General Information of Drug Combination (ID: DCR8JVT)

Drug Combination Name
Mifepristone Letrozole
Indication
Disease Entry Status REF
Complete Abortion Phase 1 [1]
Component Drugs Mifepristone   DMGZQEF Letrozole   DMH07Y3
Small molecular drug Small molecular drug
2D MOL 2D MOL
3D MOL 3D MOL

Molecular Interaction Atlas of This Drug Combination

Molecular Interaction Atlas (MIA)
Indication(s) of Mifepristone
Disease Entry ICD 11 Status REF
Cushing disease 5A70 Approved [2]
Mifepristone Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Glucocorticoid receptor (NR3C1) TTYRL6O GCR_HUMAN Modulator [7]
------------------------------------------------------------------------------------
Mifepristone Interacts with 2 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [8]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Metabolism [9]
------------------------------------------------------------------------------------
Mifepristone Interacts with 228 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Increases Expression [10]
Pro-neuropeptide Y (NPY) OT4ICV3P NPY_HUMAN Increases ADR [11]
Nuclear receptor subfamily 1 group I member 3 (NR1I3) OTS3SGH7 NR1I3_HUMAN Increases Expression [12]
Frizzled-9 (FZD9) OTTZ9MKK FZD9_HUMAN Increases Expression [5]
Forkhead box protein N3 (FOXN3) OTOJYJZP FOXN3_HUMAN Increases Expression [5]
Procollagen-lysine,2-oxoglutarate 5-dioxygenase 2 (PLOD2) OTKOZRZP PLOD2_HUMAN Increases Expression [5]
Actin-binding LIM protein 1 (ABLIM1) OTHXEK3E ABLM1_HUMAN Increases Expression [5]
Ectoderm-neural cortex protein 1 (ENC1) OTJEUB6U ENC1_HUMAN Increases Expression [5]
Histone-lysine N-methyltransferase 2D (KMT2D) OTTVHCLY KMT2D_HUMAN Decreases Expression [5]
17-beta-hydroxysteroid dehydrogenase type 6 (HSD17B6) OTSB55D2 H17B6_HUMAN Decreases Expression [5]
Branched-chain-amino-acid aminotransferase, mitochondrial (BCAT2) OT8L6EGI BCAT2_HUMAN Decreases Expression [5]
Calpain-5 (CAPN5) OTQ8QM7K CAN5_HUMAN Decreases Expression [5]
Leucine-rich repeat transmembrane protein FLRT2 (FLRT2) OTGD8TID FLRT2_HUMAN Decreases Expression [5]
Septin-4 (SEPTIN4) OTD16B30 SEPT4_HUMAN Decreases Expression [5]
Cationic amino acid transporter 4 (SLC7A4) OTAVC6QS CTR4_HUMAN Decreases Expression [5]
Proline dehydrogenase 1, mitochondrial (PRODH) OT7SQ1C7 PROD_HUMAN Decreases Expression [5]
Synaptogyrin-1 (SYNGR1) OT0MBUK5 SNG1_HUMAN Decreases Expression [5]
C-X-C motif chemokine 13 (CXCL13) OT2AT4N8 CXL13_HUMAN Decreases Expression [5]
Frizzled-6 (FZD6) OTBCPII8 FZD6_HUMAN Increases Expression [5]
Sushi repeat-containing protein SRPX2 (SRPX2) OT6A63TX SRPX2_HUMAN Increases Expression [5]
Sorting nexin-2 (SNX2) OT889MQA SNX2_HUMAN Increases Expression [5]
P antigen family member 4 (PAGE4) OT2VLWT0 PAGE4_HUMAN Decreases Expression [5]
Slit homolog 3 protein (SLIT3) OTU8MKEU SLIT3_HUMAN Decreases Expression [5]
Large neutral amino acids transporter small subunit 3 (SLC43A1) OTQJQY3S LAT3_HUMAN Decreases Expression [5]
Solute carrier family 22 member 3 (SLC22A3) OTQYGVXX S22A3_HUMAN Decreases Expression [5]
E3 ubiquitin-protein ligase NEURL1 (NEURL1) OT2C4P70 NEUL1_HUMAN Increases Expression [5]
Cystatin-F (CST7) OTQWZUVQ CYTF_HUMAN Decreases Expression [5]
Galactosylgalactosylxylosylprotein 3-beta-glucuronosyltransferase 3 (B3GAT3) OTDSN5XF B3GA3_HUMAN Decreases Expression [5]
Myelin protein zero-like protein 1 (MPZL1) OTJSUUHR MPZL1_HUMAN Decreases Expression [5]
Supervillin (SVIL) OTWQQ1WK SVIL_HUMAN Increases Expression [5]
Follistatin-related protein 3 (FSTL3) OT75489W FSTL3_HUMAN Decreases Expression [5]
Protein LDOC1 (LDOC1) OTWZH4O9 LDOC1_HUMAN Decreases Expression [5]
Coagulation factor XIII A chain (F13A1) OTO8O184 F13A_HUMAN Increases Expression [5]
Tissue-type plasminogen activator (PLAT) OTQPDNAB TPA_HUMAN Increases Expression [5]
