Details of the Target

General Information of Target

Target ID LDTP12930
Target Name Programmed cell death 1 ligand 1 (CD274)
Gene Name CD274
Gene ID 29126
Synonyms
B7H1; PDCD1L1; PDCD1LG1; PDL1; Programmed cell death 1 ligand 1; PD-L1; PDCD1 ligand 1; Programmed death ligand 1; hPD-L1; B7 homolog 1; B7-H1; CD antigen CD274
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MYRALYAFRSAEPNALAFAAGETFLVLERSSAHWWLAARARSGETGYVPPAYLRRLQGLE
QDVLQAIDRAIEAVHNTAMRDGGKYSLEQRGVLQKLIHHRKETLSRRGPSASSVAVMTSS
TSDHHLDAAAARQPNGVCRAGFERQHSLPSSEHLGADGGLYQIPLPSSQIPPQPRRAAPT
TPPPPVKRRDREALMASGSGGHNTMPSGGNSVSSGSSVSSTSLDTLYTSSSPSEPGSSCS
PTPPPVPRRGTHTTVSQVQPPPSKASAPEPPAEEEVATGTTSASDDLEALGTLSLGTTEE
KAAAEAAVPRTIGAELMELVRRNTGLSHELCRVAIGIIVGHIQASVPASSPVMEQVLLSL
VEGKDLSMALPSGQVCHDQQRLEVIFADLARRKDDAQQRSWALYEDEGVIRCYLEELLHI
LTDADPEVCKKMCKRNEFESVLALVAYYQMEHRASLRLLLLKCFGAMCSLDAAIISTLVS
SVLPVELARDMQTDTQDHQKLCYSALILAMVFSMGEAVPYAHYEHLGTPFAQFLLNIVED
GLPLDTTEQLPDLCVNLLLALNLHLPAADQNVIMAALSKHANVKIFSEKLLLLLNRGDDP
VRIFKHEPQPPHSVLKFLQDVFGSPATAAIFYHTDMMALIDITVRHIADLSPGDKLRMEY
LSLMHAIVRTTPYLQHRHRLPDLQAILRRILNEEETSPQCQMDRMIVREMCKEFLVLGEA
PS
Target Type
Successful
Target Bioclass
Immunoglobulin
Family
Immunoglobulin superfamily, BTN/MOG family
Subcellular location
Endomembrane system; Cell membrane
Function
Plays a critical role in induction and maintenance of immune tolerance to self. As a ligand for the inhibitory receptor PDCD1/PD-1, modulates the activation threshold of T-cells and limits T-cell effector response. Through a yet unknown activating receptor, may costimulate T-cell subsets that predominantly produce interleukin-10 (IL10). Can also act as a transcription coactivator: in response to hypoxia, translocates into the nucleus via its interaction with phosphorylated STAT3 and promotes transcription of GSDMC, leading to pyroptosis.; The PDCD1-mediated inhibitory pathway is exploited by tumors to attenuate anti-tumor immunity and escape destruction by the immune system, thereby facilitating tumor survival. The interaction with PDCD1/PD-1 inhibits cytotoxic T lymphocytes (CTLs) effector function. The blockage of the PDCD1-mediated pathway results in the reversal of the exhausted T-cell phenotype and the normalization of the anti-tumor response, providing a rationale for cancer immunotherapy.
TTD ID
T99948
Uniprot ID
Q9NZQ7
DrugMap ID
TTFAOU7
Ensemble ID
ENST00000381573.8
HGNC ID
HGNC:17635
ChEMBL ID
CHEMBL3580522

