Details of Drug Off-Target (DOT)

General Information of Drug Off-Target (DOT) (ID: OTDP6ILW)

DOT Name	Bcl-2 homologous antagonist/killer (BAK1)
Synonyms	Apoptosis regulator BAK; Bcl-2-like protein 7; Bcl2-L-7
Gene Name	BAK1
UniProt ID	BAK_HUMAN
3D Structure	Download 2D Sequence (FASTA) Download 3D Structure (PDB) Download
PDB ID	1BXL ; 2IMS ; 2IMT ; 2JBY ; 2JCN ; 2LP8 ; 2M5B ; 2XPX ; 2YV6 ; 3I1H ; 3QBR ; 4D2L ; 4U2U ; 4U2V ; 4UF1 ; 5AJK ; 5FMI ; 5FMK ; 5VWV ; 5VWW ; 5VWX ; 5VWY ; 5VWZ ; 5VX0 ; 5VX1 ; 6ODH ; 6UXM ; 6UXN ; 6UXO ; 6UXP ; 6UXQ ; 6UXR ; 7K02 ; 7LK4 ; 7M5A ; 7M5B ; 7OFM ; 7OFO ; 8CZF ; 8CZG ; 8CZH ; 8GSV ; 8IGC
Pfam ID	PF00452
Sequence	MASGQGPGPPRQECGEPALPSASEEQVAQDTEEVFRSYVFYRHQQEQEAEGVAAPADPEM VTLPLQPSSTMGQVGRQLAIIGDDINRRYDSEFQTMLQHLQPTAENAYEYFTKIATSLFE SGINWGRVVALLGFGYRLALHVYQHGLTGFLGQVTRFVVDFMLHHCIARWIAQRGGWVAA LNLGNGPILNVLVVLGVVLLGQFVVRRFFKS
Function	Plays a role in the mitochondrial apoptotic process. Upon arrival of cell death signals, promotes mitochondrial outer membrane (MOM) permeabilization by oligomerizing to form pores within the MOM. This releases apoptogenic factors into the cytosol, including cytochrome c, promoting the activation of caspase 9 which in turn processes and activates the effector caspases.
Tissue Specificity	Expressed in a wide variety of tissues, with highest levels in the heart and skeletal muscle.
KEGG Pathway	Platinum drug resistance (hsa01524 ) Protein processing in endoplasmic reticulum (hsa04141 ) Apoptosis (hsa04210 ) Apoptosis - multiple species (hsa04215 ) Pathways of neurodegeneration - multiple diseases (hsa05022 ) Pathogenic Escherichia coli infection (hsa05130 ) Salmonella infection (hsa05132 ) Hepatitis C (hsa05160 ) Measles (hsa05162 ) Human cytomegalovirus infection (hsa05163 ) Influenza A (hsa05164 ) Human papillomavirus infection (hsa05165 ) Kaposi sarcoma-associated herpesvirus infection (hsa05167 ) Herpes simplex virus 1 infection (hsa05168 ) Epstein-Barr virus infection (hsa05169 ) Human immunodeficiency virus 1 infection (hsa05170 ) Pathways in cancer (hsa05200 ) Transcriptio.l misregulation in cancer (hsa05202 ) Viral carcinogenesis (hsa05203 ) MicroR.s in cancer (hsa05206 ) Colorectal cancer (hsa05210 ) Pancreatic cancer (hsa05212 ) Endometrial cancer (hsa05213 ) Glioma (hsa05214 ) Thyroid cancer (hsa05216 ) Basal cell carcinoma (hsa05217 ) Melanoma (hsa05218 ) Chronic myeloid leukemia (hsa05220 ) Small cell lung cancer (hsa05222 ) Non-small cell lung cancer (hsa05223 ) Breast cancer (hsa05224 ) Hepatocellular carcinoma (hsa05225 ) Gastric cancer (hsa05226 )
Reactome Pathway	Release of apoptotic factors from the mitochondria (R-HSA-111457 ) Pyroptosis (R-HSA-5620971 ) Activation and oligomerization of BAK protein (R-HSA-111452 )

Molecular Interaction Atlas (MIA) of This DOT

Molecular Interaction Atlas (MIA)

