Target Information
Target General Infomation | |||||
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Target ID |
T56625
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Former ID |
TTDR01033
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Target Name |
Tripeptidyl-peptidase II
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Gene Name |
TPP2
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Synonyms |
CCK-inactivating peptidase tripeptidyl peptidase; TPP II; TPP-II; Tripeptidyl aminopeptidase; TPP2
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Target Type |
Clinical Trial
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Disease | Obesity [ICD9: 278; ICD10: E66] | ||||
Function |
Component of the proteolytic cascade acting downstream of the 26S proteasome in the ubiquitin-proteasome pathway. May be able to complement the 26S proteasome function to some extent under conditions in which the latter is inhibited. Stimulates adipogenesis (By similarity).
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BioChemical Class |
Peptidase
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Target Validation |
T56625
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UniProt ID | |||||
EC Number |
EC 3.4.14.10
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Sequence |
MATAATEEPFPFHGLLPKKETGAASFLCRYPEYDGRGVLIAVLDTGVDPGAPGMQVTTDG
KPKIVDIIDTTGSGDVNTATEVEPKDGEIVGLSGRVLKIPASWTNPSGKYHIGIKNGYDF YPKALKERIQKERKEKIWDPVHRVALAEACRKQEEFDVANNGSSQANKLIKEELQSQVEL LNSFEKKYSDPGPVYDCLVWHDGEVWRACIDSNEDGDLSKSTVLRNYKEAQEYGSFGTAE MLNYSVNIYDDGNLLSIVTSGGAHGTHVASIAAGHFPEEPERNGVAPGAQILSIKIGDTR LSTMETGTGLIRAMIEVINHKCDLVNYSYGEATHWPNSGRICEVINEAVWKHNIIYVSSA GNNGPCLSTVGCPGGTTSSVIGVGAYVSPDMMVAEYSLREKLPANQYTWSSRGPSADGAL GVSISAPGGAIASVPNWTLRGTQLMNGTSMSSPNACGGIALILSGLKANNIDYTVHSVRR ALENTAVKADNIEVFAQGHGIIQVDKAYDYLVQNTSFANKLGFTVTVGNNRGIYLRDPVQ VAAPSDHGVGIEPVFPENTENSEKISLQLHLALTSNSSWVQCPSHLELMNQCRHINIRVD PRGLREGLHYTEVCGYDIASPNAGPLFRVPITAVIAAKVNESSHYDLAFTDVHFKPGQIR RHFIEVPEGATWAEVTVCSCSSEVSAKFVLHAVQLVKQRAYRSHEFYKFCSLPEKGTLTE AFPVLGGKAIEFCIARWWASLSDVNIDYTISFHGIVCTAPQLNIHASEGINRFDVQSSLK YEDLAPCITLKNWVQTLRPVSAKTKPLGSRDVLPNNRQLYEMVLTYNFHQPKSGEVTPSC PLLCELLYESEFDSQLWIIFDQNKRQMGSGDAYPHQYSLKLEKGDYTIRLQIRHEQISDL ERLKDLPFIVSHRLSNTLSLDIHENHSFALLGKKKSSNLTLPPKYNQPFFVTSLPDDKIP KGAGPGCYLAGSLTLSKTELGKKADVIPVHYYLIPPPTKTKNGSKDKEKDSEKEKDLKEE FTEALRDLKIQWMTKLDSSDIYNELKETYPNYLPLYVARLHQLDAEKERMKRLNEIVDAA NAVISHIDQTALAVYIAMKTDPRPDAATIKNDMDKQKSTLVDALCRKGCALADHLLHTQA QDGAISTDAEGKEEEGESPLDSLAETFWETTKWTDLFDNKVLTFAYKHALVNKMYGRGLK FATKLVEEKPTKENWKNCIQLMKLLGWTHCASFTENWLPIMYPPDYCVF |
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Drugs and Mode of Action | |||||
Inhibitor | (2S)-aminobutyryl-(R)-pipecolinic acid amide | Drug Info | [527857] | ||
(2S)-aminobutyryl-L-prolinamide | Drug Info | [527857] | |||
(2S)-aminobutyryl-L-proline (R)-sec-butylamide | Drug Info | [527857] | |||
(2S)-aminobutyryl-L-proline isobutylamide | Drug Info | [527857] | |||
(2S)-aminobutyryl-L-proline n-butylamide | Drug Info | [527857] | |||
(2S)-aminobutyryl-L-proline n-pentylamide | Drug Info | [527857] | |||
(2S)-aminobutyryl-L-proline n-propylamide | Drug Info | [527857] | |||
(2S)-aminobutyryl-L-proline-(2S)-methylbutylamide | Drug Info | [527857] | |||
Alpha-methylalanyl-L-proline butylamide | Drug Info | [527857] | |||
example 8 [WO1999033801A1] | Drug Info | [543629] | |||
L-isoleucyl-L-prolinamide | Drug Info | [527857] | |||
L-leucyl-L-prolinamide | Drug Info | [527857] | |||
L-norleucyl-L-prolinamide | Drug Info | [527857] | |||
L-norvalyl-L-prolinamide | Drug Info | [527857] | |||
L-valyl-L-prolinamide | Drug Info | [527857] | |||
L-valyl-L-proline benzylamide | Drug Info | [527857] | |||
L-valyl-L-proline hexylamide | Drug Info | [527857] | |||
peptide 4 | Drug Info | [529332] | |||
UCL-2000 and butabindide | Drug Info | [536122] | |||
Pathways | |||||
References | |||||
Ref 527857 | J Med Chem. 2005 Nov 17;48(23):7333-42.Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach to designing exopeptidase inhibitors. | ||||
Ref 529332 | Use of lantibiotic synthetases for the preparation of bioactive constrained peptides. Bioorg Med Chem Lett. 2008 May 15;18(10):3025-8. |
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