Myc proto-oncogene protein (MYC) OTPV5LUK MYC_HUMAN Decreases Expression [5]
Prolactin (PRL) OTWFQGX7 PRL_HUMAN Increases Expression [5]
Collagen alpha-1(II) chain (COL2A1) OT5E59C8 CO2A1_HUMAN Decreases Expression [5]
Apolipoprotein C-I (APOC1) OTA58CED APOC1_HUMAN Decreases Expression [5]
Annexin A1 (ANXA1) OT5OFDJC ANXA1_HUMAN Increases Expression [5]
Plasminogen activator inhibitor 1 (SERPINE1) OTT0MPQ3 PAI1_HUMAN Decreases Expression [5]
Cyclin-dependent kinase 1 (CDK1) OTW1SC2N CDK1_HUMAN Increases Expression [5]
Protein S100-A6 (S100A6) OTHHPZQ8 S10A6_HUMAN Decreases Expression [5]
Tyrosine 3-monooxygenase (TH) OT6ZORKP TY3H_HUMAN Decreases Expression [5]
Decorin (DCN) OTWLJL7K PGS2_HUMAN Increases Expression [5]
Thrombospondin-1 (THBS1) OT0ECWK3 TSP1_HUMAN Increases Expression [5]
Stromelysin-1 (MMP3) OTGBI74Z MMP3_HUMAN Increases Expression [5]
Glutathione S-transferase A1 (GSTA1) OTA7K5XA GSTA1_HUMAN Increases Expression [5]
Inhibin beta A chain (INHBA) OTSP64PQ INHBA_HUMAN Increases Expression [5]
Matrilysin (MMP7) OTVT3SEJ MMP7_HUMAN Increases Expression [5]
Stromelysin-2 (MMP10) OTJDWW8Q MMP10_HUMAN Increases Expression [5]
Growth-regulated alpha protein (CXCL1) OT3WCTZV GROA_HUMAN Decreases Expression [5]
Fructose-bisphosphate aldolase C (ALDOC) OTEC13I5 ALDOC_HUMAN Decreases Expression [5]
Glutathione S-transferase theta-2 (GSTT2) OTANW3TJ GST2_HUMAN Decreases Expression [5]
C-C motif chemokine 3 (CCL3) OTW2H3ND CCL3_HUMAN Decreases Expression [5]
Thyroid hormone receptor alpha (THRA) OTKRLVD7 THA_HUMAN Decreases Expression [5]
Thyroid hormone receptor beta (THRB) OTBBIRHZ THB_HUMAN Increases Expression [5]
Pyruvate carboxylase, mitochondrial (PC) OT6O0V51 PYC_HUMAN Decreases Expression [5]
Creatine kinase B-type (CKB) OTUCKOTT KCRB_HUMAN Decreases Expression [5]
Cadherin-1 (CDH1) OTFJMXPM CADH1_HUMAN Increases Expression [5]
Cytochrome P450 4B1 (CYP4B1) OTJP46CB CP4B1_HUMAN Decreases Expression [5]
Retinoic acid receptor gamma (RARG) OT8LHMDH RARG_HUMAN Decreases Expression [5]
HLA class II histocompatibility antigen, DO beta chain (HLA-DOB) OTKADDUB DOB_HUMAN Decreases Expression [5]
Aminopeptidase N (ANPEP) OTP3WYFD AMPN_HUMAN Decreases Expression [5]
15-hydroxyprostaglandin dehydrogenase (HPGD) OTYZI6JB PGDH_HUMAN Decreases Expression [5]
NAD(P)H dehydrogenase 1 (NQO1) OTZGGIVK NQO1_HUMAN Decreases Expression [5]
Platelet glycoprotein 4 (CD36) OT5CZWKY CD36_HUMAN Decreases Expression [5]
Fumarylacetoacetase (FAH) OTGZA1YR FAAA_HUMAN Decreases Expression [5]
Gap junction alpha-1 protein (GJA1) OTT94MKL CXA1_HUMAN Increases Expression [5]
Insulin-like growth factor-binding protein 3 (IGFBP3) OTIX63TX IBP3_HUMAN Increases Expression [5]
Tumor necrosis factor receptor superfamily member 1A (TNFRSF1A) OT2D9DOV TNR1A_HUMAN Increases Expression [5]
Fibulin-1 (FBLN1) OT5MHHOP FBLN1_HUMAN Decreases Expression [5]
Prostaglandin G/H synthase 1 (PTGS1) OTHCRLEC PGH1_HUMAN Decreases Expression [5]
Integrin alpha-6 (ITGA6) OT3FA39C ITA6_HUMAN Increases Expression [5]
Laminin subunit alpha-2 (LAMA2) OTFROQWE LAMA2_HUMAN Decreases Expression [5]
Endothelin receptor type B (EDNRB) OTLLZV3P EDNRB_HUMAN Increases Expression [5]
Insulin-like growth factor-binding protein 5 (IGFBP5) OTRE5V0C IBP5_HUMAN Decreases Expression [5]
Atypical chemokine receptor 3 (ACKR3) OTA6GA4F ACKR3_HUMAN Decreases Expression [5]
Collagen alpha-5(IV) chain (COL4A5) OTHG60RE CO4A5_HUMAN Decreases Expression [5]
ER lumen protein-retaining receptor 2 (KDELR2) OT9QW7Q0 ERD22_HUMAN Increases Expression [5]
Catenin beta-1 (CTNNB1) OTZ932A3 CTNB1_HUMAN Increases Expression [5]
Pigment epithelium-derived factor (SERPINF1) OTWZH98J PEDF_HUMAN Decreases Expression [5]
Prostaglandin-H2 D-isomerase (PTGDS) OT71NN7C PTGDS_HUMAN Decreases Expression [5]
