Is target-based drug discovery efficient? Discovery and “off-target” mechanisms of all drugs

A Sadri - Journal of medicinal chemistry, 2023 - ACS Publications
Target-based drug discovery is the dominant paradigm of drug discovery; however, a
comprehensive evaluation of its real-world efficiency is lacking. Here, a manual systematic …

Biologic and clinical significance of androgen receptor variants in castration resistant prostate cancer

KE Ware, MA Garcia-Blanco… - Endocrine-related …, 2014 - erc.bioscientifica.com
As prostate cancer (PCa) progresses to the lethal castration resistant and metastatic form,
genetic and epigenetic adaptation, clonal selection, and evolution of the tumor …

[HTML][HTML] Decoding the androgen receptor splice variants

C Lu, J Luo - Translational andrology and urology, 2013 - ncbi.nlm.nih.gov
In the past five years, multiple structurally and functionally distinct androgen receptor (AR)
splice variants have been decoded and characterized. The mature transcripts for the …

Androgen receptor (AR) positive vs negative roles in prostate cancer cell deaths including apoptosis, anoikis, entosis, necrosis and autophagic cell death

S Wen, Y Niu, SO Lee, C Chang - Cancer treatment reviews, 2014 - Elsevier
Androgen/androgen receptor (AR) signaling plays pivotal roles in the prostate development
and homeostasis as well as in the progression of prostate cancer (PCa). Androgen …

Ursolic acid induces apoptosis of prostate cancer cells via the PI3K/Akt/mTOR pathway

Y Meng, ZM Lin, N Ge, DL Zhang, J Huang… - The American journal of …, 2015 - World Scientific
Ursolic acid (UA), a pentacyclic triterpenoid, is known to exert antitumor activity in breast,
lung, liver and colon cancers. Nonetheless, the underlying mechanism of ursolic acid in …

Combinatorial approaches of nanotherapeutics for inflammatory pathway targeted therapy of prostate cancer

RP Johnson, CK Ratnacaram, L Kumar, J Jose - Drug Resistance Updates, 2022 - Elsevier
Prostate cancer (PC) is the most prevalent male urogenital cancer worldwide. PC patients
presenting an advanced or metastatic cancer succumb to the disease, even after therapeutic …

Synergistic antitumour activity of sorafenib in combination with tetrandrine is mediated by reactive oxygen species (ROS)/Akt signaling

J Wan, T Liu, L Mei, J Li, K Gong, C Yu, W Li - British journal of cancer, 2013 - nature.com
Background: Sorafenib is a potent inhibitor against Raf kinase and several receptor tyrosine
kinases that has been approved for the clinical treatment of advanced renal and liver cancer …

Increasing AR by HIF-2α inhibitor (PT-2385) overcomes the side-effects of sorafenib by suppressing hepatocellular carcinoma invasion via alteration of pSTAT3, pAKT …

J Xu, L Zheng, J Chen, Y Sun, H Lin, R Jin… - Cell death & …, 2017 - nature.com
Although sorafenib is currently used as a standard treatment for advanced hepatocellular
carcinoma, low response rate, transient and limited efficacy, primary and acquired …

[HTML][HTML] Adaptive responses of androgen receptor signaling in castration-resistant prostate cancer

S Perner, MV Cronauer, AJ Schrader, H Klocker… - Oncotarget, 2015 - ncbi.nlm.nih.gov
Abstract Prostate Cancer (PCa) is an important age-related disease being the most common
cancer malignancy and the second leading cause of cancer mortality in men in Western …

[HTML][HTML] ROS-mediated JNK/p38-MAPK activation regulates Bax translocation in Sorafenib-induced apoptosis of EBV-transformed B cells

GB Park, Y Choi, YS Kim, HK Lee… - … journal of oncology, 2014 - spandidos-publications.com
Sorafenib (SRF) is a multi-kinase inhibitor that has been shown to have antitumor activity
against several types of cancers, but the effect of SRF on EBV-transformed B cells is …