Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTHI19T)

• DTT Name: Staphylococcus Beta-lactamase (Stap-coc blaZ)
• Synonyms: blaZ; Cephalosporinase
• Gene Name: Stap-coc blaZ
• DTT Type: Successful target; [1]
• BioChemical Class: Carbon-nitrogen hydrolase
• UniProt ID: BLAC_STAAU
• TTD ID: T38179
• EC Number: EC 3.5.2.6
• Sequence:
  MKKLIFLIVIALVLSACNSNSSHAKELNDLEKKYNAHIGVYALDTKSGKEVKFNSDKRFA
  YASTSKAINSAILLEQVPYNKLNKKVHINKDDIVAYSPILEKYVGKDITLKALIEASMTY
  SDNTANNKIIKEIGGIKKVKQRLKELGDKVTNPVRYEIELNYYSPKSKKDTSTPAAFGKT
  LNKLIANGKLSKENKKFLLDLMLNNKSGDTLIKDGVPKDYKVADKSGQAITYASRNDVAF
  VYPKGQSEPIVLVIFTNKDNKSDKPNDKLISETAKSVMKEF
• Function: This protein is a serine beta-lactamase with a substrate specificity for cephalosporins.

Molecular Interaction Atlas (MIA) of This DTT

2 Approved Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Clavulanate	DM2FGRT	Bacteremia	1A73	Approved	[2]
Tazobactam	DM3XNUI	Appendicitis	DB10	Approved	[1]

13 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
CAZ AVI	DMPG4OM	Serious infection	1H0Z	Phase 3	[3]
Enmetazobactam	DMZKTYJ	Urinary tract infection	GC08	Phase 3	[4]
Vaborbactam	DMDCFXJ	Urinary tract infection	GC08	Phase 3	[5]
CXL	DM3JFZ2	Methicillin-resistant staphylococci infection	1A00-1A09	Phase 2	[6]
MK-7655	DMLMV0O	Bacterial infection	1A00-1C4Z	Phase 2	[7]
ETX0282	DMUBD0I	Urinary tract infection	GC08	Phase 1	[8]
ME-1071	DMEMQ5J	Bacterial infection	1A00-1C4Z	Phase 1	[9]
OP-0595	DMECVP9	Bacterial infection	1A00-1C4Z	Phase 1	[10]
QPX7728	DMEXZQ2	Bacterial infection	1A00-1C4Z	Phase 1	[11]
QPX7831	DMD2P1X	Gram-negative bacterial infection	1B74-1G40	Phase 1	[12]
RASV-Sp	DM4VTX6	Streptococcus infection	1B53	Phase 1	[13]
VNRX-5133	DMNZ6XH	Bacterial infection	1A00-1C4Z	Phase 1	[14]
XNW4107	DMT0747	Bacterial infection	1A00-1C4Z	Phase 1	[15]

9 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2085-P	DM0GMJ6	Otitis media	AA80-AB0Z	Discontinued in Phase 3	[16]
DA-7101	DMHSLVO	Gram-positive bacterial infection	1B74-1G40	Discontinued in Phase 3	[17]
P1A	DMWCAQD	Toxicity	N.A.	Discontinued in Phase 2	[18]
BRL-42715	DMBC12X	Bacterial infection	1A00-1C4Z	Terminated	[19]
CL-186659	DMYML2N	Bacterial infection	1A00-1C4Z	Terminated	[16]
Ro-48-1220	DMXMP3D	Bacterial infection	1A00-1C4Z	Terminated	[20]
Ro-48-5545	DM7AUF2	Bacterial infection	1A00-1C4Z	Terminated	[21]
Ro-48-8724	DM0RZEO	Multidrug resistant infection	MG51	Terminated	[22]
SB-236049	DM5JDH1	Bacterial infection	1A00-1C4Z	Terminated	[23]