5-hydroxytryptamine receptor 2B (HTR2B) OTM1AD9J 5HT2B_HUMAN Increases Expression [5]
Glutamate receptor 1 (GRIA1) OT85LOCJ GRIA1_HUMAN Decreases Expression [5]
C-X-C motif chemokine 5 (CXCL5) OTZOUPCA CXCL5_HUMAN Increases Expression [5]
Prostacyclin receptor (PTGIR) OTWTABYM PI2R_HUMAN Increases Expression [5]
Small ribosomal subunit protein eS10 (RPS10) OTE3VSAH RS10_HUMAN Increases Expression [5]
Microtubule-associated protein 1B (MAP1B) OTVXW089 MAP1B_HUMAN Increases Expression [5]
Stromal cell-derived factor 1 (CXCL12) OT2QX5LL SDF1_HUMAN Increases Expression [5]
Transcription factor SOX-9 (SOX9) OTVDJFGN SOX9_HUMAN Increases Expression [5]
Heat shock 70 kDa protein 13 (HSPA13) OTYXMC4G HSP13_HUMAN Increases Expression [5]
DNA polymerase delta subunit 2 (POLD2) OTBNASP6 DPOD2_HUMAN Decreases Expression [5]
MARCKS-related protein (MARCKSL1) OT13J2FM MRP_HUMAN Increases Expression [5]
Steroidogenic acute regulatory protein, mitochondrial (STAR) OTFEZ5AI STAR_HUMAN Decreases Expression [5]
ADP-ribosylation factor-like protein 4D (ARL4D) OTG5I3KU ARL4D_HUMAN Decreases Expression [5]
Matrix metalloproteinase-14 (MMP14) OT9C197Z MMP14_HUMAN Increases Expression [5]
Matrix metalloproteinase-16 (MMP16) OTSFQ2BJ MMP16_HUMAN Increases Expression [5]
RNA-binding protein Nova-1 (NOVA1) OT6A9KHY NOVA1_HUMAN Increases Expression [5]
Lumican (LUM) OTSRC874 LUM_HUMAN Increases Expression [5]
ATP-citrate synthase (ACLY) OTRL9ZRP ACLY_HUMAN Increases Expression [5]
Cadherin-11 (CDH11) OTIZKPTF CAD11_HUMAN Increases Expression [5]
BH3-interacting domain death agonist (BID) OTOSHSHU BID_HUMAN Increases Expression [5]
Sestrin-3 (SESN3) OTJRY1Y5 SESN3_HUMAN Increases Expression [5]
Actin, cytoplasmic 1 (ACTB) OT1MCP2F ACTB_HUMAN Decreases Expression [5]
Ras-related protein Rap-1b (RAP1B) OTHEIIMM RAP1B_HUMAN Increases Expression [5]
26S proteasome regulatory subunit 10B (PSMC6) OTG8997V PRS10_HUMAN Increases Expression [5]
Large ribosomal subunit protein eL39 (RPL39) OTL8TZHQ RL39_HUMAN Increases Expression [5]
Contactin-associated protein 1 (CNTNAP1) OT5Y03EU CNTP1_HUMAN Decreases Expression [5]
Fractalkine (CX3CL1) OTPLGI0E X3CL1_HUMAN Increases Expression [5]
Sushi repeat-containing protein SRPX (SRPX) OT5B9LXS SRPX_HUMAN Decreases Expression [5]
C-C motif chemokine 8 (CCL8) OTCTWYN8 CCL8_HUMAN Decreases Expression [5]
Rho-related GTP-binding protein RhoG (RHOG) OTJ7J1WA RHOG_HUMAN Decreases Expression [5]
Small EDRK-rich factor 2 (SERF2) OTZQDYCZ SERF2_HUMAN Increases Expression [5]
Norrin (NDP) OTGDJ4US NDP_HUMAN Decreases Expression [5]
Angiopoietin-1 receptor (TEK) OT78YN57 TIE2_HUMAN Increases Expression [5]
Tyrosine-protein kinase BTK (BTK) OTG3CDVK BTK_HUMAN Increases Expression [5]
Serine/threonine-protein phosphatase 2A regulatory subunit B'' subunit alpha (PPP2R3A) OTSK5GFC P2R3A_HUMAN Increases Expression [5]
Early activation antigen CD69 (CD69) OTGJHSVP CD69_HUMAN Increases Expression [5]
Tight junction protein ZO-1 (TJP1) OTBDCUPK ZO1_HUMAN Increases Expression [5]
Sperm-associated antigen 1 (SPAG1) OT29JZKW SPAG1_HUMAN Increases Expression [5]
ATP-binding cassette sub-family C member 8 (ABCC8) OTCWQ54I ABCC8_HUMAN Decreases Expression [5]
Aminoacyl tRNA synthase complex-interacting multifunctional protein 1 (AIMP1) OTTA5C3U AIMP1_HUMAN Increases Expression [5]
BCL2/adenovirus E1B 19 kDa protein-interacting protein 2 (BNIP2) OTVZD4H6 BNIP2_HUMAN Increases Expression [5]
Metastasis-associated protein MTA1 (MTA1) OTBHW3S9 MTA1_HUMAN Decreases Expression [5]
Phospholipase D1 (PLD1) OTMVUKW6 PLD1_HUMAN Increases Expression [5]
Laminin subunit gamma-2 (LAMC2) OTJMTM72 LAMC2_HUMAN Increases Expression [5]
Collagen alpha-6(IV) chain (COL4A6) OTUREU5Z CO4A6_HUMAN Decreases Expression [5]
Interleukin-13 receptor subunit alpha-2 (IL13RA2) OTPC2G0X I13R2_HUMAN Increases Expression [5]
