Details of the Drug Therapeutic Target (DTT)

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

• DTT Name: Signal transducer and activator of transcription 5 (STAT5)
• Synonyms: Signal transducer and activator of transcription 5
• Gene Name: STAT5A
• DTT Type: Patented-recorded target; [1]
• UniProt ID: STA5A_HUMAN ; STA5B_HUMAN
• TTD ID: T20027
• Sequence:
  MAGWIQAQQLQGDALRQMQVLYGQHFPIEVRHYLAQWIESQPWDAIDLDNPQDRAQATQL
  LEGLVQELQKKAEHQVGEDGFLLKIKLGHYATQLQKTYDRCPLELVRCIRHILYNEQRLV
  REANNCSSPAGILVDAMSQKHLQINQTFEELRLVTQDTENELKKLQQTQEYFIIQYQESL
  RIQAQFAQLAQLSPQERLSRETALQQKQVSLEAWLQREAQTLQQYRVELAEKHQKTLQLL
  RKQQTIILDDELIQWKRRQQLAGNGGPPEGSLDVLQSWCEKLAEIIWQNRQQIRRAEHLC
  QQLPIPGPVEEMLAEVNATITDIISALVTSTFIIEKQPPQVLKTQTKFAATVRLLVGGKL
  NVHMNPPQVKATIISEQQAKSLLKNENTRNECSGEILNNCCVMEYHQATGTLSAHFRNMS
  LKRIKRADRRGAESVTEEKFTVLFESQFSVGSNELVFQVKTLSLPVVVIVHGSQDHNATA
  TVLWDNAFAEPGRVPFAVPDKVLWPQLCEALNMKFKAEVQSNRGLTKENLVFLAQKLFNN
  SSSHLEDYSGLSVSWSQFNRENLPGWNYTFWQWFDGVMEVLKKHHKPHWNDGAILGFVNK
  QQAHDLLINKPDGTFLLRFSDSEIGGITIAWKFDSPERNLWNLKPFTTRDFSIRSLADRL
  GDLSYLIYVFPDRPKDEVFSKYYTPVLAKAVDGYVKPQIKQVVPEFVNASADAGGSSATY
  MDQAPSPAVCPQAPYNMYPQNPDHVLDQDGEFDLDETMDVARHVEELLRRPMDSLDSRLS
  PPAGLFTSARGSLS
• Function: Involved in cytosolic signalling and in mediating the expression of specific genes. Aberrant STAT5 activity has been shown to be closely connected to a wide range of human cancers, and silencing this aberrant activity is an area of active research in medicinal chemistry.
• KEGG Pathway:
  ErbB signaling pathway (hsa04012)
  Necroptosis (hsa04217)
  JAK-STAT signaling pathway (hsa04630)
  Th1 and Th2 cell differentiation (hsa04658)
  Th17 cell differentiation (hsa04659)
  Prolactin signaling pathway (hsa04917)
  AGE-RAGE signaling pathway in diabetic complications (hsa04933)
  Growth hormone synthesis, secretion and action (hsa04935)
  Hepatitis B (hsa05161)
  Measles (hsa05162)
  Human T-cell leukemia virus 1 infection (hsa05166)
  Pathways in cancer (hsa05200)
  Viral carcinogenesis (hsa05203)
  Chemical carcinogenesis - receptor activation (hsa05207)
  Chronic myeloid leukemia (hsa05220)
  Acute myeloid leukemia (hsa05221)
  Non-small cell lung cancer (hsa05223)
• Reactome Pathway:
  Nuclear signaling by ERBB4 (R-HSA-1251985)
  Interleukin-7 signaling (R-HSA-1266695)
  Signaling by SCF-KIT (R-HSA-1433557)
  Signaling by cytosolic FGFR1 fusion mutants (R-HSA-1839117)
  Downstream signal transduction (R-HSA-186763)
  Signaling by Leptin (R-HSA-2586552)
  Interleukin-3, Interleukin-5 and GM-CSF signaling (R-HSA-512988)
  Interleukin-20 family signaling (R-HSA-8854691)
  Interleukin-15 signaling (R-HSA-8983432)
  Interleukin-9 signaling (R-HSA-8985947)
  Interleukin-2 signaling (R-HSA-9020558)
  Interleukin-21 signaling (R-HSA-9020958)
  Erythropoietin activates STAT5 (R-HSA-9027283)
  STAT5 Activation (R-HSA-9645135)
  Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants (R-HSA-9670439)
  Signaling by CSF3 (G-CSF) (R-HSA-9674555)
  STAT5 activation downstream of FLT3 ITD mutants (R-HSA-9702518)
  Signaling by FLT3 fusion proteins (R-HSA-9703465)
  Inactivation of CSF3 (G-CSF) signaling (R-HSA-9705462)
  Nuclear events stimulated by ALK signaling in cancer (R-HSA-9725371)
  Growth hormone receptor signaling (R-HSA-982772)
  Prolactin receptor signaling (R-HSA-1170546)

Molecular Interaction Atlas (MIA) of This DTT

5 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Indirubin derivative 1	DMB8673	N. A.	N. A.	Patented	[1]
Platinum IV complexe 1	DM8OYI4	N. A.	N. A.	Patented	[1]
PMID26394986-Compound-10	DMP8RQ4	N. A.	N. A.	Patented	[1]
PMID26394986-Compound-56	DMPNJ4X	N. A.	N. A.	Patented	[1]
PMID26394986-Compound-57	DMILUT8	N. A.	N. A.	Patented	[1]

References

• [1] A STAT inhibitor patent review: progress since 2011.Expert Opin Ther Pat. 2015;25(12):1397-421.