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HEC1 SNV: p.E187V .
MFE319 SNV: p.G264W .
TOV21G SNV: p.A97V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STPyne
 Probe Info  		K270(10.00)  LDD0277  [1]
DBIA
 Probe Info  		C272(1.18)  LDD3335  [2]
BTD
 Probe Info  		C272(0.98)  LDD1700  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0548  1-(4-(Benzo[d][1,3]dioxol-5-ylmethyl)piperazin-1-yl)-2-nitroethan-1-one MDA-MB-231 C272(0.99)  LDD2142  [3]
 LDCM0519  1-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-2-nitroethan-1-one MDA-MB-231 C272(1.10)  LDD2112  [3]
 LDCM0502  1-(Cyanoacetyl)piperidine MDA-MB-231 C272(0.66)  LDD2095  [3]
 LDCM0537  2-Cyano-N,N-dimethylacetamide MDA-MB-231 C272(0.85)  LDD2130  [3]
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C272(0.85)  LDD2117  [3]
 LDCM0558  2-Cyano-N-phenylacetamide MDA-MB-231 C272(1.13)  LDD2152  [3]
 LDCM0539  3-(4-Isopropylpiperazin-1-yl)-3-oxopropanenitrile MDA-MB-231 C272(0.61)  LDD2132  [3]
 LDCM0538  4-(Cyanoacetyl)morpholine MDA-MB-231 C272(0.74)  LDD2131  [3]
 LDCM0520  AKOS000195272 MDA-MB-231 C272(0.59)  LDD2113  [3]
 LDCM0498  BS-3668 MDA-MB-231 C272(0.50)  LDD2091  [3]
 LDCM0022  KB02 CMK C272(2.25)  LDD2302  [2]
 LDCM0023  KB03 CMK C272(2.90)  LDD2719  [2]
 LDCM0024  KB05 MONO-MAC-6 C272(1.18)  LDD3335  [2]
 LDCM0509  N-(4-bromo-3,5-dimethylphenyl)-2-nitroacetamide MDA-MB-231 C272(0.87)  LDD2102  [3]
 LDCM0528  N-(4-bromophenyl)-2-cyano-N-phenylacetamide MDA-MB-231 C272(0.36)  LDD2121  [3]
 LDCM0499  Nucleophilic fragment 12b MDA-MB-231 C272(0.77)  LDD2092  [3]
 LDCM0500  Nucleophilic fragment 13a MDA-MB-231 C272(0.94)  LDD2093  [3]
 LDCM0501  Nucleophilic fragment 13b MDA-MB-231 C272(0.91)  LDD2094  [3]
 LDCM0503  Nucleophilic fragment 14b MDA-MB-231 C272(0.82)  LDD2096  [3]
 LDCM0504  Nucleophilic fragment 15a MDA-MB-231 C272(1.06)  LDD2097  [3]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C272(0.99)  LDD2098  [3]
 LDCM0506  Nucleophilic fragment 16a MDA-MB-231 C272(0.66)  LDD2099  [3]
 LDCM0507  Nucleophilic fragment 16b MDA-MB-231 C272(1.35)  LDD2100  [3]
 LDCM0508  Nucleophilic fragment 17a MDA-MB-231 C272(0.74)  LDD2101  [3]
 LDCM0511  Nucleophilic fragment 18b MDA-MB-231 C272(1.12)  LDD2104  [3]
 LDCM0512  Nucleophilic fragment 19a MDA-MB-231 C272(1.02)  LDD2105  [3]
 LDCM0513  Nucleophilic fragment 19b MDA-MB-231 C272(0.93)  LDD2106  [3]
 LDCM0514  Nucleophilic fragment 20a MDA-MB-231 C272(0.76)  LDD2107  [3]
 LDCM0515  Nucleophilic fragment 20b MDA-MB-231 C272(0.98)  LDD2108  [3]
 LDCM0518  Nucleophilic fragment 22a MDA-MB-231 C272(0.66)  LDD2111  [3]
 LDCM0521  Nucleophilic fragment 23b MDA-MB-231 C272(0.72)  LDD2114  [3]
 LDCM0523  Nucleophilic fragment 24b MDA-MB-231 C272(0.73)  LDD2116  [3]
 LDCM0525  Nucleophilic fragment 25b MDA-MB-231 C272(1.03)  LDD2118  [3]
 LDCM0529  Nucleophilic fragment 27b MDA-MB-231 C272(1.05)  LDD2122  [3]
 LDCM0530  Nucleophilic fragment 28a MDA-MB-231 C272(1.00)  LDD2123  [3]
 LDCM0531  Nucleophilic fragment 28b MDA-MB-231 C272(0.98)  LDD2124  [3]
 LDCM0532  Nucleophilic fragment 29a MDA-MB-231 C272(0.67)  LDD2125  [3]
 LDCM0533  Nucleophilic fragment 29b MDA-MB-231 C272(0.81)  LDD2126  [3]
 LDCM0534  Nucleophilic fragment 30a MDA-MB-231 C272(1.02)  LDD2127  [3]
 LDCM0536  Nucleophilic fragment 31 MDA-MB-231 C272(0.66)  LDD2129  [3]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C272(0.66)  LDD2135  [3]
 LDCM0543  Nucleophilic fragment 38 MDA-MB-231 C272(1.61)  LDD2136  [3]
 LDCM0544  Nucleophilic fragment 39 MDA-MB-231 C272(0.85)  LDD2137  [3]
 LDCM0211  Nucleophilic fragment 3b MDA-MB-231 C272(0.98)  LDD1700  [3]
 LDCM0546  Nucleophilic fragment 40 MDA-MB-231 C272(0.61)  LDD2140  [3]
 LDCM0547  Nucleophilic fragment 41 MDA-MB-231 C272(0.65)  LDD2141  [3]
 LDCM0549  Nucleophilic fragment 43 MDA-MB-231 C272(0.99)  LDD2143  [3]
 LDCM0550  Nucleophilic fragment 5a MDA-MB-231 C272(3.45)  LDD2144  [3]
 LDCM0551  Nucleophilic fragment 5b MDA-MB-231 C272(8.54)  LDD2145  [3]
 LDCM0552  Nucleophilic fragment 6a MDA-MB-231 C272(0.62)  LDD2146  [3]
 LDCM0555  Nucleophilic fragment 7b MDA-MB-231 C272(0.97)  LDD2149  [3]
 LDCM0556  Nucleophilic fragment 8a MDA-MB-231 C272(0.49)  LDD2150  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Immunoglobulin
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Programmed cell death protein 1 (PDCD1) . Q15116
T-lymphocyte activation antigen CD80 (CD80) . P33681
Cytokine and receptor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
CKLF-like MARVEL transmembrane domain-containing protein 4 (CMTM4) Chemokine-like factor family Q8IZR5
CKLF-like MARVEL transmembrane domain-containing protein 6 (CMTM6) Chemokine-like factor family Q9NX76

