Discovery of a Novel, Potent, and Orally Active Nonpeptide Antagonist of the Human Luteinizing Hormone-Releasing Hormone (LHRH) Receptor

1998 ◽  
Vol 41 (22) ◽  
pp. 4190-4195 ◽  
Author(s):  
Nobuo Cho ◽  
Masataka Harada ◽  
Toshihiro Imaeda ◽  
Takashi Imada ◽  
Hirokazu Matsumoto ◽  
...  
Oncotarget ◽  
2013 ◽  
Vol 4 (10) ◽  
pp. 1721-1728 ◽  
Author(s):  
Andrea Treszl ◽  
Zita Steiber ◽  
Andrew V. Schally ◽  
Norman L Block ◽  
Balazs Dezso ◽  
...  

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1253
Author(s):  
Zsuzsanna Szabó ◽  
Balázs Dezső ◽  
Klára Fodor ◽  
Krisztián Szegedi ◽  
Tibor Flaskó ◽  
...  

Bladder cancer (BC) is the tenth most frequently detected cancer in both sexes. Type-I luteinizing hormone-releasing hormone (LHRH) receptor (LHRH-R-I) is expressed not only in the pituitary, but also in several types of cancer disease. There are few data about LHRH-R-I expression in human BC. This study aimed to investigate the expression of LHRH and LHRH-R-I in the transitional cell carcinoma (TCC) type of human BC. RNA was extracted from 24 human bladder tumor specimens and three BC cell lines. RT-PCR was performed to detect mRNA for LHRH and LHRH-R-I. The protein of LHRH-R-I was further studied by immunohistochemistry (IHC), ligand competition assay, and Western Blot. PCR products of LHRH were found in 19 of 24 (79%) specimens and mRNA of LHRH-R-I was detected in 20 of 24 specimens (83%). Positive immunostaining for LHRH-R-I with different expression intensity was found in all samples examined, showing negative correlation with TCC grade. Radioligand binding studies also showed the presence of specific LHRH-R-I and high affinity binding of LHRH analogs. The high incidence of LHRH-R in BC suggests that it could serve as a molecular target for therapy of human BC with cytotoxic LHRH analogs or modern powerful antagonistic analogs of LHRH.


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