Target Information
| Target General Information | Top | |||||
|---|---|---|---|---|---|---|
| Target ID |
T93283
|
|||||
| Target Name |
Prostatic acid phosphatase (ACPP)
|
|||||
| Synonyms |
Thiamine monophosphatase; TMPase; PAP
Click to Show/Hide
|
|||||
| Gene Name |
ACPP
|
|||||
| Target Type |
Clinical trial target
|
[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Prostate cancer [ICD-11: 2C82] | |||||
| Function |
A non-specific tyrosine phosphatase that dephosphorylates a diverse number of substrates under acidic conditions (pH 4-6) including alkyl, aryl, and acyl orthophosphate monoesters and phosphorylated proteins. Has lipid phosphatase activity and inactivates lysophosphatidic acid in seminal plasma.
Click to Show/Hide
|
|||||
| UniProt ID | ||||||
| EC Number |
EC 3.1.3.2
|
|||||
| Sequence |
MRAAPLLLARAASLSLGFLFLLFFWLDRSVLAKELKFVTLVFRHGDRSPIDTFPTDPIKE
SSWPQGFGQLTQLGMEQHYELGEYIRKRYRKFLNESYKHEQVYIRSTDVDRTLMSAMTNL AALFPPEGVSIWNPILLWQPIPVHTVPLSEDQLLYLPFRNCPRFQELESETLKSEEFQKR LHPYKDFIATLGKLSGLHGQDLFGIWSKVYDPLYCESVHNFTLPSWATEDTMTKLRELSE LSLLSLYGIHKQKEKSRLQGGVLVNEILNHMKRATQIPSYKKLIMYSAHDTTVSGLQMAL DVYNGLLPPYASCHLTELYFEKGEYFVEMYYRNETQHEPYPLMLPGCSPSCPLERFAELV GPVIPQDWSTECMTTNSHQGTEDSTD Click to Show/Hide
|
|||||
| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| Drugs and Modes of Action | Top | |||||
|---|---|---|---|---|---|---|
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | MVI-816 | Drug Info | Phase 2 | Prostate cancer | [2] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Modulator | [+] 1 Modulator drugs | + | ||||
| 1 | MVI-816 | Drug Info | [1] | |||
| Cell-based Target Expression Variations | Top | |||||
|---|---|---|---|---|---|---|
| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| Ligand Name: alpha-Benzyl-aminobenzyl-phosphonic acid | Ligand Info | |||||
| Structure Description | Crystal Structures of Human Prostatic Acid Phosphatase in Complex with a Phosphate Ion and alpha-Benzylaminobenzylphosphonic Acid Update the Mechanistic Picture and Offer New Insights into Inhibitor Design | PDB:1ND5 | ||||
| Method | X-ray diffraction | Resolution | 2.90 Å | Mutation | No | [3] |
| PDB Sequence |
KELKFVTLVF
10 RHGDRSPIDT20 FPTDPIKESS30 WPQGFGQLTQ40 LGMEQHYELG50 EYIRKRYRKF 60 LNESYKHEQV70 YIRSTDVDRT80 LMSAMTNLAA90 LFPPEGVSIW100 NPILLWQPIP 110 VHTVPLSEDQ120 LLYLPFRNCP130 RFQELESETL140 KSEEFQKRLH150 PYKDFIATLG 160 KLSGLHGQDL170 FGIWSKVYDP180 LYCESVHNFT190 LPSWATEDTM200 TKLRELSELS 210 LLSLYGIHKQ220 KEKSRLQGGV230 LVNEILNHMK240 RATQIPSYKK250 LIMYSAHDTT 260 VSGLQMALDV270 YNGLLPPYAS280 CHLTELYFEK290 GEYFVEMYYR300 NETQHEPYPL 310 MLPGCSPSCP320 LERFAELVGP330 VIPQDWSTEC340 MT
|
|||||
|
|
||||||
| Ligand Name: n-Propyl-tartramic acid | Ligand Info | |||||
| Structure Description | STRUCTURAL ORIGINS OF L(+)-TARTRATE INHIBITION OF HUMAN PROSTATIC ACID PHOSPHATASE | PDB:2HPA | ||||
| Method | X-ray diffraction | Resolution | 2.90 Å | Mutation | No | [4] |
| PDB Sequence |
KELKFVTLVF
1010 RHGDRSPIDT1020 FPTDPIKESS1030 WPQGFGQLTQ1040 LGMEQHYELG1050 EYIRKRYRKF 1060 LNESYKHEQV1070 YIRSTDVDRT1080 LMSAMTNLAA1090 LFPPEGVSIW1100 NPILLWQPIP 1110 VHTVPLSEDQ1120 LLYLPFRNCP1130 RFQELESETL1140 KSEEFQKRLH1150 PYKDFIATLG 1160 KLSGLHGQDL1170 FGIWSKVYDP1180 LYCESVHNFT1190 LPSWATEDTM1200 TKLRELSELS 1210 LLSLYGIHKQ1220 KEKSRLQGGV1230 LVNEILNHMK1240 RATQIPSYKK1250 LIMYSAHDTT 1260 VSGLQMALDV1270 YNGLLPPYAS1280 CHLTELYFEK1290 GEYFVEMYYR1300 NETQHEPYPL 1310 MLPGCSPSCP1320 LERFAELVGP1330 VIPQDWSTEC1340 MT
|
|||||
|
|
||||||
| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
|---|---|
|
Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Similarity Proteins
Human Tissue Distribution
|
|
|
There is no similarity protein (E value < 0.005) for this target
|
|
Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
|
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Target Poor or Non Binders | Top | |||||
|---|---|---|---|---|---|---|
| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| References | Top | |||||
|---|---|---|---|---|---|---|
| REF 1 | Company report (Madisonvaccine) | |||||
| REF 2 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800039703) | |||||
| REF 3 | Crystal structures of human prostatic acid phosphatase in complex with a phosphate ion and alpha-benzylaminobenzylphosphonic acid update the mechanistic picture and offer new insights into inhibitor design. Biochemistry. 2003 Jan 21;42(2):383-9. | |||||
| REF 4 | Structural origins of L(+)-tartrate inhibition of human prostatic acid phosphatase. J Biol Chem. 1998 Nov 13;273(46):30406-9. | |||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.