ADP-ribosylation factor-like protein 6-interacting protein 1 (ARL6IP1) OT536XAV AR6P1_HUMAN Increases Expression [5]
Receptor-type tyrosine-protein phosphatase kappa (PTPRK) OTAP5AT3 PTPRK_HUMAN Increases Expression [5]
P2Y purinoceptor 14 (P2RY14) OTDGZKED P2Y14_HUMAN Increases Expression [5]
Monocyte to macrophage differentiation factor (MMD) OTB5I4OC PAQRB_HUMAN Increases Expression [5]
TSC22 domain family protein 1 (TSC22D1) OTN4GFWD T22D1_HUMAN Increases Expression [5]
Adipogenesis regulatory factor (ADIRF) OTTJP8D4 ADIRF_HUMAN Decreases Expression [5]
Mitogen-activated protein kinase 6 (MAPK6) OTDDNF3Q MK06_HUMAN Increases Expression [5]
Laminin subunit alpha-3 (LAMA3) OTFME7HT LAMA3_HUMAN Decreases Expression [5]
Centrosomal protein kizuna (KIZ) OT5VCKSM KIZ_HUMAN Increases Expression [5]
Carboxypeptidase Z (CPZ) OT5HUR28 CBPZ_HUMAN Increases Expression [5]
F-box only protein 46 (FBXO46) OT773EPG FBX46_HUMAN Decreases Expression [5]
Plexin domain-containing protein 2 (PLXDC2) OTS1FUV6 PXDC2_HUMAN Increases Expression [5]
Acetylgalactosaminyl-O-glycosyl-glycoprotein beta-1,3-N-acetylglucosaminyltransferase (B3GNT6) OTAX8BNJ B3GN6_HUMAN Decreases Expression [5]
Protein mono-ADP-ribosyltransferase TIPARP (TIPARP) OTZ4BG4B PARPT_HUMAN Decreases Expression [5]
Kinesin-like protein KIF27 (KIF27) OTV70I2Q KIF27_HUMAN Increases Expression [5]
Osteopetrosis-associated transmembrane protein 1 (OSTM1) OTKNJDH7 OSTM1_HUMAN Increases Expression [5]
Membrane progestin receptor alpha (PAQR7) OTIWX5AM PAQR7_HUMAN Decreases Expression [5]
Secreted frizzled-related protein 1 (SFRP1) OT0U9G41 SFRP1_HUMAN Increases Expression [5]
RB1-inducible coiled-coil protein 1 (RB1CC1) OTZK8PFX RBCC1_HUMAN Increases Expression [5]
Protein phosphatase 1 regulatory subunit 1C (PPP1R1C) OTVH6BND PPR1C_HUMAN Increases Expression [5]
Kelch-like protein 6 (KLHL6) OTLDECOX KLHL6_HUMAN Increases Expression [5]
C-type lectin domain family 2 member B (CLEC2B) OT0W0M0L CLC2B_HUMAN Increases Expression [5]
(3R)-3-hydroxyacyl-CoA dehydrogenase (HSD17B8) OTX1DWEF DHB8_HUMAN Decreases Expression [5]
Tribbles homolog 2 (TRIB2) OTHSX3MX TRIB2_HUMAN Increases Expression [5]
Histone deacetylase 2 (HDAC2) OTUYVFKN HDAC2_HUMAN Increases Expression [5]
Type II iodothyronine deiodinase (DIO2) OTGPNSLH IOD2_HUMAN Increases Expression [5]
Stathmin-2 (STMN2) OT0FUHLH STMN2_HUMAN Increases Expression [5]
Seipin (BSCL2) OT73V6Y4 BSCL2_HUMAN Decreases Expression [5]
Receptor expression-enhancing protein 6 (REEP6) OTY4FPO8 REEP6_HUMAN Decreases Expression [5]
Mannose-1-phosphate guanyltransferase alpha (GMPPA) OTADC03N GMPPA_HUMAN Decreases Expression [5]
Mastermind-like protein 3 (MAML3) OTZFV53Z MAML3_HUMAN Increases Expression [5]
Translocation protein SEC62 (SEC62) OTCWEL5F SEC62_HUMAN Increases Expression [5]
Mitochondrial import inner membrane translocase subunit Tim17-A (TIMM17A) OTVFRL8G TI17A_HUMAN Increases Expression [5]
C-C motif chemokine 13 (CCL13) OTNX0JD0 CCL13_HUMAN Decreases Expression [5]
SH3-containing GRB2-like protein 3-interacting protein 1 (SGIP1) OTQW6R3Z SGIP1_HUMAN Increases Expression [5]
Receptor expression-enhancing protein 2 (REEP2) OTPCRA5O REEP2_HUMAN Decreases Expression [5]
Latexin (LXN) OTZQ2M6Y LXN_HUMAN Increases Expression [5]
Complement C1q tumor necrosis factor-related protein 6 (C1QTNF6) OT57EPQC C1QT6_HUMAN Increases Expression [5]
Cysteine-rich secretory protein LCCL domain-containing 2 (CRISPLD2) OTVSFHTL CRLD2_HUMAN Decreases Expression [5]
E3 ubiquitin-protein ligase SMURF2 (SMURF2) OT3TRVL7 SMUF2_HUMAN Increases Expression [5]
Netrin-4 (NTN4) OTDRRMP3 NET4_HUMAN Increases Expression [5]
Endothelial cell-specific molecule 1 (ESM1) OT331Y8V ESM1_HUMAN Increases Expression [5]
