Details of the Target
General Information of Target
Target ID | LDTP10637 | |||||
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Target Name | Proton-coupled folate transporter (SLC46A1) | |||||
Gene Name | SLC46A1 | |||||
Gene ID | 113235 | |||||
Synonyms |
G21; HCP1; PCFT; Proton-coupled folate transporter; HsPCFT; hPCFT; Heme carrier protein 1; PCFT/HCP1; Solute carrier family 46 member 1 |
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3D Structure | ||||||
Sequence |
MRTEAEAAGPPLEPGDFVQLPVPVIQQLYHWDCGLACSRMVLRYLGQLDDSEFERALQKL
QLTRSIWTIDLAYLMHHFGVRHRFCTQTLGVDKGYKNQSFYRKHFDTEETRVNQLFAQAK ACKVLVEKCTVSVKDIQAHLAQGHVAIVLVNSGVLHCDLCSSPVKYCCFTPSGHHCFCRT PDYQGHFIVLRGYNRATGCIFYNNPAYADPGMCSTSISNFEEARTSYGTDEDILFVYLDS |
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Target Type |
Successful
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Target Bioclass |
Transporter and channel
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Family |
Major facilitator superfamily, SLC46A family
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Subcellular location |
Cell membrane
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Function |
Proton-coupled folate symporter that mediates folate absorption using an H(+) gradient as a driving force. Involved in the intestinal absorption of folates at the brush-border membrane of the proximal jejunum, and the transport from blood to cerebrospinal fluid across the choroid plexus. Functions at acidic pH via alternate outward- and inward-open conformation states. Protonation of residues in the outward open state primes the protein for transport. Binding of folate promotes breaking of salt bridge network and subsequent closure of the extracellular gate, leading to the inward-open state and release of protons and folate. Also able to transport antifolate drugs, such as methotrexate and pemetrexed, which are established treatments for cancer and autoimmune diseases. Involved in FOLR1-mediated endocytosis by serving as a route of export of folates from acidified endosomes. Also acts as a lower-affinity, pH-independent heme carrier protein and constitutes the main importer of heme in the intestine. Imports heme in the retina and retinal pigment epithelium, in neurons of the hippocampus, in hepatocytes and in the renal epithelial cells. Hence, participates in the trafficking of heme and increases intracellular iron content.; [Isoform 2]: Inactive isoform which is not able to mediate proton-coupled folate transport.
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TTD ID | ||||||
Uniprot ID | ||||||
DrugMap ID | ||||||
Ensemble ID | ||||||
