Ph-20

Abstract

We report the first data on PH-20 expression in laryngeal cancer tissue. PH-20 expression is significantly elevated in primary laryngeal cancer tissue and seems to be even higher in metastatic lesions compared with normal laryngeal tissue. PH-20 may be a useful tumor marker and prognostic tool for laryngeal cancer.

Stromal and Epithelial Expression of Tumor Markers Hyaluronic Acid and HYAL1 Hyaluronidase in Prostate Cancer

“…The CaP HAase is inactive at pH Ͼ 5.0. This is noteworthy, since expression of PH20 transcripts has been detected in CaP tissues by RT-PCR analysis (63). However, except for LNCaP cells, we did not detect PH20 mRNA expression in other CaP cells.…”

“…Together with prostate cancer, the expression of PH20 mRNA has been demonstrated in melanoma, glioblastoma, glioma, and colonic carcinoma cell lines, as well as in invasive breast carcinomas (34,40,63). However, the pH optimum (3.8 to 4.0) of the HAase activity present in the extracts of breast primary tumors, and regional metastases is similar to the pH optimum of HAase present in human serum, and CaP SF-CM, observed in this study and it is different from that of the known pH20 isoforms (35,61,62).…”

Indole carboxamides inhibit bovine testes hyaluronidase at pH 7.0 and indole acetamides activate the enzyme at pH 3.5 by different mechanisms

“…As substrate solution, 2 mg/mL hyaluronic acid was dissolved in water. All compounds (16)(17)(18)(19)(20)(21)(22)(23)(24)(25)(26)(27)(28)(29)(30) were prepared with DMSO to give stock solutions of 10 mM.…”

“…All compounds containing an acetamide chain were less active than compounds with a carboxamide chain. Among the carboxamide series N-methyl substituted compounds (16)(17)(18) showed very low activity unless the pyridine was additionally substituted with two methyl groups in meta positions (17) which made this part of the molecule more lipophilic. The addition of Br in position R 3 seemed to have no effect as compounds 16 and 18 showed nearly the same amount of inhibition.…”

“…An additional charge would then enhance the activating effect on HA degradation. Besides the acetamide backbone, a substitution with bromine at R 3 (17,18) seemed to increase activating effect, as compound 16 showed no activity in comparison to 17 and 18, which could be the result of a more basic indole. Additional methyl groups at the pyridine, identified as important for hyaluronidase inhibitory activity, had no effect.…”