General Information of Drug Off-Target (DOT) (ID: OT5BZ1J9)

DOT Name Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1)
Synonyms
PI3-kinase regulatory subunit alpha; PI3K regulatory subunit alpha; PtdIns-3-kinase regulatory subunit alpha; Phosphatidylinositol 3-kinase 85 kDa regulatory subunit alpha; PI3-kinase subunit p85-alpha; PtdIns-3-kinase regulatory subunit p85-alpha
Gene Name PIK3R1
Related Disease
Agammaglobulinemia 7, autosomal recessive ( )
Immunodeficiency 36 ( )
Prostate cancer ( )
SHORT syndrome ( )
Adult glioblastoma ( )
Agammaglobulinemia ( )
Alcohol dependence ( )
Bladder cancer ( )
Brain neoplasm ( )
Breast cancer ( )
Breast carcinoma ( )
Breast neoplasm ( )
Bronchiectasis ( )
Bruton-type agammaglobulinemia ( )
Colon cancer ( )
Colorectal carcinoma ( )
Colorectal neoplasm ( )
Cutaneous melanoma ( )
Endometrial cancer ( )
Endometrial carcinoma ( )
Exanthem ( )
Glioma ( )
Hepatocellular carcinoma ( )
Hyperglycemia ( )
Immunodeficiency 14 ( )
Lipodystrophy ( )
Lung cancer ( )
Lung carcinoma ( )
Ovarian cancer ( )
Prostate carcinoma ( )
Prostate neoplasm ( )
Rieger anomaly ( )
Type-1/2 diabetes ( )
Urinary bladder cancer ( )
Urinary bladder neoplasm ( )
Vitiligo ( )
Burkitt lymphoma ( )
Immunodeficiency ( )
Non-insulin dependent diabetes ( )
Activated PI3K-delta syndrome ( )
Autosomal agammaglobulinemia ( )
High blood pressure ( )
Undifferentiated carcinoma ( )
Carcinoma ( )
Clear cell renal carcinoma ( )
Colon carcinoma ( )
Non-small-cell lung cancer ( )
Obesity ( )
UniProt ID
P85A_HUMAN
3D Structure
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2D Sequence (FASTA)
Download
3D Structure (PDB)
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PDB ID
1A0N ; 1AZG ; 1H9O ; 1PBW ; 1PHT ; 1PIC ; 1PKS ; 1PKT ; 2IUG ; 2IUH ; 2IUI ; 2RD0 ; 2V1Y ; 3HHM ; 3HIZ ; 3I5R ; 3I5S ; 4A55 ; 4JPS ; 4L1B ; 4L23 ; 4L2Y ; 4OVU ; 4OVV ; 4WAF ; 4YKN ; 4ZOP ; 5AUL ; 5FI4 ; 5GJI ; 5ITD ; 5M6U ; 5SW8 ; 5SWG ; 5SWO ; 5SWP ; 5SWR ; 5SWT ; 5SX8 ; 5SX9 ; 5SXA ; 5SXB ; 5SXC ; 5SXD ; 5SXE ; 5SXF ; 5SXI ; 5SXJ ; 5SXK ; 5UBT ; 5UK8 ; 5UKJ ; 5UL1 ; 5VLR ; 5XGH ; 5XGI ; 5XGJ ; 6NCT ; 6PYR ; 6PYU ; 7CIO ; 7LM2 ; 7LQ1 ; 7MYN ; 7MYO ; 7PG5 ; 7PG6 ; 7RNS ; 7TZ7 ; 8DCP ; 8DCX ; 8DD4 ; 8DD8 ; 8GUB ; 8H36 ; 8H37 ; 8ILR ; 8ILS ; 8ILV ; 8SBC ; 8SBJ ; 8TDU ; 8TGD ; 8TS7 ; 8TS8 ; 8TS9 ; 8TSA ; 8TSB ; 8TSC ; 8TSD ; 8TU6
Pfam ID
PF16454 ; PF00620 ; PF00017
Sequence
MSAEGYQYRALYDYKKEREEDIDLHLGDILTVNKGSLVALGFSDGQEARPEEIGWLNGYN
ETTGERGDFPGTYVEYIGRKKISPPTPKPRPPRPLPVAPGSSKTEADVEQQALTLPDLAE
QFAPPDIAPPLLIKLVEAIEKKGLECSTLYRTQSSSNLAELRQLLDCDTPSVDLEMIDVH
VLADAFKRYLLDLPNPVIPAAVYSEMISLAPEVQSSEEYIQLLKKLIRSPSIPHQYWLTL
QYLLKHFFKLSQTSSKNLLNARVLSEIFSPMLFRFSAASSDNTENLIKVIEILISTEWNE
RQPAPALPPKPPKPTTVANNGMNNNMSLQDAEWYWGDISREEVNEKLRDTADGTFLVRDA
STKMHGDYTLTLRKGGNNKLIKIFHRDGKYGFSDPLTFSSVVELINHYRNESLAQYNPKL
DVKLLYPVSKYQQDQVVKEDNIEAVGKKLHEYNTQFQEKSREYDRLYEEYTRTSQEIQMK
RTAIEAFNETIKIFEEQCQTQERYSKEYIEKFKREGNEKEIQRIMHNYDKLKSRISEIID
SRRRLEEDLKKQAAEYREIDKRMNSIKPDLIQLRKTRDQYLMWLTQKGVRQKKLNEWLGN
ENTEDQYSLVEDDEDLPHHDEKTWNVGSSNRNKAENLLRGKRDGTFLVRESSKQGCYACS
VVVDGEVKHCVINKTATGYGFAEPYNLYSSLKELVLHYQHTSLVQHNDSLNVTLAYPVYA
QQRR
Function
Binds to activated (phosphorylated) protein-Tyr kinases, through its SH2 domain, and acts as an adapter, mediating the association of the p110 catalytic unit to the plasma membrane. Necessary for the insulin-stimulated increase in glucose uptake and glycogen synthesis in insulin-sensitive tissues. Plays an important role in signaling in response to FGFR1, FGFR2, FGFR3, FGFR4, KITLG/SCF, KIT, PDGFRA and PDGFRB. Likewise, plays a role in ITGB2 signaling. Modulates the cellular response to ER stress by promoting nuclear translocation of XBP1 isoform 2 in a ER stress- and/or insulin-dependent manner during metabolic overloading in the liver and hence plays a role in glucose tolerance improvement.