MIA Detail

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
Fluorouracil	DMUM7HZ	Approved	Bcl-2 homologous antagonist/killer (BAK1) increases the response to substance of Fluorouracil.	[65]
Etoposide	DMNH3PG	Approved	Bcl-2 homologous antagonist/killer (BAK1) increases the response to substance of Etoposide.	[66]
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72 Drug(s) Affected the Gene/Protein Processing of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Tretinoin	DM49DUI	Approved	Tretinoin decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[1]
Acetaminophen	DMUIE76	Approved	Acetaminophen increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[2]
Doxorubicin	DMVP5YE	Approved	Doxorubicin decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[3]
Cisplatin	DMRHGI9	Approved	Cisplatin increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[4]
Estradiol	DMUNTE3	Approved	Estradiol decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[5]
Ivermectin	DMDBX5F	Approved	Ivermectin decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[6]
Quercetin	DM3NC4M	Approved	Quercetin increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[7]
Arsenic trioxide	DM61TA4	Approved	Arsenic trioxide decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[8]
Hydrogen peroxide	DM1NG5W	Approved	Hydrogen peroxide decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[9]
Vorinostat	DMWMPD4	Approved	Vorinostat increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[10]
Methotrexate	DM2TEOL	Approved	Methotrexate increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[11]
Decitabine	DMQL8XJ	Approved	Decitabine increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[12]
Menadione	DMSJDTY	Approved	Menadione affects the expression of Bcl-2 homologous antagonist/killer (BAK1).	[13]
Dexamethasone	DMMWZET	Approved	Dexamethasone increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[14]
Bortezomib	DMNO38U	Approved	Bortezomib increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[15]
Rosiglitazone	DMILWZR	Approved	Rosiglitazone increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[16]
Aspirin	DM672AH	Approved	Aspirin increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[17]
Paclitaxel	DMLB81S	Approved	Paclitaxel increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[18]
Diclofenac	DMPIHLS	Approved	Diclofenac increases the activity of Bcl-2 homologous antagonist/killer (BAK1).	[19]
Indomethacin	DMSC4A7	Approved	Indomethacin increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[17]
Menthol	DMG2KW7	Approved	Menthol increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[20]
Melphalan	DMOLNHF	Approved	Melphalan increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[21]
Capsaicin	DMGMF6V	Approved	Capsaicin increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[23]
Methamphetamine	DMPM4SK	Approved	Methamphetamine increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[24]
Sorafenib	DMS8IFC	Approved	Sorafenib decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[25]
Ritonavir	DMU764S	Approved	Ritonavir increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[26]
Docetaxel	DMDI269	Approved	Docetaxel increases the activity of Bcl-2 homologous antagonist/killer (BAK1).	[27]
Isoproterenol	DMK7MEY	Approved	Isoproterenol decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[28]
Morphine	DMRMS0L	Approved	Morphine increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[29]
Romidepsin	DMT5GNL	Approved	Romidepsin increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[30]
Mechlorethamine	DM0CVXA	Approved	Mechlorethamine increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[21]
Thiotepa	DMIZKOP	Approved	Thiotepa increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[18]
Promethazine	DM6I5GR	Approved	Promethazine increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[31]
Dextroamphetamine	DMMIHVP	Approved	Dextroamphetamine increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[24]
Levamisole	DM5EN79	Approved	Levamisole increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[33]
Urethane	DM7NSI0	Phase 4	Urethane increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[34]
Resveratrol	DM3RWXL	Phase 3	Resveratrol increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[35]
Tamibarotene	DM3G74J	Phase 3	Tamibarotene increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[36]
Epigallocatechin gallate	DMCGWBJ	Phase 3	Epigallocatechin gallate decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[37]
Curcumin	DMQPH29	Phase 3	Curcumin decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[38]
Fenretinide	DMRD5SP	Phase 3	Fenretinide increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[39]
