Cabazitaxel inhibits prostate cancer cell growth by inhibition of androgen receptor and heat shock protein expression

The Androgen Receptor in Prostate Cancer: Effect of Structure, Ligands and Spliced Variants on Therapy

“…To ensure full blockade of T production, adrenal androgen inhibitors, including corticosteroids, ketoconazole, and aminoglutethimide, may also be used [ 61 ], though the toxicities of ketoconazole often outweigh its benefits [ 17 ]. Regardless of the form of ADT, however, within 2–3 years, most PCa patients develop resistance to ADT monotherapy and progress to CRPC [ 9 , 15 , 16 , 17 , 18 , 19 ]. In addition to the above, competitive inhibitors of ligand binding to the AR-LBD, the first generation antiandrogens such as bicalutamide, nilutamide, and flutamide, were also developed; these anti-androgens allow the AR to enter the nucleus and bind to target DNA but recruits co-repressors [ 66 ] and repels co-activators [ 66 , 67 ] to halt AR transcriptional activity.…”

“…For patients with BCR or with metastatic PCa, androgen deprivation therapy (ADT), a treatment aiming to reduce cancer growth and alleviate pain by reducing circulating androgens, becomes the standard of care treatment [ 9 , 12 , 13 , 14 ]. Within 2–3 years, patients often develop resistance to ADT monotherapy, resulting in castration-resistant PCa (CRPC) [ 9 , 15 , 16 , 17 , 18 , 19 ].…”

Are IgG antibodies to heat shock proteins HSP27 and HSP60 useful markers in endometrial cancer and cervical cancer?

“…On the other hand, a marked and rapid overexpression of most HSPs in response to cellular damage is found, with cancer cells having been found to over-stimulate the synthesis of heat shock proteins [15]. This may be of fundamental importance in the pathogenesis and progression of cancerthe significant role of heat shock proteins as a therapeutic target in cancer has been demonstrated [16,17] but, on the other hand, they are also associated with drug resistance in cancer [18].…”

Desenvolvimento de nanopartículas poliméricas contendo cabazitaxel para a terapia do câncer de próstata

“…18 Além disso, muitos tumores se tornam resistentes à terapia hormonal depois de até 3 anos, sendo necessário modificar o tratamento. [19][20][21] O câncer de próstata resistente à castração (CPRC) pode variar entre assintomático e/ou sem metástase e os casos mais graves, em que há o surgimento de metástases. O principal local de metástase é o osso, representando cerca de 90% dos casos.…”

“…[31][32][33] Além disso, o CBZ age no bloqueio da translocação do receptor de andrógeno do citoplasma para o núcleo, impedindo-o de exercer sua função como fator de transcrição, o que é fundamental para o crescimento e o desenvolvimento das células cancerosas. 19,34 O CBZ possui fórmula estrutural semelhante ao seu precursor docetaxel, diferenciando-se apenas por 2 éteres metílicos ao invés de 2 grupos álcoois no anel nuclear da molécula, o que lhe confere maior lipossolubilidade (Figura 1). 35 A fórmula molecular do CBZ é C 45 H 57 NO 14, possui ponto de fusão de 157ºC e massa molar de 835,93 g/mol.…”