The Drug(s) Related To This Target

Approved
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Atezolizumab Monoclonal antibody D0YM2K
Avelumab Monoclonal antibody D0K7SX
Bavencio Monoclonal antibody D0W8HN
Durvalumab Monoclonal antibody D0LS9E
Nivolumab Monoclonal antibody DB09035
Pembrolizumab Monoclonal antibody DB09037
Rg-7446 Monoclonal antibody D0OZ4J
Sildenafil Small molecular drug DB00203
Valproic Acid Small molecular drug DB00313
Phase 3
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Cs1001 Antibody D3MP1S
Kn046 Antibody DLOQ25
Medi4736 Monoclonal antibody D04RRZ
Mpdl-3280a Monoclonal antibody D0Y5IH
Phase 2
Click To Hide/Show 9 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Bgb-a333 Antibody DC5VW9
Cx-072 Antibody D0Z2BO
Kn035 Antibody D0GF2R
M7824 Antibody D05FPZ
Nm21-1480 Antibody DUVH60
Pidilizumab Monoclonal antibody D09MRL
Bintrafusp Alfa Recombinant protein D5J3BL
Gs-4224 Small molecular drug DS6VD0
Incb86550 Small molecular drug DKM79E
Phase 1
Click To Hide/Show 19 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Anti-pd-l1 Antibody D0KP9A
Cosibelimab Antibody D17URP
Fs118 Antibody D0XO9F
Gen1046 Antibody D3HBJ1
Ibi318 Antibody DX30BA
Inbrx-105 Antibody DA1X5W
Ly3415244 Antibody DC8HR6
Mcla-145 Antibody D2QY0Z
Anti-pd-l1 Csr T Cells CAR T Cell Therapy D0W7UD
Pd-l1 T-hank CAR T Cell Therapy DH42RF
C-met/Pd-l1 Car-t Cell CAR T Cell Therapy (Dual specific) D03GTO
Faz053 Monoclonal antibody D0LU1O
Ly3300054 Monoclonal antibody D08HSS
Msb2311 Monoclonal antibody D0A8AU
Alpn-202 Protein D82UVG
Kd033 Recombinant protein DJVR06
Tak-252 Recombinant protein D9SL1N
Bms-986189 Small molecular drug D0X1GN
Ca-170 Small molecular drug D09PPU
Investigative
Click To Hide/Show 12 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Camrelizumab Monoclonal antibody DB14776
Aunp-12 Peptide DB15771
Ca-327 Small molecular drug D04ILU
Pmid30247903-compound-general Structure10 Small molecular drug D0XL3N
Pmid30247903-compound-general Structure12 Small molecular drug D09BYN
Pmid30247903-compound-general Structure5 Small molecular drug D07BOF
Pmid30247903-compound-general Structure6 Small molecular drug D0TN4F
Pmid30247903-compound-general Structure7 Small molecular drug D01TGF
Pmid30247903-compound-general Structure8 Small molecular drug D04QGF
Pmid30247903-compound-general Structure9 Small molecular drug D0GG6N
Anti-ox40 Antibody Bms 986178 . DB15773
Envafolimab . DB15769
Patented
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid30107136-compound-example1 Small molecular drug D0WQ9X
Pmid30107136-compound-example2 Small molecular drug D0OK1S

References

1 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
2 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
3 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761