R-(-)-gossypol (AT 101)

P1, N=20, Not yet recruiting, The Second Hospital of Hebei Medical University; The Second Hospital of Hebei Medical University

To inhibit SRC activity, natural compounds (e.g., gossypol, bufalin, verrucarin A) and synthetic small molecules (e.g., SI-2, SI-12, MCB-613) have been developed, demonstrating preclinical efficacy across several human diseases...This review summarizes current knowledge of SRC biology in benign gynecologic disorders, outlines their mechanistic roles in disease progression, and highlights opportunities for clinical translation. Targeting SRCs may ultimately represent a novel, non-hormonal, fertility-preserving therapeutic strategy in women's health.

This study also describes differential responses of TNBC cell lines to polyphenol treatment, highlighting the importance of considering genetic variability in therapeutic strategies, as well as the importance of the interaction of polyphenols with the gut microbiome, which may establish the bioavailability and effectiveness of these compounds toward therapeutic outcomes. Further preclinical and clinical studies are warranted to fully elucidate the therapeutic potential of polyphenols and translate these findings into clinical practice, thereby improving outcomes for patients with TNBC worldwide.

= 28.44), surpassing celecoxib. Molecular docking and dynamics confirmed strong and stable binding to Mcl-1 and COX-2. In silico ADMET predictions indicated favorable drug-like and pharmacokinetic properties for the active compounds.

Administration of (±)-gossypol (40 mg/kg/day ip) for five consecutive days was well tolerated, with no observable signs of systemic toxicity, such as >5 % weight loss or behavioral abnormalities on mice. These findings revealed that (±)-gossypol, in addition to its tumor suppressive effect, can inhibit pro-angiogenic effects of Ehrlich's ascites carcinoma (EAC) cells and have a protective effect in breast cancer.

Western blot analysis revealed a dose-dependent reduction in PIK3R2, GRB2, and MAPK1 expression in Gossypol-treated groups compared to controls (p < 0.05). Gossypol may exhibit anti-cervical cancer effects by modulating the PI3K/AKT signaling pathway.

This malignancy represents a medical challenge due to the tumor´s localization in the brain, high rates of Temozolomide (TMZ) resistance, and extensive malignant cell parenchymal infiltration, among other factors...Interestingly, L-06 than L-37 exhibited an antimigratory effect on glioblastoma stem cells loaded onto aligned nanofibers at concentrations where no antiproliferative activity were observed, unlike G-15, a poorly water soluble GPER antagonist. Collectively, these findings establish a preclinical foundation for L-37 and L-06 as potential anti-glioblastoma agents and support their further investigation as therapeutic candidates.

This work demonstrated a new regulatory pathway of TNBC to promote the expression of mitochondrial genes by upregulating the nuclear gene LRPPRC, resulting in increased OXPHOS. We also suggested a promising therapeutic target LRPPRC for TNBC, and its inhibitor, the traditional gynecological medicine GAA, presented significant antitumor activity.

These nanoparticles effectively suppress proneural subtype tumor growth both in vitro and in vivo, surpassing their efficacy against the mesenchymal subtype. The results offer several novel insights into the role of LDH isoenzyme in subtype classification between mesenchymal and proneural GBM and provide a promising therapeutic approach for proneural subtype GBM.

Overall, gossypol enhanced ponatinib's anticancer effects in HCC cells. Notably, this new combination appears to be potential adjuvant targeted chemotherapy, a discovery that warrants more clinical investigation, in the management of patients with HCC.

With the Mn2+-endowed r1 relaxivity (1.38 mM-1 s-1), the DPGMA nanocomplexes can also be used for tumor MR imaging. The designed dendrimer-mediated MPN platform may be developed as an advanced nanomedicine to tackle other cancer types.

(-)-gossypol acetate and (+)-gossypol acetate play positive roles in the treatment and prevention of uterine fibroids. Gossypol optical isomers cause liver damage through multiple targets and pathways.