HGNC ID | ||||||
ChEMBL ID |
Probe(s) Labeling This Target
ABPP Probe
Probe name | Structure | Binding Site(Ratio) | Interaction ID | Ref | |
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DBIA Probe Info |
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C21(1.26) | LDD3313 | [1] | |
BTD Probe Info |
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C21(1.26) | LDD2136 | [2] | |
IPM Probe Info |
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N.A. | LDD0005 | [3] | |
TFBX Probe Info |
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N.A. | LDD0148 | [4] |
Competitor(s) Related to This Target
Competitor ID | Name | Cell line | Binding Site(Ratio) | Interaction ID | Ref |
---|---|---|---|---|---|
LDCM0214 | AC1 | HEK-293T | C21(1.04) | LDD1507 | [5] |
LDCM0215 | AC10 | HEK-293T | C21(1.06) | LDD1508 | [5] |
LDCM0226 | AC11 | HEK-293T | C21(0.92) | LDD1509 | [5] |
LDCM0237 | AC12 | HEK-293T | C21(0.95) | LDD1510 | [5] |
LDCM0276 | AC17 | HEK-293T | C21(1.04) | LDD1515 | [5] |
LDCM0277 | AC18 | HEK-293T | C21(0.96) | LDD1516 | [5] |
LDCM0278 | AC19 | HEK-293T | C21(1.04) | LDD1517 | [5] |
LDCM0279 | AC2 | HEK-293T | C21(0.89) | LDD1518 | [5] |
LDCM0280 | AC20 | HEK-293T | C21(0.96) | LDD1519 | [5] |
LDCM0285 | AC25 | HEK-293T | C21(1.04) | LDD1524 | [5] |
LDCM0286 | AC26 | HEK-293T | C21(0.96) | LDD1525 | [5] |
LDCM0287 | AC27 | HEK-293T | C21(1.01) | LDD1526 | [5] |
LDCM0288 | AC28 | HEK-293T | C21(1.08) | LDD1527 | [5] |
LDCM0290 | AC3 | HEK-293T | C21(0.96) | LDD1529 | [5] |
LDCM0294 | AC33 | HEK-293T | C21(1.07) | LDD1533 | [5] |
LDCM0295 | AC34 | HEK-293T | C21(0.97) | LDD1534 | [5] |
LDCM0296 | AC35 | HEK-293T | C21(1.07) | LDD1535 | [5] |
LDCM0297 | AC36 | HEK-293T | C21(1.03) | LDD1536 | [5] |
LDCM0301 | AC4 | HEK-293T | C21(1.06) | LDD1540 | [5] |
LDCM0303 | AC41 | HEK-293T | C21(1.04) | LDD1542 | [5] |
LDCM0304 | AC42 | HEK-293T | C21(0.96) | LDD1543 | [5] |
LDCM0305 | AC43 | HEK-293T | C21(1.02) | LDD1544 | [5] |
LDCM0306 | AC44 | HEK-293T | C21(0.98) | LDD1545 | [5] |
LDCM0311 | AC49 | HEK-293T | C21(1.02) | LDD1550 | [5] |
LDCM0313 | AC50 | HEK-293T | C21(0.94) | LDD1552 | [5] |
LDCM0314 | AC51 | HEK-293T | C21(0.90) | LDD1553 | [5] |
LDCM0315 | AC52 | HEK-293T | C21(0.99) | LDD1554 | [5] |
LDCM0320 | AC57 | HEK-293T | C21(1.06) | LDD1559 | [5] |
LDCM0321 | AC58 | HEK-293T | C21(0.99) | LDD1560 | [5] |
LDCM0322 | AC59 | HEK-293T | C21(0.98) | LDD1561 | [5] |
LDCM0324 | AC60 | HEK-293T | C21(1.12) | LDD1563 | [5] |
LDCM0356 | AKOS034007680 | HEK-293T | C21(1.07) | LDD1570 | [5] |
LDCM0369 | CL100 | HEK-293T | C21(0.97) | LDD1573 | [5] |
