Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTQ7R2V)

• DTT Name: Tripeptidyl-peptidase II (TPP2)
• Synonyms: Tripeptidyl aminopeptidase; TPP2; TPP-II; TPP II; CCK-inactivating peptidase tripeptidyl peptidase
• Gene Name: TPP2
• DTT Type: Discontinued target; [1]
• BioChemical Class: Peptidase
• UniProt ID: TPP2_HUMAN
• TTD ID: T56625
• 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
• 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.
• Reactome Pathway: Antigen processing (R-HSA-983168)

Molecular Interaction Atlas (MIA) of This DTT

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
UCL-2000; butabindide	DML51D0	Obesity	5B81	Discontinued in Phase 1	[1]

18 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(2S)-aminobutyryl-(R)-pipecolinic acid amide	DMWQK86	Discovery agent	N.A.	Investigative	[2]
(2S)-aminobutyryl-L-prolinamide	DMG0QKL	Discovery agent	N.A.	Investigative	[2]
(2S)-aminobutyryl-L-proline (R)-sec-butylamide	DMTFP0Z	Discovery agent	N.A.	Investigative	[2]
(2S)-aminobutyryl-L-proline isobutylamide	DMO5ZEK	Discovery agent	N.A.	Investigative	[2]
(2S)-aminobutyryl-L-proline n-butylamide	DM12Q9O	Discovery agent	N.A.	Investigative	[2]
(2S)-aminobutyryl-L-proline n-pentylamide	DM1DJX2	Discovery agent	N.A.	Investigative	[2]
(2S)-aminobutyryl-L-proline n-propylamide	DM6WXJO	Discovery agent	N.A.	Investigative	[2]
(2S)-aminobutyryl-L-proline-(2S)-methylbutylamide	DMEWU6Z	Discovery agent	N.A.	Investigative	[2]
Alpha-methylalanyl-L-proline butylamide	DM7DBTZ	Discovery agent	N.A.	Investigative	[2]
example 8 [WO1999033801A1]	DMFSHXW	Discovery agent	N.A.	Investigative	[3]
L-isoleucyl-L-prolinamide	DMVSAUL	Discovery agent	N.A.	Investigative	[2]
L-leucyl-L-prolinamide	DM41MS3	Discovery agent	N.A.	Investigative	[2]
L-norleucyl-L-prolinamide	DM7V30L	Discovery agent	N.A.	Investigative	[2]
L-norvalyl-L-prolinamide	DMIXFGC	Discovery agent	N.A.	Investigative	[2]
L-valyl-L-prolinamide	DMH7TNA	Discovery agent	N.A.	Investigative	[2]
L-valyl-L-proline benzylamide	DMQZ13A	Discovery agent	N.A.	Investigative	[2]
L-valyl-L-proline hexylamide	DMX4DRV	Discovery agent	N.A.	Investigative	[2]
peptide 4	DM45RTZ	Discovery agent	N.A.	Investigative	[4]

References

• [1] Emerging drugs for obesity: linking novel biological mechanisms to pharmaceutical pipelines. Expert Opin Emerg Drugs. 2005 Aug;10(3):643-60.
• [2] Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach ... J Med Chem. 2005 Nov 17;48(23):7333-42.
• [3] URL: 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).
• [4] Use of lantibiotic synthetases for the preparation of bioactive constrained peptides. Bioorg Med Chem Lett. 2008 May 15;18(10):3025-8.