Target Information
| Target General Information | Top | |||||
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| Target ID |
T92794
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| Target Name |
Urea transporter 1 (SLC14A1)
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| Synonyms |
Urea transporter, erythrocyte; UTE; UT1; Solute carrier family 14 member 1; RACH1; JK; HUT11
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| Gene Name |
SLC14A1
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| Target Type |
Literature-reported target
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[1] | ||||
| Function |
Urea channel that facilitates transmembrane urea transport down a concentration gradient. A constriction of the transmembrane channel functions as selectivity filter through which urea is expected to pass in dehydrated form. The rate of urea conduction is increased by hypotonic stress. Plays an important role in the kidney medulla collecting ducts, where it allows rapid equilibration between the lumen of the collecting ducts and the interstitium, and thereby prevents water loss driven by the high concentration of urea in the urine. Facilitates urea transport across erythrocyte membranes. May also play a role in transmembrane water transport, possibly by indirect means.
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| BioChemical Class |
Urea transporter family
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| UniProt ID | ||||||
| Sequence |
MEDSPTMVRVDSPTMVRGENQVSPCQGRRCFPKALGYVTGDMKELANQLKDKPVVLQFID
WILRGISQVVFVNNPVSGILILVGLLVQNPWWALTGWLGTVVSTLMALLLSQDRSLIASG LYGYNATLVGVLMAVFSDKGDYFWWLLLPVCAMSMTCPIFSSALNSMLSKWDLPVFTLPF NMALSMYLSATGHYNPFFPAKLVIPITTAPNISWSDLSALELLKSIPVGVGQIYGCDNPW TGGIFLGAILLSSPLMCLHAAIGSLLGIAAGLSLSAPFEDIYFGLWGFNSSLACIAMGGM FMALTWQTHLLALGCALFTAYLGVGMANFMAEVGLPACTWPFCLATLLFLIMTTKNSNIY KMPLSKVTYPEENRIFYLQAKKRMVESPL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| Cell-based Target Expression Variations | Top | |||||
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| Cell-based Target Expression Variations | ||||||
| Drug Binding Sites of Target | Top | |||||
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| Ligand Name: B-Octylglucoside | Ligand Info | |||||
| Structure Description | X-ray Structure of the Human Urea Channel SLC14A1/UT1 | PDB:6QD5 | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | Yes | [2] |
| PDB Sequence |
FPKALGYVTG
40 DMKELANQLK50 DKPVVLQFID60 WILRGISQVV70 FVNNPVSGIL80 ILVGLLVQNP 90 WWALTGWLGT100 VVSTLMALLL110 SQDRSLIASG120 LYGYNATLVG130 VLMAVFSDKG 140 DYFWWLLLPV150 CAMSMTCPIF160 SSALNSVLSK170 WDLPVFTLPF180 NMALSMYLSA 190 TGHYNPFFPA200 KLVIPITTAP210 QISWSDLSAL220 ELLKSIPVGV230 GQIYGCDNPW 240 TGGIFLGAIL250 LSSPLMCLHA260 AIGSLLGIAA270 GLSLSAPFEN280 IYFGLWGFNS 290 SLACIAMGGM300 FMALTWQTHL310 LALGCALFTA320 YLGVGMANFM330 AEVGLPACTW 340 PFCLATLLFL350 IMTTKNSNIY360 KMPLSKVTYP370 EENRIFYLQA380 KKRMVE |
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ALA34
3.942
TYR37
3.833
GLU44
4.356
GLN48
3.976
GLN68
2.964
PHE71
3.657
ASN73
3.906
PRO90
4.903
LEU94
3.829
LEU105
3.910
LEU108
2.589
LEU109
4.207
SER111
3.057
ARG114
3.814
LEU116
3.843
LEU121
3.715
TYR122
3.400
LYS139
2.824
TYR142
3.061
PHE143
3.618
TRP144
2.872
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| Ligand Name: Cholesterol hemisuccinate | Ligand Info | |||||
| Structure Description | X-ray Structure of the Human Urea Channel SLC14A1/UT1 | PDB:6QD5 | ||||
| Method | X-ray diffraction | Resolution | 2.40 Å | Mutation | Yes | [2] |
| PDB Sequence |
FPKALGYVTG
40 DMKELANQLK50 DKPVVLQFID60 WILRGISQVV70 FVNNPVSGIL80 ILVGLLVQNP 90 WWALTGWLGT100 VVSTLMALLL110 SQDRSLIASG120 LYGYNATLVG130 VLMAVFSDKG 140 DYFWWLLLPV150 CAMSMTCPIF160 SSALNSVLSK170 WDLPVFTLPF180 NMALSMYLSA 190 TGHYNPFFPA200 KLVIPITTAP210 QISWSDLSAL220 ELLKSIPVGV230 GQIYGCDNPW 240 TGGIFLGAIL250 LSSPLMCLHA260 AIGSLLGIAA270 GLSLSAPFEN280 IYFGLWGFNS 290 SLACIAMGGM300 FMALTWQTHL310 LALGCALFTA320 YLGVGMANFM330 AEVGLPACTW 340 PFCLATLLFL350 IMTTKNSNIY360 KMPLSKVTYP370 EENRIFYLQA380 KKRMVE |
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| Click to View More Binding Site Information of This Target with Different Ligands | ||||||
| Different Human System Profiles of Target | Top |
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Human Similarity Proteins
of target is determined by comparing the sequence similarity of all human proteins with the target based on BLAST. The similarity proteins for a target are defined as the proteins with E-value < 0.005 and outside the protein families of the target.
A target that has fewer human similarity proteins outside its family is commonly regarded to possess a greater capacity to avoid undesired interactions and thus increase the possibility of finding successful drugs
(Brief Bioinform, 21: 649-662, 2020).
Human Tissue Distribution
of target is determined from a proteomics study that quantified more than 12,000 genes across 32 normal human tissues. Tissue Specificity (TS) score was used to define the enrichment of target across tissues.
The distribution of targets among different tissues or organs need to be taken into consideration when assessing the target druggability, as it is generally accepted that the wider the target distribution, the greater the concern over potential adverse effects
(Nat Rev Drug Discov, 20: 64-81, 2021).
Human Similarity Proteins
Human Tissue Distribution
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There is no similarity protein (E value < 0.005) for this target
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Note:
If a protein has TS (tissue specficity) scores at least in one tissue >= 2.5, this protein is called tissue-enriched (including tissue-enriched-but-not-specific and tissue-specific). In the plots, the vertical lines are at thresholds 2.5 and 4.
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| References | Top | |||||
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| REF 1 | Nanomolar-Potency 1,2,4-Triazoloquinoxaline Inhibitors of the Kidney Urea Transporter UT-A1. J Med Chem. 2018 Apr 12;61(7):3209-3217. | |||||
| REF 2 | X-ray Structure of the Human Urea Channel SLC14A1/UT1 | |||||
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