Target General Infomation
Target ID
T77594
Former ID
TTDI02087
Target Name
78 kDa glucose-regulated protein
Gene Name
HSPA5
Synonyms
Endoplasmic reticulum lumenal Ca(2+)binding protein grp78; GRP78; Heat shock 70 kDa protein 5; Immunoglobulin heavy chainbinding protein; HSPA5
Target Type
Clinical Trial
Disease Melanoma [ICD9: 172; ICD10: C43]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Function
Probably plays a role in facilitating the assembly of multimeric protein complexes inside the endoplasmic reticulum. Involved in the correct folding of proteins and degradation of misfolded proteins via its interaction with DNAJC10, probably to facilitate the release of DNAJC10 from its substrate.
BioChemical Class
Heat shock protein
UniProt ID
Sequence
MKLSLVAAMLLLLSAARAEEEDKKEDVGTVVGIDLGTTYSCVGVFKNGRVEIIANDQGNR
ITPSYVAFTPEGERLIGDAAKNQLTSNPENTVFDAKRLIGRTWNDPSVQQDIKFLPFKVV
EKKTKPYIQVDIGGGQTKTFAPEEISAMVLTKMKETAEAYLGKKVTHAVVTVPAYFNDAQ
RQATKDAGTIAGLNVMRIINEPTAAAIAYGLDKREGEKNILVFDLGGGTFDVSLLTIDNG
VFEVVATNGDTHLGGEDFDQRVMEHFIKLYKKKTGKDVRKDNRAVQKLRREVEKAKRALS
SQHQARIEIESFYEGEDFSETLTRAKFEELNMDLFRSTMKPVQKVLEDSDLKKSDIDEIV
LVGGSTRIPKIQQLVKEFFNGKEPSRGINPDEAVAYGAAVQAGVLSGDQDTGDLVLLDVC
PLTLGIETVGGVMTKLIPRNTVVPTKKSQIFSTASDNQPTVTIKVYEGERPLTKDNHLLG
TFDLTGIPPAPRGVPQIEVTFEIDVNGILRVTAEDKGTGNKNKITITNDQNRLTPEEIER
MVNDAEKFAEEDKKLKERIDTRNELESYAYSLKNQIGDKEKLGGKLSSEDKETMEKAVEE
KIEWLESHQDADIEDFKAKKKELEEIVQPIISKLYGSAGPPPTGEEDTAEKDEL
Drugs and Mode of Action
Drug(s) IT-139 Drug Info Phase 1 Solid tumours [549255]
NKP-1339 Drug Info Phase 1 Solid tumours [523587]
SAM-6 Drug Info Phase 1 Melanoma [524124]
Inhibitor IT-139 Drug Info [544275]
NKP-1339 Drug Info [544275]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Protein export
Protein processing in endoplasmic reticulum
Antigen processing and presentation
Thyroid hormone synthesis
Prion diseases
NetPath Pathway TSH Signaling Pathway
TCR Signaling Pathway
PANTHER Pathway Apoptosis signaling pathway
Parkinson disease
PathWhiz Pathway Retinol Metabolism
Reactome Platelet degranulation
Regulation of HSF1-mediated heat shock response
WikiPathways MAPK Signaling Pathway
Apoptosis-related network due to altered Notch3 in ovarian cancer
Activation of Chaperone Genes by ATF6-alpha
Parkin-Ubiquitin Proteasomal System pathway
Unfolded Protein Response
Response to elevated platelet cytosolic Ca2+
References
Ref 523587ClinicalTrials.gov (NCT01415297) Dose Escalation Study of NKP-1339 to Treat Advanced Solid Tumors. U.S. National Institutes of Health.
Ref 524124ClinicalTrials.gov (NCT01727778) Safety and Preliminary Efficacy Study of the Antibody PAT-SM6 in Patients With Relapsed or Refractory Multiple Myeloma. U.S. National Institutes of Health.
Ref 549255Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034247)
Ref 529312A new tumor-specific variant of GRP78 as target for antibody-based therapy. Lab Invest. 2008 Apr;88(4):375-86.
Ref 544275NKP-1339, a first-in-class anticancer drug showing mild side effects and activity in patients suffering from advanced refractory cancer. BMC Pharmacol Toxicol. 2012; 13(Suppl 1): A82.

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