Tissue Specificity Isoform 2 is expressed in skeletal muscle and brain, and at lower levels in kidney and cardiac muscle. Isoform 2 and isoform 4 are present in skeletal muscle (at protein level).
KEGG Pathway
EGFR tyrosine ki.se inhibitor resistance (hsa01521 )
Endocrine resistance (hsa01522 )
Platinum drug resistance (hsa01524 )
ErbB sig.ling pathway (hsa04012 )
Ras sig.ling pathway (hsa04014 )
Rap1 sig.ling pathway (hsa04015 )
cAMP sig.ling pathway (hsa04024 )
Chemokine sig.ling pathway (hsa04062 )
HIF-1 sig.ling pathway (hsa04066 )
FoxO sig.ling pathway (hsa04068 )
Phosphatidylinositol sig.ling system (hsa04070 )
Sphingolipid sig.ling pathway (hsa04071 )
Phospholipase D sig.ling pathway (hsa04072 )
Autophagy - animal (hsa04140 )
mTOR sig.ling pathway (hsa04150 )
PI3K-Akt sig.ling pathway (hsa04151 )
AMPK sig.ling pathway (hsa04152 )
Apoptosis (hsa04210 )
Longevity regulating pathway (hsa04211 )
Longevity regulating pathway - multiple species (hsa04213 )
Cellular senescence (hsa04218 )
Axon guidance (hsa04360 )
VEGF sig.ling pathway (hsa04370 )
Osteoclast differentiation (hsa04380 )
Focal adhesion (hsa04510 )
Sig.ling pathways regulating pluripotency of stem cells (hsa04550 )
Platelet activation (hsa04611 )
Neutrophil extracellular trap formation (hsa04613 )
Toll-like receptor sig.ling pathway (hsa04620 )
C-type lectin receptor sig.ling pathway (hsa04625 )
JAK-STAT sig.ling pathway (hsa04630 )
.tural killer cell mediated cytotoxicity (hsa04650 )
T cell receptor sig.ling pathway (hsa04660 )
B cell receptor sig.ling pathway (hsa04662 )
Fc epsilon RI sig.ling pathway (hsa04664 )
Fc gamma R-mediated phagocytosis (hsa04666 )
TNF sig.ling pathway (hsa04668 )
Leukocyte transendothelial migration (hsa04670 )
Neurotrophin sig.ling pathway (hsa04722 )
Cholinergic sy.pse (hsa04725 )
Inflammatory mediator regulation of TRP channels (hsa04750 )
Regulation of actin cytoskeleton (hsa04810 )
Insulin sig.ling pathway (hsa04910 )
Progesterone-mediated oocyte maturation (hsa04914 )
Estrogen sig.ling pathway (hsa04915 )
Prolactin sig.ling pathway (hsa04917 )
Thyroid hormone sig.ling pathway (hsa04919 )
Regulation of lipolysis in adipocytes (hsa04923 )
Relaxin sig.ling pathway (hsa04926 )
GnRH secretion (hsa04929 )
Type II diabetes mellitus (hsa04930 )
Insulin resistance (hsa04931 )
Non-alcoholic fatty liver disease (hsa04932 )
AGE-RAGE sig.ling pathway in diabetic complications (hsa04933 )
Growth hormone synthesis, secretion and action (hsa04935 )
Aldosterone-regulated sodium reabsorption (hsa04960 )
Carbohydrate digestion and absorption (hsa04973 )
Alzheimer disease (hsa05010 )
Spinocerebellar ataxia (hsa05017 )
Prion disease (hsa05020 )
Bacterial invasion of epithelial cells (hsa05100 )
Shigellosis (hsa05131 )
Yersinia infection (hsa05135 )
Chagas disease (hsa05142 )
Amoebiasis (hsa05146 )
Hepatitis C (hsa05160 )
Hepatitis B (hsa05161 )
Measles (hsa05162 )
Human cytomegalovirus infection (hsa05163 )
Influenza A (hsa05164 )
Human papillomavirus infection (hsa05165 )
Human T-cell leukemia virus 1 infection (hsa05166 )
Kaposi sarcoma-associated herpesvirus infection (hsa05167 )
Herpes simplex virus 1 infection (hsa05168 )
Epstein-Barr virus infection (hsa05169 )
Human immunodeficiency virus 1 infection (hsa05170 )
Coro.virus disease - COVID-19 (hsa05171 )
Pathways in cancer (hsa05200 )
Viral carcinogenesis (hsa05203 )
Proteoglycans in cancer (hsa05205 )
MicroR.s in cancer (hsa05206 )
Chemical carcinogenesis - receptor activation (hsa05207 )
Chemical carcinogenesis - reactive oxygen species (hsa05208 )
Colorectal cancer (hsa05210 )
Re.l cell carcinoma (hsa05211 )
Pancreatic cancer (hsa05212 )
Endometrial cancer (hsa05213 )
Glioma (hsa05214 )
Prostate cancer (hsa05215 )
Melanoma (hsa05218 )
Chronic myeloid leukemia (hsa05220 )
Acute myeloid leukemia (hsa05221 )
Small cell lung cancer (hsa05222 )
Non-small cell lung cancer (hsa05223 )
Breast cancer (hsa05224 )
Hepatocellular carcinoma (hsa05225 )
Gastric cancer (hsa05226 )
Central carbon metabolism in cancer (hsa05230 )
Choline metabolism in cancer (hsa05231 )
PD-L1 expression and PD-1 checkpoint pathway in cancer (hsa05235 )
Diabetic cardiomyopathy (hsa05415 )
Lipid and atherosclerosis (hsa05417 )
Fluid shear stress and atherosclerosis (hsa05418 )
Reactome Pathway
IRS-mediated signalling (R-HSA-112399 )
GPVI-mediated activation cascade (R-HSA-114604 )
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants (R-HSA-1236382 )
PI3K events in ERBB4 signaling (R-HSA-1250342 )
PIP3 activates AKT signaling (R-HSA-1257604 )
Interleukin-7 signaling (R-HSA-1266695 )
Signaling by SCF-KIT (R-HSA-1433557 )
Synthesis of PIPs at the plasma membrane (R-HSA-1660499 )
GAB1 signalosome (R-HSA-180292 )
Signaling by cytosolic FGFR1 fusion mutants (R-HSA-1839117 )
Downstream signal transduction (R-HSA-186763 )