43 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(P-Iodophenylacetylamino)Methylphosphinic Acid	DMB8NWI	Discovery agent	N.A.	Investigative	[24]
1-Aminopropane-1,2,3-tricarboxylic acid	DMPYCK5	Discovery agent	N.A.	Investigative	[25]
2-(N-Morpholino)-Ethanesulfonic Acid	DMZVHSB	Discovery agent	N.A.	Investigative	[24]
2-(Sulfanylmethyl)phenylphosphonic acid	DM5CEG8	Discovery agent	N.A.	Investigative	[26]
2-mercaptophenylphosphonic acid	DM8HSBT	Discovery agent	N.A.	Investigative	[26]
2-Methyl-2,4-Pentanediol	DMD45CU	Discovery agent	N.A.	Investigative	[24]
2-phenyl-1H-imidazole-4-carboxylic acid	DMZI7O1	Discovery agent	N.A.	Investigative	[27]
3-Amino-3-(methoxycarbonyl)-1,5-pentandioic acid	DMV4XGT	Discovery agent	N.A.	Investigative	[25]
3-ethoxycarbonylpyroglutamate	DM4YL5Q	Discovery agent	N.A.	Investigative	[25]
3-Nitrophenylboronic Acid	DMPMX8R	Discovery agent	N.A.	Investigative	[24]
4,4'-Biphenyldiboronic Acid	DMFGQ02	Discovery agent	N.A.	Investigative	[24]
4-(Carboxyvin-2-Yl)Phenylboronic Acid	DMSG9LV	Discovery agent	N.A.	Investigative	[24]
4-Carboxyphenylboronic Acid	DM8A2QO	Discovery agent	N.A.	Investigative	[24]
4-iodo-acetamido phenylboronic acid	DMFSH2I	Discovery agent	N.A.	Investigative	[24]
4-Methyl-3-(2-oxo-azetidin-1-yl)-benzoic acid	DMH6QZO	Discovery agent	N.A.	Investigative	[28]
4-[(METHYLSULFONYL)AMINO]BENZOIC ACID	DMXKT6M	Discovery agent	N.A.	Investigative	[27]
5-Fluoro-2-sulfanyl-phenylphosphonic acid	DMUCLAV	Discovery agent	N.A.	Investigative	[26]
5-hydroxymethylbenzo[b]thiophen-2-ylboronic acid	DMN9FPV	Discovery agent	N.A.	Investigative	[29]
5-methyl-benzo[b]thiophen-2-ylboronic acid	DMLJVB7	Discovery agent	N.A.	Investigative	[29]
Acetate Ion	DMD08RH	Discovery agent	N.A.	Investigative	[24]
Acylated Ceftazidime	DMIZ5VO	Discovery agent	N.A.	Investigative	[24]
Alpha-Sulfanyl(2,4-dichlorobenzyl)phosphonic acid	DMWL172	Discovery agent	N.A.	Investigative	[26]
Alpha-Sulfanyl(2-methoxybenzyl)phosphonic acid	DM42M6I	Discovery agent	N.A.	Investigative	[26]
Alpha-Sulfanyl(4-bromobenzyl)phosphonic acid	DMRIWDV	Discovery agent	N.A.	Investigative	[26]
Alpha-Sulfanyl(4-chlorobenzyl)phosphonic acid	DMP6GXU	Discovery agent	N.A.	Investigative	[26]
Alpha-Sulfanyl(4-fluorobenzyl)phosphonic acid	DMP9V42	Discovery agent	N.A.	Investigative	[26]
Alpha-Sulfanylbenzylphosphonic acid	DMWB07I	Discovery agent	N.A.	Investigative	[26]
Alpha-Sulfanylpropylphosphonic acid	DM19NAI	Discovery agent	N.A.	Investigative	[26]
Benzo[b]thiophen-2-ylboronic acid	DMJQSLW	Discovery agent	N.A.	Investigative	[24]
Carbamic Acid	DMJQ3LN	Discovery agent	N.A.	Investigative	[24]
Degraded Cephaloridine	DMKRT20	Discovery agent	N.A.	Investigative	[24]
Diisopropyl 1-mercaptopropylphosphonate	DMNR439	Discovery agent	N.A.	Investigative	[26]
Diisopropyl 2-(sulfanylmethyl)phenylphosphonate	DMVFJAH	Discovery agent	N.A.	Investigative	[26]
Diisopropyl mercapto(phenyl)methylphosphonate	DMHKE3M	Discovery agent	N.A.	Investigative	[26]
Hydrolyzed Cephalothin	DMWH92F	Discovery agent	N.A.	Investigative	[24]
M-Aminophenylboronic Acid	DM213MD	Discovery agent	N.A.	Investigative	[24]
N-2-Thiophen-2-Yl-Acetamide Boronic Acid	DMLK0J8	Discovery agent	N.A.	Investigative	[24]
PCNOTAXIME GROUP	DMGS6YH	Discovery agent	N.A.	Investigative	[27]
Sucrose	DMVWUCF	Discovery agent	N.A.	Investigative	[30]
Thiophene-2-ylboronic acid	DML3OHW	Discovery agent	N.A.	Investigative	[29]
Tribenzyl 2-aminopropane-1,2,3-tricarboxylate	DMYSX0K	Discovery agent	N.A.	Investigative	[25]
Triethyl 2-aminopropane-1,2,3-tricarboxylate	DM5Q7K8	Discovery agent	N.A.	Investigative	[25]
[[N-(Benzyloxycarbonyl)Amino]Methyl]Phosphate	DM86305	Discovery agent	N.A.	Investigative	[24]

References

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