Details of the Target

General Information of Target

Target ID LDTP05956
Target Name Protein patched homolog 1 (PTCH1)
Gene Name PTCH1
Gene ID 5727
Synonyms
PTCH; Protein patched homolog 1; PTC; PTC1
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MASAGNAAEPQDRGGGGSGCIGAPGRPAGGGRRRRTGGLRRAAAPDRDYLHRPSYCDAAF
ALEQISKGKATGRKAPLWLRAKFQRLLFKLGCYIQKNCGKFLVVGLLIFGAFAVGLKAAN
LETNVEELWVEVGGRVSRELNYTRQKIGEEAMFNPQLMIQTPKEEGANVLTTEALLQHLD
SALQASRVHVYMYNRQWKLEHLCYKSGELITETGYMDQIIEYLYPCLIITPLDCFWEGAK
LQSGTAYLLGKPPLRWTNFDPLEFLEELKKINYQVDSWEEMLNKAEVGHGYMDRPCLNPA
DPDCPATAPNKNSTKPLDMALVLNGGCHGLSRKYMHWQEELIVGGTVKNSTGKLVSAHAL
QTMFQLMTPKQMYEHFKGYEYVSHINWNEDKAAAILEAWQRTYVEVVHQSVAQNSTQKVL
SFTTTTLDDILKSFSDVSVIRVASGYLLMLAYACLTMLRWDCSKSQGAVGLAGVLLVALS
VAAGLGLCSLIGISFNAATTQVLPFLALGVGVDDVFLLAHAFSETGQNKRIPFEDRTGEC
LKRTGASVALTSISNVTAFFMAALIPIPALRAFSLQAAVVVVFNFAMVLLIFPAILSMDL
YRREDRRLDIFCCFTSPCVSRVIQVEPQAYTDTHDNTRYSPPPPYSSHSFAHETQITMQS
TVQLRTEYDPHTHVYYTTAEPRSEISVQPVTVTQDTLSCQSPESTSSTRDLLSQFSDSSL
HCLEPPCTKWTLSSFAEKHYAPFLLKPKAKVVVIFLFLGLLGVSLYGTTRVRDGLDLTDI
VPRETREYDFIAAQFKYFSFYNMYIVTQKADYPNIQHLLYDLHRSFSNVKYVMLEENKQL
PKMWLHYFRDWLQGLQDAFDSDWETGKIMPNNYKNGSDDGVLAYKLLVQTGSRDKPIDIS
QLTKQRLVDADGIINPSAFYIYLTAWVSNDPVAYAASQANIRPHRPEWVHDKADYMPETR
LRIPAAEPIEYAQFPFYLNGLRDTSDFVEAIEKVRTICSNYTSLGLSSYPNGYPFLFWEQ
YIGLRHWLLLFISVVLACTFLVCAVFLLNPWTAGIIVMVLALMTVELFGMMGLIGIKLSA
VPVVILIASVGIGVEFTVHVALAFLTAIGDKNRRAVLALEHMFAPVLDGAVSTLLGVLML
AGSEFDFIVRYFFAVLAILTILGVLNGLVLLPVLLSFFGPYPEVSPANGLNRLPTPSPEP
PPSVVRFAMPPGHTHSGSDSSDSEYSSQTTVSGLSEELRHYEAQQGAGGPAHQVIVEATE
NPVFAHSTVVHPESRHHPPSNPRQQPHLDSGSLPPGRQGQQPRRDPPREGLWPPPYRPRR
DAFEISTEGHSGPSNRARWGPRGARSHNPRNPASTAMGSSVPGYCQPITTVTASASVTVA
VHPPPVPGPGRNPRGGLCPGYPETDHGLFEDPHVPFHVRCERRDSKVEVIELQDVECEER
PRGSSSN
Target Bioclass
Transporter and channel
Family
Patched family
Subcellular location
Cell membrane
Function
Acts as a receptor for sonic hedgehog (SHH), indian hedgehog (IHH) and desert hedgehog (DHH). Associates with the smoothened protein (SMO) to transduce the hedgehog's proteins signal. Seems to have a tumor suppressor function, as inactivation of this protein is probably a necessary, if not sufficient step for tumorigenesis.
Uniprot ID
Q13635
Ensemble ID
ENST00000331920.11
HGNC ID
HGNC:9585
ChEMBL ID
CHEMBL5169150

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
22RV1 SNV: p.A966T .
A172 SNV: p.G492R .
CAL51 Deletion: p.S1203AfsTer52 .
CCK81 SNV: p.Q1284R .
COLO678 SNV: p.Y1013Ter .
G415 SNV: p.Q700Ter .
HCC827 SNV: p.T314N .
HUH28 SNV: p.L732V .
Ishikawa (Heraklio) 02 ER Deletion: p.R1308EfsTer64 .
KMCH1 SNV: p.V1090L .
MELHO SNV: p.Y1013Ter .
MEWO SNV: p.P725L .
NCIH1155 SNV: p.Y1013Ter; p.I1022V; p.S1232L .
NCIH1993 SNV: p.L723F .
NCIH446 SNV: p.G244W .
NUGC3 Insertion: p.R1308QfsTer17 .
SKMEL2 Substitution: p.G91N .
SNGM Deletion: p.S1203AfsTer52 .
SNU245 SNV: p.G38R .
SW1116 SNV: p.Y1013Ter .
TE4 SNV: p.T1355P .
VCAP SNV: p.G37V .

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
CY4
 Probe Info  		C1437(0.00); D1434(0.00)  LDD0247  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Sonic hedgehog protein (SHH) Hedgehog family Q15465
3-hydroxyisobutyrate dehydrogenase, mitochondrial (HIBADH) HIBADH-related family P31937
Beta-adrenergic receptor kinase 1 (GRK2) AGC Ser/Thr protein kinase family P25098
Transporter and channel
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Stomatin (STOM) Band 7/mec-2 family P27105
G2/mitotic-specific cyclin-B1 (CCNB1) Cyclin family P14635
Huntingtin (HTT) Huntingtin family P42858
Immunoglobulin
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Sialic acid-binding Ig-like lectin 12 (SIGLEC12) SIGLEC (sialic acid binding Ig-like lectin) family Q96PQ1
B-cell antigen receptor complex-associated protein alpha chain (CD79A) . P11912
Cell adhesion molecule-related/down-regulated by oncogenes (CDON) . Q4KMG0
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein FAM209A (FAM209A) FAM209 family Q5JX71
Transcriptional coactivator YAP1 (YAP1) YAP1 family P46937
Amyloid protein-binding protein 2 (APPBP2) . Q92624

References

1 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.