有一些G蛋白偶合受體的功能，在癌症生物學是有相關聯的; 然而對於G蛋白偶合受體，在腫瘤上的表現，到目前還少有被探討。利用一系列的放射性標記配位體結合受體實驗方法，剖析了G蛋白偶合受體在腫瘤上的表達，而發現在HeLaS3腫瘤細胞上，有一種5-HT1A受體(5-羥色胺受體1A或血清張力素受體1A)辨識結合位置可被其作用劑的放射性標記配位體 [3H]8-OH-DPAT以高量、專一性、呈飽和態的結合。
在後續的競爭結合研究實驗中，多種血清張力素受體的作用藥物及運送體抑制劑都能呈現濃度-依賴關係，有效地拮抗[3H]8-OH-DPAT的結合，而8-OH-DPAT亦能拮抗放射性標記的生物胺運送體結合位。顯示5-HT1A受體的作用劑[3H]8-OH-DPAT不但可以以非常高專一性的結合到HeLaS3腫瘤活細胞上，而且具有多樣式的結合位置，其中有部分是與再吸收的運送體有關。
[125I]RTI-55和 [3H]paroxetine都能以飽和方式，結合到HeLaS3腫瘤細胞上; 一種或多種與5-HT受體相關的亞型受體被顯現出來。因此，表示HeLaS3腫瘤細胞內具有不同型式的5-HT受體系統的相關結合位置。

這些實驗觀察的結果，將可能有助於說明5-HT運送體與受體系統在腫瘤細胞的關聯性及其可能的致癌機轉及所牽涉的藥理作用。

Some G protein-coupled receptors (GPCRs) have functional links to cancer biology, yet the manifestation of GPCRs in tumor types is little studied to date. Using a battery of radioligand binding assays for profiling GPCR targets on HeLaS3 cells; high level of specific binding of a 5-HT1A receptor recognition binding agonist [3H]8-OH-DPAT was observed in these cells and characterized.
Follow-up studies in competition experiments, several serotonergic compounds and biogenic amine transporter inhibitors competed effectively against [3H]8-OH-DPAT binding with concentration–dependent relationship; 8-OH-DPAT displayed affinity for the labeled amine transporter sites, demonstrated that 5-HT1A receptor agonist [3H]8-OH-DPAT not only binds to intact HeLaS3 cells with high specific binding, but also has multiple binding sites, some of which relate to uptake.
[125I]RTI-55 and [3H]paroxetine bound in a saturable fashion to HeLaS3 cells. One or more of the related to 5-HT receptor subtypes was manifested in HeLaS3 cells. It is suggested that HeLaS3 cells contain distinct types of the related to 5-HT receptor system binding sites.
These observations could help elucidate the relevance of the 5-HT transporter and receptor systems as well as the possible tumorigenic mechanisms with attendant pharmacological implications in tumor cells.

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