Camptothecin	DM6CHNJ	Phase 3	Camptothecin decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[3]
Atorvastatin	DMF28YC	Phase 3 Trial	Atorvastatin increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[40]
Genistein	DM0JETC	Phase 2/3	Genistein increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[41]
phorbol 12-myristate 13-acetate	DMJWD62	Phase 2	phorbol 12-myristate 13-acetate increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[42]
PD-0325901	DM27D4J	Phase 2	PD-0325901 increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[30]
URSOLIC ACID	DM4SOAW	Phase 2	URSOLIC ACID increases the activity of Bcl-2 homologous antagonist/killer (BAK1).	[43]
Delphinidin	DMS2WIN	Phase 2	Delphinidin increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[44]
Tetrandrine	DMAOJBX	Phase 1	Tetrandrine increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[46]
PF-3758309	DM36PKZ	Phase 1	PF-3758309 increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[47]
BETULINIC ACID	DMBUI2A	Phase 1	BETULINIC ACID increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[48]
PMID26394986-Compound-22	DM43Z1G	Patented	PMID26394986-Compound-22 increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[14]
Perillyl alcohol	DMFWC3O	Discontinued in Phase 2	Perillyl alcohol increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[50]
Dioscin	DM5H2W9	Preclinical	Dioscin increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[51]
Bisphenol A	DM2ZLD7	Investigative	Bisphenol A decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[52]
Coumarin	DM0N8ZM	Investigative	Coumarin increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[53]
Deguelin	DMXT7WG	Investigative	Deguelin increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[54]
3R14S-OCHRATOXIN A	DM2KEW6	Investigative	3R14S-OCHRATOXIN A decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[55]
Paraquat	DMR8O3X	Investigative	Paraquat decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[56]
geraniol	DMS3CBD	Investigative	geraniol increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[50]
Okadaic acid	DM47CO1	Investigative	Okadaic acid increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[57]
(E)-4-(3,5-dimethoxystyryl)phenol	DMYXI2V	Investigative	(E)-4-(3,5-dimethoxystyryl)phenol increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[58]
Linalool	DMGZQ5P	Investigative	Linalool increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[59]
Farnesol	DMV2X1B	Investigative	Farnesol increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[50]
LICOAGROCHACONE A	DMWY0TN	Investigative	LICOAGROCHACONE A increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[60]
NORCANTHARIDIN	DM9B6Y1	Investigative	NORCANTHARIDIN increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[61]
CHLORANIL	DMCHGF1	Investigative	CHLORANIL increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[62]
Hyperforin	DM2L3PE	Investigative	Hyperforin increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[63]
DEMETHOXYCURCUMIN	DMO5UGV	Investigative	DEMETHOXYCURCUMIN decreases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[38]
Methylenedioxymethamphetamine	DMYVU47	Investigative	Methylenedioxymethamphetamine increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[24]
PI-3065	DMCQUWI	Investigative	PI-3065 increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[64]
2-Amino-1-(4-methylthiophenyl)propane	DMJ2Z9G	Investigative	2-Amino-1-(4-methylthiophenyl)propane increases the expression of Bcl-2 homologous antagonist/killer (BAK1).	[24]
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⏷ Show the Full List of 72 Drug(s)

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

Drug Name	Drug ID	Highest Status	Interaction	REF
Sulindac	DM2QHZU	Approved	Sulindac affects the localization of Bcl-2 homologous antagonist/killer (BAK1).	[22]
Venetoclax	DM8I94Y	Approved	Venetoclax affects the folding of Bcl-2 homologous antagonist/killer (BAK1).	[32]
Mivebresib	DMCPF90	Phase 1	Mivebresib affects the folding of Bcl-2 homologous antagonist/killer (BAK1).	[32]
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3 Drug(s) Affected the Post-Translational Modifications of This DOT

Drug Name	Drug ID	Highest Status	Interaction	REF
Benzo(a)pyrene	DMN7J43	Phase 1	Benzo(a)pyrene decreases the methylation of Bcl-2 homologous antagonist/killer (BAK1).	[45]
AMG 176	DM0Q7NO	Phase 1	AMG 176 decreases the ubiquitination of Bcl-2 homologous antagonist/killer (BAK1).	[49]
MG-132	DMKA2YS	Preclinical	MG-132 increases the ubiquitination of Bcl-2 homologous antagonist/killer (BAK1).	[49]
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