PI3K events in ERBB2 signaling (R-HSA-1963642 )
PI3K/AKT activation (R-HSA-198203 )
Signaling by ALK (R-HSA-201556 )
Downstream TCR signaling (R-HSA-202424 )
Role of phospholipids in phagocytosis (R-HSA-2029485 )
Tie2 Signaling (R-HSA-210993 )
Constitutive Signaling by Aberrant PI3K in Cancer (R-HSA-2219530 )
DAP12 signaling (R-HSA-2424491 )
Role of LAT2/NTAL/LAB on calcium mobilization (R-HSA-2730905 )
Nephrin family interactions (R-HSA-373753 )
Costimulation by the CD28 family (R-HSA-388841 )
CD28 dependent PI3K/Akt signaling (R-HSA-389357 )
G alpha (q) signalling events (R-HSA-416476 )
GP1b-IX-V activation signalling (R-HSA-430116 )
VEGFA-VEGFR2 Pathway (R-HSA-4420097 )
Interleukin-3, Interleukin-5 and GM-CSF signaling (R-HSA-512988 )
Constitutive Signaling by EGFRvIII (R-HSA-5637810 )
PI-3K cascade (R-HSA-5654689 )
PI-3K cascade (R-HSA-5654695 )
PI-3K cascade (R-HSA-5654710 )
PI-3K cascade (R-HSA-5654720 )
Signaling by FGFR2 in disease (R-HSA-5655253 )
Signaling by FGFR4 in disease (R-HSA-5655291 )
Signaling by FGFR1 in disease (R-HSA-5655302 )
Signaling by FGFR3 in disease (R-HSA-5655332 )
RAF/MAP kinase cascade (R-HSA-5673001 )
Interleukin-4 and Interleukin-13 signaling (R-HSA-6785807 )
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling (R-HSA-6811558 )
MET activates PI3K/AKT signaling (R-HSA-8851907 )
RET signaling (R-HSA-8853659 )
RHOA GTPase cycle (R-HSA-8980692 )
Extra-nuclear estrogen signaling (R-HSA-9009391 )
RHOB GTPase cycle (R-HSA-9013026 )
RHOC GTPase cycle (R-HSA-9013106 )
CDC42 GTPase cycle (R-HSA-9013148 )
RAC1 GTPase cycle (R-HSA-9013149 )
RAC2 GTPase cycle (R-HSA-9013404 )
RHOD GTPase cycle (R-HSA-9013405 )
RHOG GTPase cycle (R-HSA-9013408 )
RHOJ GTPase cycle (R-HSA-9013409 )
RHOU GTPase cycle (R-HSA-9013420 )
RAC3 GTPase cycle (R-HSA-9013423 )
RHOV GTPase cycle (R-HSA-9013424 )
Erythropoietin activates Phosphoinositide-3-kinase (PI3K) (R-HSA-9027276 )
Activated NTRK2 signals through PI3K (R-HSA-9028335 )
RHOF GTPase cycle (R-HSA-9035034 )
Interleukin receptor SHC signaling (R-HSA-912526 )
Regulation of signaling by CBL (R-HSA-912631 )
Activated NTRK3 signals through PI3K (R-HSA-9603381 )
FLT3 Signaling (R-HSA-9607240 )
Signaling by ERBB2 KD Mutants (R-HSA-9664565 )
Signaling by ERBB2 ECD mutants (R-HSA-9665348 )
Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants (R-HSA-9670439 )
Signaling by PDGFRA transmembrane, juxtamembrane and kinase domain mutants (R-HSA-9673767 )
Signaling by PDGFRA extracellular domain mutants (R-HSA-9673770 )
Signaling by CSF1 (M-CSF) in myeloid cells (R-HSA-9680350 )
RND3 GTPase cycle (R-HSA-9696264 )
RND2 GTPase cycle (R-HSA-9696270 )
RND1 GTPase cycle (R-HSA-9696273 )
Signaling by FLT3 fusion proteins (R-HSA-9703465 )
Signaling by FLT3 ITD and TKD mutants (R-HSA-9703648 )
Signaling by ALK fusions and activated point mutants (R-HSA-9725370 )
Antigen activates B Cell Receptor (BCR) leading to generation of second messengers (R-HSA-983695 )
PI3K Cascade (R-HSA-109704 )
BioCyc Pathway
MetaCyc:ENSG00000145675-MONOMER

Molecular Interaction Atlas (MIA) of This DOT

48 Disease(s) Related to This DOT
Disease Name Disease ID Evidence Level Mode of Inheritance REF
Agammaglobulinemia 7, autosomal recessive DISWT394 Definitive Autosomal recessive [1]
Immunodeficiency 36 DISFGFCW Definitive Autosomal dominant [2]
Prostate cancer DISF190Y Definitive Altered Expression [3]
SHORT syndrome DIS4TAKA Definitive Autosomal dominant [4]
Adult glioblastoma DISVP4LU Strong Biomarker [5]
Agammaglobulinemia DISXMS80 Strong Biomarker [6]
Alcohol dependence DIS4ZSCO Strong Biomarker [7]
Bladder cancer DISUHNM0 Strong Biomarker [8]
Brain neoplasm DISY3EKS Strong Genetic Variation [9]
Breast cancer DIS7DPX1 Strong Biomarker [10]
Breast carcinoma DIS2UE88 Strong Biomarker [10]
Breast neoplasm DISNGJLM Strong Biomarker [11]
Bronchiectasis DIS5MYEE Strong Biomarker [12]
Bruton-type agammaglobulinemia DISQ5ZYP Strong Genetic Variation [13]
Colon cancer DISVC52G Strong Biomarker [14]
Colorectal carcinoma DIS5PYL0 Strong Biomarker [15]
Colorectal neoplasm DISR1UCN Strong Genetic Variation [9]
Cutaneous melanoma DIS3MMH9 Strong Genetic Variation [9]
Endometrial cancer DISW0LMR Strong Genetic Variation [16]
Endometrial carcinoma DISXR5CY Strong Genetic Variation [16]
Exanthem DISAFOQN Strong Genetic Variation [17]
Glioma DIS5RPEH Strong Biomarker [18]
Hepatocellular carcinoma DIS0J828 Strong Biomarker [19]
Hyperglycemia DIS0BZB5 Strong Biomarker [20]
Immunodeficiency 14 DISI1EMU Strong Genetic Variation [21]
Lipodystrophy DIS3SGVD Strong Biomarker [22]
Lung cancer DISCM4YA Strong Biomarker [23]
Lung carcinoma DISTR26C Strong Biomarker [23]
Ovarian cancer DISZJHAP Strong Genetic Variation [24]
Prostate carcinoma DISMJPLE Strong Altered Expression [3]