LDCM0371 | CL102 | HEK-293T | C21(1.05) | LDD1575 | [5] |
LDCM0372 | CL103 | HEK-293T | C21(0.93) | LDD1576 | [5] |
LDCM0373 | CL104 | HEK-293T | C21(0.97) | LDD1577 | [5] |
LDCM0375 | CL106 | HEK-293T | C21(1.01) | LDD1579 | [5] |
LDCM0376 | CL107 | HEK-293T | C21(0.95) | LDD1580 | [5] |
LDCM0377 | CL108 | HEK-293T | C21(0.94) | LDD1581 | [5] |
LDCM0380 | CL110 | HEK-293T | C21(1.08) | LDD1584 | [5] |
LDCM0381 | CL111 | HEK-293T | C21(0.96) | LDD1585 | [5] |
LDCM0382 | CL112 | HEK-293T | C21(1.00) | LDD1586 | [5] |
LDCM0384 | CL114 | HEK-293T | C21(1.26) | LDD1588 | [5] |
LDCM0385 | CL115 | HEK-293T | C21(0.96) | LDD1589 | [5] |
LDCM0386 | CL116 | HEK-293T | C21(1.05) | LDD1590 | [5] |
LDCM0388 | CL118 | HEK-293T | C21(1.16) | LDD1592 | [5] |
LDCM0389 | CL119 | HEK-293T | C21(0.92) | LDD1593 | [5] |
LDCM0391 | CL120 | HEK-293T | C21(1.05) | LDD1595 | [5] |
LDCM0393 | CL122 | HEK-293T | C21(1.07) | LDD1597 | [5] |
LDCM0394 | CL123 | HEK-293T | C21(1.08) | LDD1598 | [5] |
LDCM0395 | CL124 | HEK-293T | C21(1.02) | LDD1599 | [5] |
LDCM0397 | CL126 | HEK-293T | C21(1.09) | LDD1601 | [5] |
LDCM0398 | CL127 | HEK-293T | C21(0.94) | LDD1602 | [5] |
LDCM0399 | CL128 | HEK-293T | C21(1.01) | LDD1603 | [5] |
LDCM0401 | CL14 | HEK-293T | C21(0.99) | LDD1605 | [5] |
LDCM0402 | CL15 | HEK-293T | C21(1.05) | LDD1606 | [5] |
LDCM0403 | CL16 | HEK-293T | C21(1.07) | LDD1607 | [5] |
LDCM0404 | CL17 | HEK-293T | C21(1.12) | LDD1608 | [5] |
LDCM0405 | CL18 | HEK-293T | C21(1.02) | LDD1609 | [5] |
LDCM0406 | CL19 | HEK-293T | C21(0.90) | LDD1610 | [5] |
LDCM0407 | CL2 | HEK-293T | C21(1.01) | LDD1611 | [5] |
LDCM0408 | CL20 | HEK-293T | C21(0.96) | LDD1612 | [5] |
LDCM0414 | CL26 | HEK-293T | C21(1.06) | LDD1618 | [5] |
LDCM0415 | CL27 | HEK-293T | C21(0.94) | LDD1619 | [5] |
LDCM0416 | CL28 | HEK-293T | C21(1.00) | LDD1620 | [5] |
LDCM0417 | CL29 | HEK-293T | C21(0.95) | LDD1621 | [5] |
LDCM0418 | CL3 | HEK-293T | C21(0.90) | LDD1622 | [5] |
LDCM0419 | CL30 | HEK-293T | C21(1.00) | LDD1623 | [5] |
LDCM0420 | CL31 | HEK-293T | C21(1.05) | LDD1624 | [5] |
LDCM0421 | CL32 | HEK-293T | C21(1.01) | LDD1625 | [5] |
LDCM0428 | CL39 | HEK-293T | C21(0.96) | LDD1632 | [5] |
LDCM0429 | CL4 | HEK-293T | C21(0.99) | LDD1633 | [5] |
LDCM0430 | CL40 | HEK-293T | C21(0.98) | LDD1634 | [5] |
LDCM0431 | CL41 | HEK-293T | C21(0.97) | LDD1635 | [5] |
LDCM0432 | CL42 | HEK-293T | C21(0.91) | LDD1636 | [5] |
LDCM0433 | CL43 | HEK-293T | C21(0.98) | LDD1637 | [5] |
LDCM0434 | CL44 | HEK-293T | C21(1.10) | LDD1638 | [5] |
LDCM0440 | CL5 | HEK-293T | C21(1.05) | LDD1644 | [5] |
LDCM0441 | CL50 | HEK-293T | C21(1.08) | LDD1645 | [5] |
