Details of the Target

General Information of Target

Target ID LDTP01822
Target Name Kininogen-1 (KNG1)
Gene Name KNG1
Gene ID 3827
Synonyms
BDK; KNG; Kininogen-1; Alpha-2-thiol proteinase inhibitor; Fitzgerald factor; High molecular weight kininogen; HMWK; Williams-Fitzgerald-Flaujeac factor) [Cleaved into: Kininogen-1 heavy chain; T-kinin; Ile-Ser-Bradykinin; Bradykinin; Kallidin I; Lysyl-bradykinin; Kallidin II; Kininogen-1 light chain; Low molecular weight growth-promoting factor]
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MKLITILFLCSRLLLSLTQESQSEEIDCNDKDLFKAVDAALKKYNSQNQSNNQFVLYRIT
EATKTVGSDTFYSFKYEIKEGDCPVQSGKTWQDCEYKDAAKAATGECTATVGKRSSTKFS
VATQTCQITPAEGPVVTAQYDCLGCVHPISTQSPDLEPILRHGIQYFNNNTQHSSLFMLN
EVKRAQRQVVAGLNFRITYSIVQTNCSKENFLFLTPDCKSLWNGDTGECTDNAYIDIQLR
IASFSQNCDIYPGKDFVQPPTKICVGCPRDIPTNSPELEETLTHTITKLNAENNATFYFK
IDNVKKARVQVVAGKKYFIDFVARETTCSKESNEELTESCETKKLGQSLDCNAEVYVVPW
EKKIYPTVNCQPLGMISLMKRPPGFSPFRSSRIGEIKEETTVSPPHTSMAPAQDEERDSG
KEQGHTRRHDWGHEKQRKHNLGHGHKHERDQGHGHQRGHGLGHGHEQQHGLGHGHKFKLD
DDLEHQGGHVLDHGHKHKHGHGHGKHKNKGKKNGKHNGWKTEHLASSSEDSTTPSAQTQE
KTEGPTPIPSLAKPGVTVTFSDFQDSDLIATMMPPISPAPIQSDDDWIPDIQIDPNGLSF
NPISDFPDTTSPKCPGRPWKSVSEINPTTQMKESYYFDLTDGLS
Target Type
Clinical trial
Target Bioclass
Other
Subcellular location
Secreted, extracellular space
Function
Kininogens are inhibitors of thiol proteases. HMW-kininogen plays an important role in blood coagulation by helping to position optimally prekallikrein and factor XI next to factor XII; HMW-kininogen inhibits the thrombin- and plasmin-induced aggregation of thrombocytes. LMW-kininogen inhibits the aggregation of thrombocytes. LMW-kininogen is in contrast to HMW-kininogen not involved in blood clotting.; [Bradykinin]: The active peptide bradykinin is a potent vasodilatator that is released from HMW-kininogen shows a variety of physiological effects: (A) influence in smooth muscle contraction, (B) induction of hypotension, (C) natriuresis and diuresis, (D) decrease in blood glucose level, (E) it is a mediator of inflammation and causes (E1) increase in vascular permeability, (E2) stimulation of nociceptors (4E3) release of other mediators of inflammation (e.g. prostaglandins), (F) it has a cardioprotective effect (directly via bradykinin action, indirectly via endothelium-derived relaxing factor action).
TTD ID
T30731
Uniprot ID
P01042
DrugMap ID
TTDJ4MY
Ensemble ID
ENST00000287611.8
HGNC ID
HGNC:6383

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CAMA1 SNV: p.D641N .
COLO320 SNV: p.E61K .
HLF SNV: p.R428S DBIA    Probe Info 
HT SNV: p.E633D .
IGR1 SNV: p.D255N DBIA    Probe Info 
IGROV1 SNV: p.M375I .
JURKAT SNV: p.S621L .
MFE296 SNV: p.F256C .
MFE319 SNV: p.G504R .
NCIH1299 SNV: p.W360R .
NCIH1650 SNV: p.P382L .
SNGM SNV: p.N51T .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C328(1.70)  LDD3318  [1]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 A2058 C328(1.75)  LDD2253  [1]
 LDCM0023  KB03 A2058 C328(1.85)  LDD2670  [1]
 LDCM0024  KB05 MELHO C328(1.70)  LDD3318  [1]

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840