Prostate neoplasm DISHDKGQ Strong Biomarker [25]
Rieger anomaly DISNBLZ5 Strong Biomarker [26]
Type-1/2 diabetes DISIUHAP Strong Biomarker [27]
Urinary bladder cancer DISDV4T7 Strong Biomarker [8]
Urinary bladder neoplasm DIS7HACE Strong Biomarker [8]
Vitiligo DISR05SL Strong Biomarker [28]
Burkitt lymphoma DIS9D5XU moderate Biomarker [29]
Immunodeficiency DIS093I0 moderate Genetic Variation [13]
Non-insulin dependent diabetes DISK1O5Z moderate Genetic Variation [30]
Activated PI3K-delta syndrome DISRL9M9 Supportive Autosomal dominant [31]
Autosomal agammaglobulinemia DISRW8BT Supportive Autosomal dominant [1]
High blood pressure DISY2OHH Disputed Biomarker [32]
Undifferentiated carcinoma DISIAZST Disputed Biomarker [33]
Carcinoma DISH9F1N Limited Biomarker [34]
Clear cell renal carcinoma DISBXRFJ Limited Biomarker [35]
Colon carcinoma DISJYKUO Limited Biomarker [14]
Non-small-cell lung cancer DIS5Y6R9 Limited Biomarker [36]
Obesity DIS47Y1K Limited Biomarker [37]
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⏷ Show the Full List of 48 Disease(s)
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DOT
This DOT Affected the Drug Response of 2 Drug(s)
Drug Name Drug ID Highest Status Interaction REF
Cisplatin DMRHGI9 Approved Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) decreases the response to substance of Cisplatin. [83]
Daunorubicin DMQUSBT Approved Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) affects the response to substance of Daunorubicin. [84]
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42 Drug(s) Affected the Gene/Protein Processing of This DOT
Drug Name Drug ID Highest Status Interaction REF
Valproate DMCFE9I Approved Valproate increases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [38]
Ciclosporin DMAZJFX Approved Ciclosporin decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [39]
Tretinoin DM49DUI Approved Tretinoin increases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [40]
Acetaminophen DMUIE76 Approved Acetaminophen decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [41]
Doxorubicin DMVP5YE Approved Doxorubicin decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [42]
Ivermectin DMDBX5F Approved Ivermectin increases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [43]
Arsenic DMTL2Y1 Approved Arsenic decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [44]
Quercetin DM3NC4M Approved Quercetin decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [45]
Arsenic trioxide DM61TA4 Approved Arsenic trioxide decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [46]
Testosterone DM7HUNW Approved Testosterone decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [48]
Carbamazepine DMZOLBI Approved Carbamazepine affects the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [49]
Zoledronate DMIXC7G Approved Zoledronate increases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [50]
Dexamethasone DMMWZET Approved Dexamethasone increases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [51]
Folic acid DMEMBJC Approved Folic acid affects the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [52]
Rosiglitazone DMILWZR Approved Rosiglitazone increases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [53]
Aspirin DM672AH Approved Aspirin decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [54]
Diclofenac DMPIHLS Approved Diclofenac affects the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [49]
Amphotericin B DMTAJQE Approved Amphotericin B decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [56]
Melphalan DMOLNHF Approved Melphalan decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [57]
Obeticholic acid DM3Q1SM Approved Obeticholic acid decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [58]
Imatinib DM7RJXL Approved Imatinib decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [59]
Nefazodone DM4ZS8M Approved Nefazodone decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [60]
Atazanavir DMSYRBX Approved Atazanavir decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [60]
Cantharidin DMBP5N3 Approved Cantharidin decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [61]
Urethane DM7NSI0 Phase 4 Urethane increases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [62]
SNDX-275 DMH7W9X Phase 3 SNDX-275 decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [63]
Resveratrol DM3RWXL Phase 3 Resveratrol increases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [64]
Seocalcitol DMKL9QO Phase 3 Seocalcitol increases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [65]
Contigoside B DMX9V8K Phase 2/3 Contigoside B increases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [67]
Tocopherol DMBIJZ6 Phase 2 Tocopherol decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [68]