Exosome complex component RRP46 (EXOSC5) OTADUQ7H EXOS5_HUMAN Decreases Expression [5]
Protein reprimo (RPRM) OTNNBAS1 RPRM_HUMAN Decreases Expression [5]
E3 ubiquitin-protein ligase RNF146 (RNF146) OTE4CO7E RN146_HUMAN Increases Expression [5]
DNA damage-inducible transcript 4 protein (DDIT4) OTHY8SY4 DDIT4_HUMAN Decreases Expression [5]
CKLF-like MARVEL transmembrane domain-containing protein 6 (CMTM6) OT70T27A CKLF6_HUMAN Increases Expression [5]
Ankyrin repeat domain-containing protein 10 (ANKRD10) OTIZ2VK8 ANR10_HUMAN Increases Expression [5]
LIM and cysteine-rich domains protein 1 (LMCD1) OT3AWE8O LMCD1_HUMAN Decreases Expression [5]
Sentrin-specific protease 1 (SENP1) OTO8J4VV SENP1_HUMAN Increases Expression [5]
Phosphatidylethanolamine N-methyltransferase (PEMT) OTKXRUL9 PEMT_HUMAN Decreases Expression [5]
DnaJ homolog subfamily B member 9 (DNAJB9) OT38EQT6 DNJB9_HUMAN Increases Expression [5]
Alpha-catulin (CTNNAL1) OTESJ6JD CTNL1_HUMAN Increases Expression [5]
Alpha-N-acetylgalactosaminide alpha-2,6-sialyltransferase 2 (ST6GALNAC2) OT9PBQVT SIA7B_HUMAN Increases Expression [5]
Polypyrimidine tract-binding protein 2 (PTBP2) OTF4S7NE PTBP2_HUMAN Increases Expression [5]
Frizzled-4 (FZD4) OTGLZIE0 FZD4_HUMAN Increases Expression [5]
Frizzled-10 (FZD10) OTSAENLT FZD10_HUMAN Increases Expression [5]
Lysosomal thioesterase PPT2 (PPT2) OTD5VJ9A PPT2_HUMAN Increases Expression [5]
Sorting nexin-12 (SNX12) OTARRSWB SNX12_HUMAN Decreases Expression [5]
HIG1 domain family member 1A, mitochondrial (HIGD1A) OTS351DV HIG1A_HUMAN Increases Expression [5]
Band 4.1-like protein 3 (EPB41L3) OTS6CHG2 E41L3_HUMAN Increases Expression [5]
Long-chain fatty acid transport protein 5 (SLC27A5) OT4OK511 S27A5_HUMAN Decreases Expression [5]
Axin-2 (AXIN2) OTRMGQNU AXIN2_HUMAN Increases Expression [5]
Cytosolic Fe-S cluster assembly factor NUBP2 (NUBP2) OTYOTM2B NUBP2_HUMAN Increases Expression [5]
Adhesion G-protein coupled receptor G1 (ADGRG1) OTQBB8NT AGRG1_HUMAN Decreases Expression [5]
Calcineurin-binding protein cabin-1 (CABIN1) OT4G5CIK CABIN_HUMAN Increases Expression [5]
SEC23-interacting protein (SEC23IP) OTTZ0FXP S23IP_HUMAN Increases Expression [5]
11-beta-hydroxysteroid dehydrogenase type 2 (HSD11B2) OTHF4H9U DHI2_HUMAN Increases Expression [13]
Nitric oxide synthase 3 (NOS3) OTLDT7NR NOS3_HUMAN Decreases Expression [14]
Bile salt export pump (ABCB11) OTRU7THO ABCBB_HUMAN Decreases Activity [15]
Glucocorticoid receptor (NR3C1) OTCI2YDI GCR_HUMAN Decreases Expression [16]
ATP-binding cassette sub-family C member 3 (ABCC3) OTC3IJV4 MRP3_HUMAN Increases Expression [17]
Interleukin-1 receptor-associated kinase-like 2 (IRAK2) OT6Y1QZN IRAK2_HUMAN Decreases Expression [18]
Nuclear receptor subfamily 1 group I member 2 (NR1I2) OTC5U0N5 NR1I2_HUMAN Increases Activity [19]
T-cell surface glycoprotein CD4 (CD4) OT7Z5LNF CD4_HUMAN Decreases Expression [20]
Interleukin-6 (IL6) OTUOSCCU IL6_HUMAN Decreases Secretion [21]
Retinoblastoma-associated protein (RB1) OTQJUJMZ RB_HUMAN Increases Activity [22]
Progesterone receptor (PGR) OT0FZ3QE PRGR_HUMAN Decreases Activity [23]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Increases Cleavage [24]
Androgen receptor (AR) OTUBKAZZ ANDR_HUMAN Decreases Activity [25]
Apoptosis regulator Bcl-2 (BCL2) OT9DVHC0 BCL2_HUMAN Decreases Expression [26]
Cyclin-A2 (CCNA2) OTPHHYZJ CCNA2_HUMAN Decreases Expression [27]
Brain-derived neurotrophic factor (BDNF) OTLGH7EW BDNF_HUMAN Decreases Expression [28]
Aryl hydrocarbon receptor (AHR) OTFE4EYE AHR_HUMAN Increases Activity [19]
Caspase-3 (CASP3) OTIJRBE7 CASP3_HUMAN Decreases Expression [24]
Proliferation marker protein Ki-67 (MKI67) OTA8N1QI KI67_HUMAN Decreases Expression [29]
Cyclin-dependent kinase inhibitor 1B (CDKN1B) OTNY5LLZ CDN1B_HUMAN Increases Expression [30]
