The current treatment paradigm for pancreatic ductal adenocarcinoma and barriers to therapeutic efficacy

DR Principe, PW Underwood, M Korc… - Frontiers in …, 2021 - frontiersin.org
Pancreatic ductal adenocarcinoma (PDAC) has a dismal prognosis, with a median survival
time of 10-12 months. Clinically, these poor outcomes are attributed to several factors …

Colchicine-binding site inhibitors from chemistry to clinic: a review

EC McLoughlin, NM O'Boyle - Pharmaceuticals, 2020 - mdpi.com
It is over 50 years since the discovery of microtubules, and they have become one of the
most important drug targets for anti-cancer therapies. Microtubules are predominantly …

Intrinsic and extrinsic factors affecting microtubule dynamics in normal and cancer cells

F Borys, E Joachimiak, H Krawczyk, H Fabczak - Molecules, 2020 - mdpi.com
Microtubules (MTs), highly dynamic structures composed of α-and β-tubulin heterodimers,
are involved in cell movement and intracellular traffic and are essential for cell division …

βIII-tubulin overexpression in cancer: Causes, consequences, and potential therapies

A Kanakkanthara, JH Miller - Biochimica et Biophysica Acta (BBA)-Reviews …, 2021 - Elsevier
Class III β-tubulin (βIII-tubulin) is frequently overexpressed in human tumors and is
associated with resistance to microtubule-targeting agents, tumor aggressiveness, and poor …

Structure-Guided Design, Synthesis, and Biological Evaluation of (2-(1H-Indol-3-yl)-1H-imidazol-4-yl)(3,4,5-trimethoxyphenyl) Methanone (ABI-231) Analogues …

Q Wang, KE Arnst, Y Wang, G Kumar… - Journal of Medicinal …, 2019 - ACS Publications
ABI-231 is a potent, orally bioavailable tubulin inhibitor that interacts with the colchicine
binding site and is currently undergoing clinical trials for prostate cancer. Guided by the …

Tannic acid inhibits lipid metabolism and induce ROS in prostate cancer cells

PKB Nagesh, P Chowdhury, E Hatami, S Jain, N Dan… - Scientific reports, 2020 - nature.com
Prostate cancer (PCa) cells exploit the aberrant lipid signaling and metabolism as their
survival advantage. Also, intracellular storage lipids act as fuel for the PCa proliferation …

A Phase Ib/II Study of Sabizabulin, a Novel Oral Cytoskeleton Disruptor, in Men with Metastatic Castration-resistant Prostate Cancer with Progression on an Androgen …

MC Markowski, R Tutrone, C Pieczonka… - Clinical Cancer …, 2022 - AACR
Purpose: Sabizabulin, an oral cytoskeleton disruptor, was tested in a phase Ib/II clinical
study in men with metastatic castration-resistant prostate cancer (mCRPC). Patients and …

Molecular mechanisms associated with chemoresistance in esophageal cancer

M Lohan-Codeço, ML Barambo-Wagner… - Cellular and Molecular …, 2022 - Springer
Esophageal cancer (EC) is one of the most incident and lethal tumors worldwide. Although
surgical resection is an important approach in EC treatment, late diagnosis, metastasis and …

Tubulin inhibitors binding to colchicine-site: a review from 2015 to 2019

LY **a, YL Zhang, R Yang, ZC Wang… - Current medicinal …, 2020 - ingentaconnect.com
Due to the three domains of the colchicine-site which is conducive to the combination with
small molecule compounds, colchicine-site on the tubulin has become a common target for …

Cross-linked polyphenol-based drug nano-self-assemblies engineered to blockade prostate cancer senescence

PKB Nagesh, P Chowdhury, E Hatami… - … applied materials & …, 2019 - ACS Publications
Cellular senescence is one of the prevailing issues in cancer therapeutics that promotes
cancer relapse, chemoresistance, and recurrence. Patients undergoing persistent …