(+)-JQ1 DM1CZSJ Phase 1 (+)-JQ1 decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [70]
LY294002 DMY1AFS Phase 1 LY294002 decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [71]
Geldanamycin DMS7TC5 Discontinued in Phase 2 Geldanamycin increases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [72]
Celastrol DMWQIJX Preclinical Celastrol decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [73]
Wortmannin DM8EVK5 Terminated Wortmannin decreases the activity of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [74]
Trichostatin A DM9C8NX Investigative Trichostatin A decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [38]
Formaldehyde DM7Q6M0 Investigative Formaldehyde decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [77]
Glyphosate DM0AFY7 Investigative Glyphosate decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [78]
QUERCITRIN DM1DH96 Investigative QUERCITRIN affects the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [79]
Bilirubin DMI0V4O Investigative Bilirubin decreases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [80]
U0126 DM31OGF Investigative U0126 increases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [71]
OXYBENZONE DMMZYX6 Investigative OXYBENZONE increases the expression of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [81]
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⏷ Show the Full List of 42 Drug(s)
7 Drug(s) Affected the Post-Translational Modifications of This DOT
Drug Name Drug ID Highest Status Interaction REF
Hydrogen peroxide DM1NG5W Approved Hydrogen peroxide decreases the phosphorylation of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [47]
Dasatinib DMJV2EK Approved Dasatinib decreases the phosphorylation of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [55]
Coprexa DMA0WEK Phase 3 Coprexa decreases the phosphorylation of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [66]
Benzo(a)pyrene DMN7J43 Phase 1 Benzo(a)pyrene decreases the methylation of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [69]
ABT-100 DMPFLS5 Terminated ABT-100 decreases the phosphorylation of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [75]
Bisphenol A DM2ZLD7 Investigative Bisphenol A increases the methylation of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [76]
3h-Indole-5,6-Diol DMBFCTZ Investigative 3h-Indole-5,6-Diol increases the phosphorylation of Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1). [82]
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⏷ Show the Full List of 7 Drug(s)

References

1 Agammaglobulinemia and absent B lineage cells in a patient lacking the p85 subunit of PI3K. J Exp Med. 2012 Mar 12;209(3):463-70. doi: 10.1084/jem.20112533. Epub 2012 Feb 20.
2 Technical standards for the interpretation and reporting of constitutional copy-number variants: a joint consensus recommendation of the American College of Medical Genetics and Genomics (ACMG) and the Clinical Genome Resource (ClinGen). Genet Med. 2020 Feb;22(2):245-257. doi: 10.1038/s41436-019-0686-8. Epub 2019 Nov 6.
3 LSD1 Activates PI3K/AKT Signaling Through Regulating p85 Expression in Prostate Cancer Cells.Front Oncol. 2019 Aug 2;9:721. doi: 10.3389/fonc.2019.00721. eCollection 2019.
4 PIK3R1 mutations cause syndromic insulin resistance with lipoatrophy. Am J Hum Genet. 2013 Jul 11;93(1):141-9. doi: 10.1016/j.ajhg.2013.05.019. Epub 2013 Jun 27.
5 Yes and PI3K bind CD95 to signal invasion of glioblastoma.Cancer Cell. 2008 Mar;13(3):235-48. doi: 10.1016/j.ccr.2008.02.003.
6 Heterozygous splice mutation in PIK3R1 causes human immunodeficiency with lymphoproliferation due to dominant activation of PI3K.J Exp Med. 2014 Dec 15;211(13):2537-47. doi: 10.1084/jem.20141759. Epub 2014 Dec 8.
7 Can we identify genes for alcohol consumption in samples ascertained for heterogeneous purposes?.Alcohol Clin Exp Res. 2009 Apr;33(4):729-39. doi: 10.1111/j.1530-0277.2008.00890.x. Epub 2009 Jan 22.
8 p85 Inactivates MMP-2 and Suppresses Bladder Cancer Invasion by Inhibiting MMP-14 Transcription and TIMP-2 Degradation.Neoplasia. 2019 Sep;21(9):908-920. doi: 10.1016/j.neo.2019.07.007. Epub 2019 Aug 8.
9 Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity.Nat Biotechnol. 2016 Feb;34(2):155-63. doi: 10.1038/nbt.3391. Epub 2015 Nov 30.
10 Significant prognostic values of differentially expressed-aberrantly methylated hub genes in breast cancer.J Cancer. 2019 Oct 21;10(26):6618-6634. doi: 10.7150/jca.33433. eCollection 2019.
11 microRNA-155 positively regulates glucose metabolism via PIK3R1-FOXO3a-cMYC axis in breast cancer.Oncogene. 2018 May;37(22):2982-2991. doi: 10.1038/s41388-018-0124-4. Epub 2018 Mar 12.
12 Respiratory Manifestations of the Activated Phosphoinositide 3-Kinase Delta Syndrome.Front Immunol. 2018 Mar 5;9:338. doi: 10.3389/fimmu.2018.00338. eCollection 2018.