Tumor necrosis factor ligand superfamily member 6 (FASLG) OTZARCHH TNFL6_HUMAN Increases Expression [26]
Cathelicidin antimicrobial peptide (CAMP) OT3Y8011 CAMP_HUMAN Decreases Expression [18]
Forkhead box protein L2 (FOXL2) OTFRQUYL FOXL2_HUMAN Increases Expression [30]
Neutrophil defensin 1 (DEFA1) OT5N1B9B DEF1_HUMAN Decreases Expression [18]
Neutrophil defensin 3 (DEFA3) OTO3N8E1 DEF3_HUMAN Decreases Expression [18]
Transcription factor E2F1 (E2F1) OTLKYBBC E2F1_HUMAN Decreases Expression [27]
Apoptosis regulator BAX (BAX) OTAW0V4V BAX_HUMAN Increases Expression [26]
Protein GREB1 (GREB1) OTU6ZA26 GREB1_HUMAN Increases Expression [31]
Progesterone-induced-blocking factor 1 (PIBF1) OTCBT1A1 PIBF1_HUMAN Decreases Expression [18]
Interleukin-1 receptor-associated kinase 4 (IRAK4) OT9JTJWC IRAK4_HUMAN Decreases Expression [18]
Toll-like receptor 7 (TLR7) OT3HZV7Z TLR7_HUMAN Decreases Expression [18]
Semaphorin-3B (SEMA3B) OTCZCPMS SEM3B_HUMAN Increases Response To Substance [32]
Semaphorin-3F (SEMA3F) OTQFMS8S SEM3F_HUMAN Increases Response To Substance [32]
------------------------------------------------------------------------------------
⏷ Show the Full List of 228 DOT(s)
Indication(s) of Letrozole
Disease Entry ICD 11 Status REF
Estrogen-receptor positive breast cancer N.A. Approved [3]
Hormonally-responsive breast cancer 2C60-2C65 Approved [4]
Letrozole Interacts with 1 DTT Molecule(s)
DTT Name DTT ID UniProt ID Mode of Action REF
Aromatase (CYP19A1) TTSZLWK CP19A_HUMAN Inhibitor [33]
------------------------------------------------------------------------------------
Letrozole Interacts with 3 DME Molecule(s)
DME Name DME ID UniProt ID Mode of Action REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Metabolism [34]
Aromatase (CYP19A1) DEQX145 CP19A_HUMAN Metabolism [35]
Cytochrome P450 2A6 (CYP2A6) DEJVYAZ CP2A6_HUMAN Metabolism [36]
------------------------------------------------------------------------------------
Letrozole Interacts with 18 DOT Molecule(s)
DOT Name DOT ID UniProt ID Mode of Action REF
Aromatase (CYP19A1) OTZ6XF74 CP19A_HUMAN Decreases Activity [37]
Cytochrome P450 3A4 (CYP3A4) OTQGYY83 CP3A4_HUMAN Increases Oxidation [38]
Cytochrome P450 2A6 (CYP2A6) OT52TWG3 CP2A6_HUMAN Increases Oxidation [38]
Adenylate kinase isoenzyme 1 (AK1) OT614AR3 KAD1_HUMAN Increases ADR [11]
Dickkopf-related protein 1 (DKK1) OTRDLUSP DKK1_HUMAN Increases Expression [39]
Follitropin subunit beta (FSHB) OTGLS283 FSHB_HUMAN Increases Expression [40]
Lutropin subunit beta (LHB) OT5GBOVJ LSHB_HUMAN Increases Expression [40]
Progesterone receptor (PGR) OT0FZ3QE PRGR_HUMAN Decreases Expression [41]
Leukemia inhibitory factor (LIF) OTO46S5S LIF_HUMAN Increases Expression [39]
Gap junction alpha-1 protein (GJA1) OTT94MKL CXA1_HUMAN Decreases Expression [42]
G1/S-specific cyclin-D1 (CCND1) OT8HPTKJ CCND1_HUMAN Decreases Expression [43]
G1/S-specific cyclin-D2 (CCND2) OTDULQF9 CCND2_HUMAN Decreases Expression [43]
Cyclin-dependent kinase inhibitor 1 (CDKN1A) OTQWHCZE CDN1A_HUMAN Increases Expression [44]
Leukemia inhibitory factor receptor (LIFR) OT36W9O5 LIFR_HUMAN Increases Expression [39]
Proliferation marker protein Ki-67 (MKI67) OTA8N1QI KI67_HUMAN Decreases Expression [41]
Small ribosomal subunit protein eS6 (RPS6) OTT4D1LN RS6_HUMAN Decreases Phosphorylation [43]
Lanosterol 14-alpha demethylase (CYP51A1) OTAYHG9C CP51A_HUMAN Decreases Activity [45]
Fibroblast growth factor 22 (FGF22) OTVIX6J0 FGF22_HUMAN Increases Expression [39]
------------------------------------------------------------------------------------
⏷ Show the Full List of 18 DOT(s)

References

1 ClinicalTrials.gov (NCT01475318) Study on Combined Use of Letrozole, Mifepristone and Misoprostol in Termination of Pregnancy
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: 2805).
