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. 2021 Nov 23;13(23):5891. doi: 10.3390/cancers13235891

Table 1.

Overview of expression level of bitter taste receptors at gene and protein level in cancerous cell lines and tissues compared to non-cancerous cell lines and tissues as well as analysed agonists.

Cancer Type Cells or Tissues TAS2Rs/TAS2Rs
Regulation
Agonists Used in Functional Assay with Cell Lines Ref.
Breast cancer MCF-7 and MDA-MB-231 vs. MCF-10A TAS2R4 ↓, TAS2R4 ↓
No differences for TAS2R1, 10, 20 (49), 38 at gene and protein level
Quinine, dextromethorphan, PTC
(verified with MCF-7, MDA-MB-231, MCF-10A)
[24]
Breast cancer MDA-MB-231 vs. MCF-10A TAS2R14 ↑, TAS2R20
No differences for other TAS2Rs
[25]
Breast cancer Breast cancer tissues vs.
non-cancerous breast tissues
TAS2R4
TAS2R14
TAS2R14 ↑
Quinine, apigenin
(verified with MDA-MB-231 andMCF-10A)
[17]
Ovarian
cancer
OVCAR4, OVCAR8, ovarian cystadenocarcinoma tissue vs.
normal fallopian tube tissue; SKOV3 and IGROV1 vs. normal uterine tissue
TAS2R1 ↓ in OVCAR8,
TAS2R4 and 14 ↓ in OVCAR8 and SKOV3,
TAS2R10 and 14 ↓ in cancer tissue, TAS2R38 ↓ in all analysed cell lines and cancer tissue
Noscapine and
diphenhydramine for TAS2R14
(verified with SKOV3)
[18]
Endometrial cancer HEC-1a vs. normal uterine
tissue
TAS2R1, 14, 38 [18]
Prostate
cancer
PC3, LNCAP, DU145
vs. BPH1
TAS2R1, 4, 10, 14 ↓ in PC3, LNCAP, DU145,
TAS2R38 ↓ in LNCAP, DU145
Noscapine for TAS2R14
(verified with PC3, DU145)
[18]
Pancreatic cancer Primary human pancreatic
tumour tissues, T3M4, SU.86.86, PANC-1, MiaPaCa-2, Colo357,
Capan-1, BxPC-3, AsPC-1
TAS2R10
TAS2R10
Caffeine
(verified with BxPC-3 and PANC-1)
[20]
Pancreatic cancer Tumour infiltrating leukocytes; pancreatic tumour tissues vs. non-cancerous pancreatic tissues;
SU.86.86, T3M4, MiaPaCa-2, and RLT
TAS2R38 PTC, N-acetyl-dodecanoyl-homoserine lactone (AHL-12)
(verified with SU.86.86 and RLT)
[26]
Neuroblastoma SK-N-BE(2)C vs. SH-SY5Y TAS2R8
TAS2R10
Denatonium benzoate
(verified with SK-N-BE(2)C)
[22]
Acute
myeloid
leukemia
Primary acute myeloid
leukemia cells, in silico gene
expression profiling of samples from a database,
OCI-AML3, THP-1
Analyses of 18 to 24 TAS2Rs out of 25 TAS2Rs & identification of all TAS2Rs but not in all
approaches
Denatonium benzoate, quinine
(verified with primary acute myeloidleukemia cells,
OCI-AML3, THP-1)
[19]
Head and neck
squamous cell
carcinoma
Cancerous vs. non-cancerous
tissues; SCC4, SCC15, SCC47, SCC90, SCC152,OCTT2 and VU147T
Analysis of all TAS2Rs,
highest gene expression of TAS2R4, 14, 19, 20, 30, 43, 45 in cancer cell lines,
TAS2R4, 8, 10, 13, 14, 30, 42, 46 in
SCC4, SCC47, TAS2R4, 8, 10, 30, 39 in SCC47, SCC90, SCC152
Denatonium benzoate, quinine, thujone, diphenidol, flufenamic acid, parthenolide, N-3-oxo-dodecanoyl-L-homoserine lactone (3-oxo-C12HSL)
(verified in different settings with the used cancer cell lines)
[21]

↑: increased expression level; ↓: decreased expression level