Target Information

Target General Infomation
Target ID
T56625
Former ID
TTDR01033
Target Name
Tripeptidyl-peptidase II
Gene Name
TPP2
Synonyms
CCK-inactivating peptidase tripeptidyl peptidase; TPP II; TPP-II; Tripeptidyl aminopeptidase; TPP2
Target Type
Clinical Trial
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).
BioChemical Class
Peptidase
Target Validation
T56625
UniProt ID
P29144
EC Number
EC 3.4.14.10
Sequence
MATAATEEPFPFHGLLPKKETGAASFLCRYPEYDGRGVLIAVLDTGVDPGAPGMQVTTDG
KPKIVDIIDTTGSGDVNTATEVEPKDGEIVGLSGRVLKIPASWTNPSGKYHIGIKNGYDF
YPKALKERIQKERKEKIWDPVHRVALAEACRKQEEFDVANNGSSQANKLIKEELQSQVEL
LNSFEKKYSDPGPVYDCLVWHDGEVWRACIDSNEDGDLSKSTVLRNYKEAQEYGSFGTAE
MLNYSVNIYDDGNLLSIVTSGGAHGTHVASIAAGHFPEEPERNGVAPGAQILSIKIGDTR
LSTMETGTGLIRAMIEVINHKCDLVNYSYGEATHWPNSGRICEVINEAVWKHNIIYVSSA
GNNGPCLSTVGCPGGTTSSVIGVGAYVSPDMMVAEYSLREKLPANQYTWSSRGPSADGAL
GVSISAPGGAIASVPNWTLRGTQLMNGTSMSSPNACGGIALILSGLKANNIDYTVHSVRR
ALENTAVKADNIEVFAQGHGIIQVDKAYDYLVQNTSFANKLGFTVTVGNNRGIYLRDPVQ
VAAPSDHGVGIEPVFPENTENSEKISLQLHLALTSNSSWVQCPSHLELMNQCRHINIRVD
PRGLREGLHYTEVCGYDIASPNAGPLFRVPITAVIAAKVNESSHYDLAFTDVHFKPGQIR
RHFIEVPEGATWAEVTVCSCSSEVSAKFVLHAVQLVKQRAYRSHEFYKFCSLPEKGTLTE
AFPVLGGKAIEFCIARWWASLSDVNIDYTISFHGIVCTAPQLNIHASEGINRFDVQSSLK
YEDLAPCITLKNWVQTLRPVSAKTKPLGSRDVLPNNRQLYEMVLTYNFHQPKSGEVTPSC
PLLCELLYESEFDSQLWIIFDQNKRQMGSGDAYPHQYSLKLEKGDYTIRLQIRHEQISDL
ERLKDLPFIVSHRLSNTLSLDIHENHSFALLGKKKSSNLTLPPKYNQPFFVTSLPDDKIP
KGAGPGCYLAGSLTLSKTELGKKADVIPVHYYLIPPPTKTKNGSKDKEKDSEKEKDLKEE
FTEALRDLKIQWMTKLDSSDIYNELKETYPNYLPLYVARLHQLDAEKERMKRLNEIVDAA
NAVISHIDQTALAVYIAMKTDPRPDAATIKNDMDKQKSTLVDALCRKGCALADHLLHTQA
QDGAISTDAEGKEEEGESPLDSLAETFWETTKWTDLFDNKVLTFAYKHALVNKMYGRGLK
FATKLVEEKPTKENWKNCIQLMKLLGWTHCASFTENWLPIMYPPDYCVF
Drugs and Mode of Action
Drug(s) UCL-2000 and butabindide Drug Info Discontinued in Phase 1 Obesity [1]
Inhibitor (2S)-aminobutyryl-(R)-pipecolinic acid amide Drug Info [2]
(2S)-aminobutyryl-L-prolinamide Drug Info [2]
(2S)-aminobutyryl-L-proline (R)-sec-butylamide Drug Info [2]
(2S)-aminobutyryl-L-proline isobutylamide Drug Info [2]
(2S)-aminobutyryl-L-proline n-butylamide Drug Info [2]
(2S)-aminobutyryl-L-proline n-pentylamide Drug Info [2]
(2S)-aminobutyryl-L-proline n-propylamide Drug Info [2]
(2S)-aminobutyryl-L-proline-(2S)-methylbutylamide Drug Info [2]
Alpha-methylalanyl-L-proline butylamide Drug Info [2]
example 8 [WO1999033801A1] Drug Info [3]
L-isoleucyl-L-prolinamide Drug Info [2]
L-leucyl-L-prolinamide Drug Info [2]
L-norleucyl-L-prolinamide Drug Info [2]
L-norvalyl-L-prolinamide Drug Info [2]
L-valyl-L-prolinamide Drug Info [2]
L-valyl-L-proline benzylamide Drug Info [2]
L-valyl-L-proline hexylamide Drug Info [2]
peptide 4 Drug Info [4]
UCL-2000 and butabindide Drug Info [5]
Pathways
Reactome Ubiquitination &amp
Proteasome degradation
References
REF 1Clinical pipeline report, company report or official report of University College London.
REF 2J 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 3(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2423).
REF 4Use of lantibiotic synthetases for the preparation of bioactive constrained peptides. Bioorg Med Chem Lett. 2008 May 15;18(10):3025-8.
REF 5Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.

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