13 Too much of a good thing: immunodeficiency due to hyperactive PI3K signaling.J Clin Invest. 2014 Sep;124(9):3688-90. doi: 10.1172/JCI77198. Epub 2014 Aug 18.
14 Inhibition of Growth and Metastasis of Colon Cancer by Delivering 5-Fluorouracil-loaded Pluronic P85 Copolymer Micelles.Sci Rep. 2016 Feb 11;6:20896. doi: 10.1038/srep20896.
15 DC-SIGN-LEF1/TCF1-miR-185 feedback loop promotes colorectal cancer invasion and metastasis.Cell Death Differ. 2020 Jan;27(1):379-395. doi: 10.1038/s41418-019-0361-2. Epub 2019 Jun 19.
16 A First-in-Human Phase 1 Study of LY3023414, an Oral PI3K/mTOR Dual Inhibitor, in Patients with Advanced Cancer.Clin Cancer Res. 2018 Jul 15;24(14):3253-3262. doi: 10.1158/1078-0432.CCR-17-3421. Epub 2018 Apr 10.
17 High-throughput screening identified inherited genetic variations in the EGFR pathway contributing to skin toxicity of EGFR inhibitors.Pharmacogenomics. 2015;16(14):1605-19. doi: 10.2217/pgs.15.97. Epub 2015 Sep 30.
18 Next-generation whole exome sequencing of glioblastoma with a primitive neuronal component.Brain Tumor Pathol. 2019 Jul;36(3):129-134. doi: 10.1007/s10014-019-00334-1. Epub 2019 Feb 4.
19 5-Hydroxytryptamine Receptor 1D Aggravates Hepatocellular Carcinoma Progression Through FoxO6 in AKT-Dependent and Independent Manners.Hepatology. 2019 May;69(5):2031-2047. doi: 10.1002/hep.30430. Epub 2019 Mar 10.
20 Ginsenoside Rb1 increases insulin sensitivity through suppressing 11-hydroxysteroid dehydrogenase type I.Am J Transl Res. 2017 Mar 15;9(3):1049-1057. eCollection 2017.
21 Conformational disruption of PI3K regulation by immunodeficiency mutations in PIK3CD and PIK3R1.Proc Natl Acad Sci U S A. 2017 Feb 21;114(8):1982-1987. doi: 10.1073/pnas.1617244114. Epub 2017 Feb 6.
22 Metformin paradoxically worsens insulin resistance in SHORT syndrome.Diabetol Metab Syndr. 2019 Oct 1;11:81. doi: 10.1186/s13098-019-0477-z. eCollection 2019.
23 Insulin growth factor signaling is regulated by microRNA-486, an underexpressed microRNA in lung cancer.Proc Natl Acad Sci U S A. 2013 Sep 10;110(37):15043-8. doi: 10.1073/pnas.1307107110. Epub 2013 Aug 26.
24 PI3K oncogenic mutations mediate resistance to afatinib in HER2/neu overexpressing gynecological cancers.Gynecol Oncol. 2019 Apr;153(1):158-164. doi: 10.1016/j.ygyno.2019.01.002. Epub 2019 Jan 7.
25 Sequencing of prostate cancers identifies new cancer genes, routes of progression and drug targets.Nat Genet. 2018 May;50(5):682-692. doi: 10.1038/s41588-018-0086-z. Epub 2018 Apr 16.
26 Iris Malformation and Anterior Segment Dysgenesis in Mice and Humans With a Mutation in PI 3-Kinase.Invest Ophthalmol Vis Sci. 2017 Jun 1;58(7):3100-3106. doi: 10.1167/iovs.16-21347.
27 Candidate gene association study in type 2 diabetes indicates a role for genes involved in beta-cell function as well as insulin action.PLoS Biol. 2003 Oct;1(1):E20. doi: 10.1371/journal.pbio.0000020. Epub 2003 Oct 13.
28 Reduced Nrf2 activation in PI3K phosphorylation-impaired vitiliginous keratinocytes increases susceptibility to ROS-generating chemical-induced apoptosis.Environ Toxicol. 2017 Dec;32(12):2481-2491. doi: 10.1002/tox.22461. Epub 2017 Aug 24.
29 The genetic landscape of mutations in Burkitt lymphoma.Nat Genet. 2012 Dec;44(12):1321-5. doi: 10.1038/ng.2468. Epub 2012 Nov 11.
30 PIK3R1 gene polymorphisms are associated with type 2 diabetes and related features in the Turkish population.Adv Clin Exp Med. 2018 Jul;27(7):921-927. doi: 10.17219/acem/68985.
31 A human immunodeficiency caused by mutations in the PIK3R1 gene. J Clin Invest. 2014 Sep;124(9):3923-8. doi: 10.1172/JCI75746. Epub 2014 Aug 18.
32 Chronic blockade of phosphatidylinositol 3-kinase in the nucleus tractus solitarii is prohypertensive in the spontaneously hypertensive rat.Hypertension. 2009 Jan;53(1):97-103. doi: 10.1161/HYPERTENSIONAHA.108.122341. Epub 2008 Nov 17.
33 Allelic imbalance and altered expression of genes in chromosome 2q11-2q16 from rat mammary gland carcinomas induced by 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine.Oncogene. 2003 Feb 27;22(8):1253-60. doi: 10.1038/sj.onc.1206233.
34 Genomic profiling of metaplastic breast carcinomas reveals genetic heterogeneity and relationship to ductal carcinoma.Mod Pathol. 2018 Nov;31(11):1661-1674. doi: 10.1038/s41379-018-0081-z. Epub 2018 Jun 26.
