2	DM4DOUB	Patented	PMID28460551-Compound-2 decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[36]
SCH 727965	DMCJLD1	Discontinued in Phase 3	SCH 727965 decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[38]
THAPSIGARGIN	DMDMQIE	Preclinical	THAPSIGARGIN increases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[30]
PJ34	DMXO6YH	Preclinical	PJ34 decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[39]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[14]
Trichostatin A	DM9C8NX	Investigative	Trichostatin A decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[40]
Coumestrol	DM40TBU	Investigative	Coumestrol increases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[13]
geraniol	DMS3CBD	Investigative	geraniol decreases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[41]
[3H]methyltrienolone	DMTSGOW	Investigative	[3H]methyltrienolone increases the expression of Breast cancer type 2 susceptibility protein (BRCA2).	[42]

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

Drug Name	Drug ID	Highest Status	Interaction	REF
TAK-243	DM4GKV2	Phase 1	TAK-243 decreases the sumoylation of Breast cancer type 2 susceptibility protein (BRCA2).	[35]
PMID28870136-Compound-52	DMFDERP	Patented	PMID28870136-Compound-52 affects the phosphorylation of Breast cancer type 2 susceptibility protein (BRCA2).	[37]

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