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. 2021 Dec 4;15(1):101281. doi: 10.1016/j.tranon.2021.101281

Table 6.

Other receptor antagonists.

Subtype Drug Material basis Model Effect Mechanism References
5-HT antagonists SB269970 17 MCF-7
T47D
MDA-MB-231
Antiproliferation and anti-invasion Gα-activated cAMP and Gβγ-activated kinase signaling during invasion and Gβγ-activated PI3K/Akt signaling during proliferation [50]
BJ-1113 19 MCF-7
MDA-MB-231
The inhibitory effect of BJ-1113 against MDA-MB-231 tumor growth was greater than that of SB269970, a 5-HT7 receptor antagonist
mAChR antagonists Cevimeline 20 MCF-7
MDA-MB-231
Inhibited cell proliferation PLC activation [30]
4-DAMP 18 MCF-7
MDA-MB-231
Inhibited cell proliferation PLC activation [69,120,123]
Darifenacin 22 MCF-7
MDA-MB-231
Inhibited cell proliferation PLC activation [86,99,106]
nAChR antagonists Epigallocatechin-3-gallate (EGCG)
24 MCF-7 Inhibited cell proliferation Blocking α9-nAChR signaling pathway [144]
Garcinol 21 MCF-10A
MDA-MB-231
NOD.CB17-PRKDC (SCID)
Inhibited cell proliferation Downregulate the expression of α9-nAChR and cyclin D3 protein [27]
mGluR1-specific antagonists Riluzole 29 Inhibited cell proliferation in a dose-response manner in all EC types Inhibition of angiogenesis [41,136]
BAY36–7620 27 [25,137]
YM 298,198 28 MCF-7 Inhibited cell proliferation in all the cell types, except HUVEC Inhibition of angiogenesis [135]
H3R antagonists OUP-186 30 MDA-MB-231
MCF-7
Induced breast cancer cell death Activated caspase-3/7 [142]
Clobenpropit 31 MDA-MB-231
MCF-7
Cell death was only slightly induced Activated caspase-3/7
JNJ7777120 32 MDA-MB-231
MCF-7
Inhibited cell migration and invasion Reduced E-cadherin, cytoplasmic and nuclear β-catenin, and nuclear Slug and an increase in vimentin and α-smooth muscle actin expression [48]
Peptide neurotransmitter antagonists Scorpion venom 33 MDA-MB-231 Reduced motility and invasion in breast cancer cells Inhibited MMP activity; upregulation of p53 and downregulation of Bcl-xL and BID protein expression by modulating signaling proteins Erk1/2 and STAT3 and DNA damage in breast and colorectal cancer cell lines [4,5]
NTS agonist JMV449 34 MCF-7 Promoted apoptosis MAPK activation caused the expression of B-cell lymphoma-2 (BCL-2) [131]
NTS antagonist SR48692 35 [77]

In summary, we highlight in the Fig. 5 which are the potential targets for drug development.