35 Anticancer activity of Schiff base-Poloxamer P85 combination against kidney cancer.Int Urol Nephrol. 2018 Feb;50(2):247-255. doi: 10.1007/s11255-017-1782-9. Epub 2017 Dec 29.
36 MiR-486-5p Serves as a Good Biomarker in Nonsmall Cell Lung Cancer and Suppresses Cell Growth With the Involvement of a Target PIK3R1.Front Genet. 2019 Jul 26;10:688. doi: 10.3389/fgene.2019.00688. eCollection 2019.
37 Phosphatidylinositol 3-kinase/Akt signaling stimulates colonic mucosal cell survival during aging.Am J Physiol Gastrointest Liver Physiol. 2006 Jan;290(1):G49-55. doi: 10.1152/ajpgi.00106.2005. Epub 2005 Aug 25.
38 From transient transcriptome responses to disturbed neurodevelopment: role of histone acetylation and methylation as epigenetic switch between reversible and irreversible drug effects. Arch Toxicol. 2014 Jul;88(7):1451-68.
39 Comparison of HepG2 and HepaRG by whole-genome gene expression analysis for the purpose of chemical hazard identification. Toxicol Sci. 2010 May;115(1):66-79.
40 Retinoic acid receptor alpha amplifications and retinoic acid sensitivity in breast cancers. Clin Breast Cancer. 2013 Oct;13(5):401-8.
41 Gene expression data from acetaminophen-induced toxicity in human hepatic in vitro systems and clinical liver samples. Data Brief. 2016 Mar 26;7:1052-1057. doi: 10.1016/j.dib.2016.03.069. eCollection 2016 Jun.
42 Bringing in vitro analysis closer to in vivo: studying doxorubicin toxicity and associated mechanisms in 3D human microtissues with PBPK-based dose modelling. Toxicol Lett. 2018 Sep 15;294:184-192.
43 Quantitative proteomics reveals a broad-spectrum antiviral property of ivermectin, benefiting for COVID-19 treatment. J Cell Physiol. 2021 Apr;236(4):2959-2975. doi: 10.1002/jcp.30055. Epub 2020 Sep 22.
44 Genome-wide analysis of BEAS-2B cells exposed to trivalent arsenicals and dimethylthioarsinic acid. Toxicology. 2010 Jan 31;268(1-2):31-9.
45 Anticarcinogenic action of quercetin by downregulation of phosphatidylinositol 3-kinase (PI3K) and protein kinase C (PKC) via induction of p53 in hepatocellular carcinoma (HepG2) cell line. Mol Biol Rep. 2015 Sep;42(9):1419-29. doi: 10.1007/s11033-015-3921-7. Epub 2015 Aug 27.
46 Arsenic trioxide reduces the expression of E2F1, cyclin E, and phosphorylation of PI3K signaling molecules in acute leukemia cells. Environ Toxicol. 2021 Sep;36(9):1785-1792. doi: 10.1002/tox.23299. Epub 2021 May 27.
47 Repression of Kisspeptin1 weakens hydrogen peroxide-caused injury in HTR8 cells via adjusting PI3K/AKT/mTOR pathway. J Biochem Mol Toxicol. 2020 May;34(5):e22461. doi: 10.1002/jbt.22461. Epub 2020 Feb 11.
48 The exosome-like vesicles derived from androgen exposed-prostate stromal cells promote epithelial cells proliferation and epithelial-mesenchymal transition. Toxicol Appl Pharmacol. 2021 Jan 15;411:115384. doi: 10.1016/j.taap.2020.115384. Epub 2020 Dec 25.
49 Drug-induced endoplasmic reticulum and oxidative stress responses independently sensitize toward TNF-mediated hepatotoxicity. Toxicol Sci. 2014 Jul;140(1):144-59. doi: 10.1093/toxsci/kfu072. Epub 2014 Apr 20.
50 Interleukin-19 as a translational indicator of renal injury. Arch Toxicol. 2015 Jan;89(1):101-6.
51 Identification of mechanisms of action of bisphenol a-induced human preadipocyte differentiation by transcriptional profiling. Obesity (Silver Spring). 2014 Nov;22(11):2333-43.
52 Effects of folate deficiency on gene expression in the apoptosis and cancer pathways in colon cancer cells. Carcinogenesis. 2006 May;27(5):916-24. doi: 10.1093/carcin/bgi312. Epub 2005 Dec 16.
53 Regulation of gene expression by activation of the peroxisome proliferator-activated receptor gamma with rosiglitazone (BRL 49653) in human adipocytes. Biochem Biophys Res Commun. 1999 Nov;265(1):265-71. doi: 10.1006/bbrc.1999.1657.
54 Lunasin, a novel seed peptide, sensitizes human breast cancer MDA-MB-231 cells to aspirin-arrested cell cycle and induced apoptosis. Chem Biol Interact. 2010 Jul 30;186(2):127-34. doi: 10.1016/j.cbi.2010.04.027. Epub 2010 May 21.
55 Combination of arsenic trioxide and Dasatinib: a new strategy to treat Philadelphia chromosome-positive acute lymphoblastic leukaemia. J Cell Mol Med. 2018 Mar;22(3):1614-1626.
56 Differential expression of microRNAs and their predicted targets in renal cells exposed to amphotericin B and its complex with copper (II) ions. Toxicol Mech Methods. 2017 Sep;27(7):537-543. doi: 10.1080/15376516.2017.1333554. Epub 2017 Jun 8.
57 Bone marrow osteoblast damage by chemotherapeutic agents. PLoS One. 2012;7(2):e30758. doi: 10.1371/journal.pone.0030758. Epub 2012 Feb 17.
58 Pharmacotoxicology of clinically-relevant concentrations of obeticholic acid in an organotypic human hepatocyte system. Toxicol In Vitro. 2017 Mar;39:93-103.