LDCM0443 | CL52 | HEK-293T | C21(1.00) | LDD1646 | [5] |
LDCM0444 | CL53 | HEK-293T | C21(1.08) | LDD1647 | [5] |
LDCM0445 | CL54 | HEK-293T | C21(1.14) | LDD1648 | [5] |
LDCM0446 | CL55 | HEK-293T | C21(0.95) | LDD1649 | [5] |
LDCM0447 | CL56 | HEK-293T | C21(1.10) | LDD1650 | [5] |
LDCM0451 | CL6 | HEK-293T | C21(1.08) | LDD1654 | [5] |
LDCM0454 | CL62 | HEK-293T | C21(1.15) | LDD1657 | [5] |
LDCM0455 | CL63 | HEK-293T | C21(0.89) | LDD1658 | [5] |
LDCM0456 | CL64 | HEK-293T | C21(0.96) | LDD1659 | [5] |
LDCM0457 | CL65 | HEK-293T | C21(1.02) | LDD1660 | [5] |
LDCM0458 | CL66 | HEK-293T | C21(0.98) | LDD1661 | [5] |
LDCM0459 | CL67 | HEK-293T | C21(0.91) | LDD1662 | [5] |
LDCM0460 | CL68 | HEK-293T | C21(1.01) | LDD1663 | [5] |
LDCM0462 | CL7 | HEK-293T | C21(0.90) | LDD1665 | [5] |
LDCM0467 | CL74 | HEK-293T | C21(1.10) | LDD1670 | [5] |
LDCM0469 | CL76 | HEK-293T | C21(0.91) | LDD1672 | [5] |
LDCM0470 | CL77 | HEK-293T | C21(1.07) | LDD1673 | [5] |
LDCM0471 | CL78 | HEK-293T | C21(0.97) | LDD1674 | [5] |
LDCM0472 | CL79 | HEK-293T | C21(0.91) | LDD1675 | [5] |
LDCM0473 | CL8 | HEK-293T | C21(1.73) | LDD1676 | [5] |
LDCM0474 | CL80 | HEK-293T | C21(1.09) | LDD1677 | [5] |
LDCM0480 | CL86 | HEK-293T | C21(1.20) | LDD1683 | [5] |
LDCM0481 | CL87 | HEK-293T | C21(0.99) | LDD1684 | [5] |
LDCM0482 | CL88 | HEK-293T | C21(1.06) | LDD1685 | [5] |
LDCM0483 | CL89 | HEK-293T | C21(1.01) | LDD1686 | [5] |
LDCM0485 | CL90 | HEK-293T | C21(1.15) | LDD1688 | [5] |
LDCM0486 | CL91 | HEK-293T | C21(1.04) | LDD1689 | [5] |
LDCM0487 | CL92 | HEK-293T | C21(1.08) | LDD1690 | [5] |
LDCM0493 | CL98 | HEK-293T | C21(1.02) | LDD1696 | [5] |
LDCM0494 | CL99 | HEK-293T | C21(1.01) | LDD1697 | [5] |
LDCM0495 | E2913 | HEK-293T | C21(0.82) | LDD1698 | [5] |
LDCM0213 | Electrophilic fragment 2 | MDA-MB-231 | C21(2.29) | LDD1702 | [2] |
LDCM0468 | Fragment33 | HEK-293T | C21(0.93) | LDD1671 | [5] |
LDCM0427 | Fragment51 | HEK-293T | C21(1.01) | LDD1631 | [5] |
LDCM0022 | KB02 | A2780 | C21(1.68) | LDD2254 | [1] |
LDCM0023 | KB03 | MDA-MB-231 | C21(4.26) | LDD1701 | [2] |
LDCM0024 | KB05 | Hs 936.T | C21(1.26) | LDD3313 | [1] |
LDCM0543 | Nucleophilic fragment 38 | MDA-MB-231 | C21(1.26) | LDD2136 | [2] |
LDCM0544 | Nucleophilic fragment 39 | MDA-MB-231 | C21(0.79) | LDD2137 | [2] |
The Interaction Atlas With This Target
The Drug(s) Related To This Target
Approved
Investigative
Drug Name | Drug Type | External ID | |||
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Premetrexed | Small molecular drug | D0UZ9U | |||
[3h]Folinic Acid | Small molecular drug | D0R4PS | |||
[3h]N5-methylfolate | Small molecular drug | D0C2VP |
References