A potent estrogen receptor and microtubule specific purine-benzothiazole-based fluorescent molecular probe induces apoptotic death of breast cancer cells.
Surajit BarmanSubhajit GhoshRajsekhar RoyVarsha GuptaSatyajit GhoshSurajit GhoshPublished in: Scientific reports (2022)
Breast cancer is the most common malignancy in women and is a heterogeneous disease at molecular level. Early detection and specificity are the key prerequisite for the treatment of this deadly cancer. To address these issues attention on the breast cancer specific receptor protein(s) is the most realistic option. Herein estrogen (E) and progesterone (Pg) receptors(R) were considered to design fluorescent molecular probes with possible therapeutic option. We adopted QSAR technique to design a library of benzothiazole-purine hybrid molecules. Molecular docking offers us three screened molecules as most potential. Among these molecules one abbreviated as "CPIB" showed blue fluorescence and detected ER positive cancer cells at 1 nM concentration. At elevated concentration, CPIB induces apoptotic deaths of same cancer cells through targeting intracellular microtubules without affecting normal cells or ER negative cells. CPIB is one of its kind with two-in-one potential of "Detection and Destroy" ability targeting ER positive breast cancer cells.
Keyphrases
- estrogen receptor
- breast cancer cells
- molecular docking
- living cells
- induced apoptosis
- single molecule
- cell death
- cell cycle arrest
- quantum dots
- anti inflammatory
- fluorescent probe
- type diabetes
- papillary thyroid
- oxidative stress
- polycystic ovary syndrome
- working memory
- risk assessment
- human health
- squamous cell carcinoma
- breast cancer risk
- pregnancy outcomes
- replacement therapy
- childhood cancer
- squamous cell
- smoking cessation
- protein protein