59 A systems biology understanding of the synergistic effects of arsenic sulfide and Imatinib in BCR/ABL-associated leukemia. Proc Natl Acad Sci U S A. 2009 Mar 3;106(9):3378-83.
60 Robustness testing and optimization of an adverse outcome pathway on cholestatic liver injury. Arch Toxicol. 2020 Apr;94(4):1151-1172. doi: 10.1007/s00204-020-02691-9. Epub 2020 Mar 10.
61 Cantharidin suppresses gastric cancer cell migration/invasion by inhibiting the PI3K/Akt signaling pathway via CCAT1. Chem Biol Interact. 2020 Feb 1;317:108939. doi: 10.1016/j.cbi.2020.108939. Epub 2020 Jan 13.
62 Ethyl carbamate induces cell death through its effects on multiple metabolic pathways. Chem Biol Interact. 2017 Nov 1;277:21-32.
63 A transcriptome-based classifier to identify developmental toxicants by stem cell testing: design, validation and optimization for histone deacetylase inhibitors. Arch Toxicol. 2015 Sep;89(9):1599-618.
64 Molecular mechanisms of resveratrol action in lung cancer cells using dual protein and microarray analyses. Cancer Res. 2007 Dec 15;67(24):12007-17. doi: 10.1158/0008-5472.CAN-07-2464.
65 Expression profiling in squamous carcinoma cells reveals pleiotropic effects of vitamin D3 analog EB1089 signaling on cell proliferation, differentiation, and immune system regulation. Mol Endocrinol. 2002 Jun;16(6):1243-56.
66 Copper deprivation enhances the chemosensitivity of pancreatic cancer to rapamycin by mTORC1/2 inhibition. Chem Biol Interact. 2023 Sep 1;382:110546. doi: 10.1016/j.cbi.2023.110546. Epub 2023 Jun 7.
67 Improved Preventive Effects of Combined Bioactive Compounds Present in Different Blueberry Varieties as Compared to Single Phytochemicals. Nutrients. 2018 Dec 29;11(1):61. doi: 10.3390/nu11010061.
68 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
69 Air pollution and DNA methylation alterations in lung cancer: A systematic and comparative study. Oncotarget. 2017 Jan 3;8(1):1369-1391. doi: 10.18632/oncotarget.13622.
70 Bromodomain-containing protein 4 (BRD4) regulates RNA polymerase II serine 2 phosphorylation in human CD4+ T cells. J Biol Chem. 2012 Dec 14;287(51):43137-55.
71 The Specific Inhibition of SOD1 Selectively Promotes Apoptosis of Cancer Cells via Regulation of the ROS Signaling Network. Oxid Med Cell Longev. 2019 Feb 18;2019:9706792. doi: 10.1155/2019/9706792. eCollection 2019.
72 Identification of transcriptome signatures and biomarkers specific for potential developmental toxicants inhibiting human neural crest cell migration. Arch Toxicol. 2016 Jan;90(1):159-80.
73 Gene expression signature-based chemical genomic prediction identifies a novel class of HSP90 pathway modulators. Cancer Cell. 2006 Oct;10(4):321-30.
74 Expression and purification of PI3 kinase alpha and development of an ATP depletion and an alphascreen PI3 kinase activity assay. J Biomol Screen. 2008 Dec;13(10):1035-40. doi: 10.1177/1087057108326079. Epub 2008 Nov 25.
75 Farnesyltransferase inhibitor, ABT-100, is a potent liver cancer chemopreventive agent. Clin Cancer Res. 2005 Jun 1;11(11):4266-74. doi: 10.1158/1078-0432.CCR-04-2386.
76 Expression and DNA methylation changes in human breast epithelial cells after bisphenol A exposure. Int J Oncol. 2012 Jul;41(1):369-77.
77 Gene expression changes in primary human nasal epithelial cells exposed to formaldehyde in vitro. Toxicol Lett. 2010 Oct 5;198(2):289-95.
78 Glyphosate-based herbicides at low doses affect canonical pathways in estrogen positive and negative breast cancer cell lines. PLoS One. 2019 Jul 11;14(7):e0219610. doi: 10.1371/journal.pone.0219610. eCollection 2019.
79 Molecular mechanisms of quercitrin-induced apoptosis in non-small cell lung cancer. Arch Med Res. 2014 Aug;45(6):445-54.
80 Global changes in gene regulation demonstrate that unconjugated bilirubin is able to upregulate and activate select components of the endoplasmic reticulum stress response pathway. J Biochem Mol Toxicol. 2010 Mar-Apr;24(2):73-88.
81 Chromatin modifiers: A new class of pollutants with potential epigenetic effects revealed by in vitro assays and transcriptomic analyses. Toxicology. 2023 Jan 15;484:153413. doi: 10.1016/j.tox.2022.153413. Epub 2022 Dec 26.
82 Danhong formula alleviates endothelial dysfunction and reduces blood pressure in hypertension by regulating MicroRNA 24 - Phosphatidylinositol 3-Kinase-Serine/Threonine Kinase- Endothelial Nitric Oxide Synthase axis. J Ethnopharmacol. 2024 Apr 6;323:117615. doi: 10.1016/j.jep.2023.117615. Epub 2023 Dec 30.
83 HDAC4-regulated STAT1 activation mediates platinum resistance in ovarian cancer. Cancer Res. 2011 Jul 1;71(13):4412-22. doi: 10.1158/0008-5472.CAN-10-4111. Epub 2011 May 13.
84 Mapping genes that contribute to daunorubicin-induced cytotoxicity. Cancer Res. 2007 Jun 1;67(11):5425-33. doi: 10.1158/0008-5472.CAN-06-4431.