3 Letrozole FDA Label
4 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: 5209).
5 Mifepristone induced progesterone withdrawal reveals novel regulatory pathways in human endometrium. Mol Hum Reprod. 2007 Sep;13(9):641-54.
6 [Induction of apoptosis by mifepristone in androgen-independent prostate cancer cell lines in vitro]. Zhonghua Wai Ke Za Zhi. 2006 Mar 15;44(6):382-5.
7 The glucocorticoid agonist activities of mifepristone (RU486) and progesterone are dependent on glucocorticoid receptor levels but not on EC50 values. Steroids. 2007 Jun;72(6-7):600-8.
8 Evaluation of strategies for the assessment of drug-drug interactions involving cytochrome P450 enzymes. Eur J Drug Metab Pharmacokinet. 2018 Dec;43(6):737-750.
9 Comparative analysis of substrate and inhibitor interactions with CYP3A4 and CYP3A5. Xenobiotica. 2006 Apr;36(4):287-99.
10 A cell-based reporter gene assay for determining induction of CYP3A4 in a high-volume system. J Pharmacol Exp Ther. 2002 Oct;303(1):412-23.
11 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
12 Ketoconazole and miconazole are antagonists of the human glucocorticoid receptor: consequences on the expression and function of the constitutive androstane receptor and the pregnane X receptor. Mol Pharmacol. 2006 Jul;70(1):329-39.
13 Effect of the interaction between lipoxygenase pathway and progesterone on the regulation of hydroxysteroid 11-Beta dehydrogenase 2 in cultured human term placental trophoblasts. Biol Reprod. 2008 Mar;78(3):514-20.
14 Influence of progesterone on endometrial nitric oxide synthase expression. Fertil Steril. 2009 May;91(5 Suppl):2157-62.
15 A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development. Toxicol Sci. 2013 Nov;136(1):216-41.
16 Metformin suppresses CYP1A1 and CYP1B1 expression in breast cancer cells by down-regulating aryl hydrocarbon receptor expression. Toxicol Appl Pharmacol. 2014 Oct 1;280(1):138-48.
17 Induction of ABCC3 (MRP3) by pregnane X receptor activators. Drug Metab Dispos. 2003 Nov;31(11):1296-9. doi: 10.1124/dmd.31.11.1296.
18 Expression and modulation of progesterone induced blocking factor (PIBF) and innate immune factors in human leukemia cell lines by progesterone and mifepristone. Leuk Lymphoma. 2007 Aug;48(8):1610-7. doi: 10.1080/10428190701471999.
19 Improved assays for xenosensor activation based on reverse transfection. Toxicol In Vitro. 2015 Oct;29(7):1759-65. doi: 10.1016/j.tiv.2015.07.011. Epub 2015 Jul 14.
20 Rimexolone inhibits proliferation, cytokine expression and signal transduction of human CD4+ T-cells. Immunol Lett. 2010 Jun 15;131(1):24-32. doi: 10.1016/j.imlet.2010.03.009. Epub 2010 Apr 2.
21 [Regulatory effects of mifepristone and progesterone on the secretion of interleukin-6 by cultured eutopic and etopic endometrial cells]. Zhonghua Fu Chan Ke Za Zhi. 2001 Oct;36(10):603-5.
22 Mifepristone induces growth arrest, caspase activation, and apoptosis of estrogen receptor-expressing, antiestrogen-resistant breast cancer cells. Clin Cancer Res. 2004 Aug 1;10(15):5215-25. doi: 10.1158/1078-0432.CCR-03-0637.
23 The estrogenic activity of synthetic progestins used in oral contraceptives enhances fatty acid synthase-dependent breast cancer cell proliferation and survival. Int J Oncol. 2005 Jun;26(6):1507-15.
