Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TT9V5JH)

• DTT Name: Phospholipase A2 (PLA2G1B)
• Synonyms: Secreted phospholipase A(2); Phosphatidylcholine 2-acylhydrolase 1B; PLA2G1B; Group IB phospholipase A2
• Gene Name: PLA2G1B
• DTT Type: Successful target; [1]
• BioChemical Class: Carboxylic ester hydrolase
• UniProt ID: PA21B_HUMAN
• TTD ID: T31479
• EC Number: EC 3.1.1.4
• Sequence:
  MKLLVLAVLLTVAAADSGISPRAVWQFRKMIKCVIPGSDPFLEYNNYGCYCGLGGSGTPV
  DELDKCCQTHDNCYDQAKKLDSCKFLLDNPYTHTYSYSCSGSAITCSSKNKECEAFICNC
  DRNAAICFSKAPYNKAHKNLDTKKYCQS
• Function: PA2 catalyzes the calcium-dependent hydrolysis of the 2- acyl groups in 3-sn-phosphoglycerides, this releases glycerophospholipids and arachidonic acid that serve as the precursors of signal molecules.
• KEGG Pathway:
  Glycerophospholipid metabolism (hsa00564)
  Ether lipid metabolism (hsa00565)
  Arachidonic acid metabolism (hsa00590)
  Linoleic acid metabolism (hsa00591)
  alpha-Linolenic acid metabolism (hsa00592)
  Metabolic pathways (hsa01100)
  Ras signaling pathway (hsa04014)
  Vascular smooth muscle contraction (hsa04270)
  Pancreatic secretion (hsa04972)
  Fat digestion and absorption (hsa04975)
• Reactome Pathway:
  Acyl chain remodelling of PE (R-HSA-1482839)
  Acyl chain remodelling of PI (R-HSA-1482922)
  Acyl chain remodelling of PC (R-HSA-1482788)
• BioCyc Pathway: MetaCyc:HS10199-MON

Molecular Interaction Atlas (MIA) of This DTT

5 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Cholic Acid	DM7OKQV	Cholelithiasis	DC11	Approved	[2]
Clobetasol	DMUXP52	Rosacea	ED90.0	Approved	[1]
Clocortolone	DM9ZMQH	Exanthem		Approved	[3]
Diflorasone	DMI9PRJ	Exanthem		Approved	[4]
Miltefosine	DMND304	Chronic urticaria		Approved	[5]

7 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
AllerB	DM78DOT	Allergy	4A80-4A85	Phase 2b	[6]
MANOALIDE	DMB4A8I	Arthritis	FA20	Phase 2	[7]
MRX-4	DMQZWYE	Allergic rhinitis	CA08.0	Phase 2	[8]
MRX-6	DMLVQKF	Contact dermatitis	EK0Z	Phase 2	[9]
URSOLIC ACID	DM4SOAW	Metabolic syndrome x	5C50-5D2Z	Phase 2	[10]
Varespladib	DM5JJ83	Snakebite	N.A.	Phase 2	[11]
Rilapladib	DMB9861	Arteriosclerosis	BD40	Phase 1	[12]

8 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Darapladib	DMSWLA3	Arteriosclerosis	BD40	Discontinued in Phase 3	[13]
BMY-30129	DMA4UCP	Pruritus	EC90	Discontinued in Phase 2	[14]
EPC-K1	DMZKBU9	Nerve injury	ND56.4	Discontinued in Phase 2	[15]
SC-106	DMTZ7E4	Rheumatoid arthritis	FA20	Discontinued in Phase 2	[16]
WAY-123641	DMPE5XM	Asthma	CA23	Discontinued in Phase 2	[17]
PF-05212372	DMD83VY	Asthma	CA23	Discontinued in Phase 1	[18]
SB-435495	DM92BXN	Arteriosclerosis	BD40	Discontinued in Phase 1	[19]
YM-26734	DMEHAI2	Rheumatoid arthritis	FA20	Terminated	[20]

28 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-Methyl-2,4-Pentanediol	DMD45CU	Discovery agent	N.A.	Investigative	[2]
3,9-dihydroxy-2,10-diprenylpterocap-6a-ene	DMXZ8RJ	Discovery agent	N.A.	Investigative	[21]
4'-hydroxy-6,3',5'-triprenylisoflavonone	DM7PWOL	Discovery agent	N.A.	Investigative	[21]
ABYSSINONE V	DMH3CK2	Discovery agent	N.A.	Investigative	[21]
Acetate Ion	DMD08RH	Discovery agent	N.A.	Investigative	[2]
AGN-190383	DM53R94	Discovery agent	N.A.	Investigative	[22]
Alpha-D-Mannose	DMF5DLW	Discovery agent	N.A.	Investigative	[2]
BM-162115	DMDNPML	Inflammation	1A00-CA43.1	Investigative	[23]
BOLINAQUINONE	DMVB6UG	Discovery agent	N.A.	Investigative	[24]
CACOSPONGIONOLIDE	DMIPJUS	Discovery agent	N.A.	Investigative	[25]
CACOSPONGIONOLIDE B	DMCSXNW	Discovery agent	N.A.	Investigative	[25]
Cacospongionolide E	DM2DYAV	Discovery agent	N.A.	Investigative	[25]
folipastatin	DMEPZ2I	Discovery agent	N.A.	Investigative	[26]
HELENAQUINONE	DM5MOLY	Discovery agent	N.A.	Investigative	[27]
Heptanoic Acid	DM4NY9H	Discovery agent	N.A.	Investigative	[28]
Hexane-1,6-Diol	DMWAPGI	Discovery agent	N.A.	Investigative	[2]
Hyrtiosulawesine	DMWLJ5S	Discovery agent	N.A.	Investigative	[29]
Lpc-Ether	DM1JGDM	Discovery agent	N.A.	Investigative	[2]
LY178002	DMI01YM	Discovery agent	N.A.	Investigative	[30]
LY256548	DM1KCHN	Discovery agent	N.A.	Investigative	[30]
Mepacrine	DMU8L7C	Discovery agent	N.A.	Investigative	[31]
methylglyoxal	DMRC3OZ	Discovery agent	N.A.	Investigative	[2]
N-Tridecanoic Acid	DMNZ37C	Discovery agent	N.A.	Investigative	[28]
P-Anisic Acid	DM8HWS9	Discovery agent	N.A.	Investigative	[2]
Petrosaspongiolide M	DMR8ZBT	Discovery agent	N.A.	Investigative	[32]
Petrosaspongiolide P	DMMVZFN	Discovery agent	N.A.	Investigative	[33]
SB-203347	DM3AWMF	Discovery agent	N.A.	Investigative	[34]
WA-8242-A1	DMNRBDP	Discovery agent	N.A.	Investigative	[35]

Molecular Expression Atlas (MEA) of This DTT

Disease Name	ICD 11	Studied Tissue	p-value	Fold-Change	Z-score
Coronary artery disease	BA80-BA8Z	Peripheral blood	2.72E-01	-0.04	-0.17
Asthma	CA23	Nasal and bronchial airway	5.61E-01	1.50E-02	0.03
Rheumatoid arthritis	FA20	Synovial tissue	2.65E-01	-0.08	-0.21
Atopic dermatitis	EA90	Skin	1.05E-05	-0.11	-0.87
Sensitive skin	EA90	Skin	2.98E-01	0.07	0.52

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