24 Effects of progesterone and anti-progestin (mifepristone) treatment on proliferation and apoptosis of the human ovarian cancer cell line, OVCAR-3. Oncol Rep. 2006 Apr;15(4):743-8.
25 Chemical genomics profiling of environmental chemical modulation of human nuclear receptors. Environ Health Perspect. 2011 Aug;119(8):1142-8. doi: 10.1289/ehp.1002952. Epub 2011 May 4.
26 Effect of mifepristone on proliferation and apoptosis of Ishikawa endometrial adenocarcinoma cells. Fertil Steril. 2005 Jul;84(1):202-11. doi: 10.1016/j.fertnstert.2005.01.126.
27 Mifepristone inhibits ovarian cancer cell growth in vitro and in vivo. Clin Cancer Res. 2007 Jun 1;13(11):3370-9. doi: 10.1158/1078-0432.CCR-07-0164.
28 Changes in brain-derived neurotrophic factor following treatment with mifepristone in bipolar disorder and schizophrenia. Aust N Z J Psychiatry. 2007 Apr;41(4):321-6. doi: 10.1080/00048670701213211.
29 The effect of mifepristone on breast cell proliferation in premenopausal women evaluated through fine needle aspiration cytology. Hum Reprod. 2008 Sep;23(9):2072-9. doi: 10.1093/humrep/den228. Epub 2008 Jun 24.
30 MiR-17-5p/FOXL2/CDKN1B signal programming in oocytes mediates transgenerational inheritance of diminished ovarian reserve in female offspring rats induced by prenatal dexamethasone exposure. Cell Biol Toxicol. 2023 Jun;39(3):867-883. doi: 10.1007/s10565-021-09645-6. Epub 2021 Sep 19.
31 A Gene Expression Biomarker Identifies Chemical Modulators of Estrogen Receptor in an MCF-7 Microarray Compendium. Chem Res Toxicol. 2021 Feb 15;34(2):313-329. doi: 10.1021/acs.chemrestox.0c00243. Epub 2021 Jan 6.
32 Progesterone and 1,25-dihydroxyvitamin D? inhibit endometrial cancer cell growth by upregulating semaphorin 3B and semaphorin 3F. Mol Cancer Res. 2011 Nov;9(11):1479-92. doi: 10.1158/1541-7786.MCR-11-0213. Epub 2011 Sep 20.
33 Aromatase inhibitors--theoretical concept and present experiences in the treatment of endometriosis. Zentralbl Gynakol. 2003 Jul-Aug;125(7-8):247-51.
34 Inhibition of drug metabolizing cytochrome P450s by the aromatase inhibitor drug letrozole and its major oxidative metabolite 4,4'-methanol-bisbenzonitrile in vitro. Cancer Chemother Pharmacol. 2009 Oct;64(5):867-75.
35 Double-blind, randomised, multicentre endocrine trial comparing two letrozole doses, in postmenopausal breast cancer patients. Eur J Cancer. 1999 Feb;35(2):208-13.
36 Letrozole concentration is associated with CYP2A6 variation but not with arthralgia in patients with breast cancer. Breast Cancer Res Treat. 2018 Nov;172(2):371-379.
37 Aromatase inhibition: translation into a successful therapeutic approach. Clin Cancer Res. 2005 Apr 15;11(8):2809-21. doi: 10.1158/1078-0432.CCR-04-2187.
38 Deactivation of anti-cancer drug letrozole to a carbinol metabolite by polymorphic cytochrome P450 2A6 in human liver microsomes. Xenobiotica. 2009 Nov;39(11):795-802. doi: 10.3109/00498250903171395.
39 Clomiphene citrate versus letrozole: molecular analysis of the endometrium in women with polycystic ovary syndrome. Fertil Steril. 2011 Oct;96(4):1051-6. doi: 10.1016/j.fertnstert.2011.07.1092.
40 Aromatase inhibition, testosterone, and seizures. Epilepsy Behav. 2004 Apr;5(2):260-3. doi: 10.1016/j.yebeh.2003.12.001.
41 Aromatase inhibitors: cellular and molecular effects. J Steroid Biochem Mol Biol. 2005 May;95(1-5):83-9. doi: 10.1016/j.jsbmb.2005.04.010.
42 Inhibition of estrogen receptor reduces connexin 43 expression in breast cancers. Toxicol Appl Pharmacol. 2018 Jan 1;338:182-190. doi: 10.1016/j.taap.2017.11.020. Epub 2017 Nov 24.
43 Dual inhibition of mTOR and estrogen receptor signaling in vitro induces cell death in models of breast cancer. Clin Cancer Res. 2005 Jul 15;11(14):5319-28. doi: 10.1158/1078-0432.CCR-04-2402.
44 Synergistic activity of letrozole and sorafenib on breast cancer cells. Breast Cancer Res Treat. 2010 Nov;124(1):79-88. doi: 10.1007/s10549-009-0714-5. Epub 2010 Jan 7.
45 Comparison of lanosterol-14 alpha-demethylase (CYP51) of human and Candida albicans for inhibition by different antifungal azoles. Toxicology. 2006 Nov 10;228(1):24-32. doi: 10.1016/j.tox.2006.08.007. Epub 2006 Aug 12.