Hypoxia-targeted drug delivery

A Sharma, JF Arambula, S Koo, R Kumar… - Chemical Society …, 2019 - pubs.rsc.org
Hypoxia is a state of low oxygen tension found in numerous solid tumours. It is typically
associated with abnormal vasculature, which results in a reduced supply of oxygen and …

Toward a Detailed Understanding of Base Excision Repair Enzymes:  Transition State and Mechanistic Analyses of N-Glycoside Hydrolysis and N-Glycoside …

PJ Berti, JAB McCann - Chemical reviews, 2006 - ACS Publications
This review focuses on the chemistry performed by base excision repair (BER) enzymes,
enzymes that remove nucleobases from DNA in the first step of the repair of many types of …

Diverse, high-quality test set for the validation of protein− ligand docking performance

MJ Hartshorn, ML Verdonk, G Chessari… - Journal of medicinal …, 2007 - ACS Publications
A procedure for analyzing and classifying publicly available crystal structures has been
developed. It has been used to identify high-resolution protein− ligand complexes that can …

The dual role of thymidine phosphorylase in cancer development and chemotherapy

A Bronckaers, F Gago, J Balzarini… - Medicinal research …, 2009 - Wiley Online Library
Thymidine phosphorylase (TP), also known as “platelet‐derived endothelial cell growth
factor”(PD‐ECGF), is an enzyme, which is upregulated in a wide variety of solid tumors …

Functionalized nitroimidazole scaffold construction and their pharmaceutical applications: a 1950–2021 comprehensive overview

R Gupta, S Sharma, R Singh, RA Vishwakarma… - Pharmaceuticals, 2022 - mdpi.com
Nitroimidazole represents one of the most essential and unique scaffolds in drug discovery
since its discovery in the 1950s. It was K. Maeda in Japan who reported in 1953 the first …

Therapeutic potential of the dual‐targeted TAS‐102 formulation in the treatment of gastrointestinal malignancies

OH Temmink, T Emura, M De Bruin… - Cancer …, 2007 - Wiley Online Library
Current treatment modalities for cancer combine cytotoxic drugs against DNA and novel
targeted drugs affecting signal transduction pathways, which are required for growth …

DrugPred: a structure-based approach to predict protein druggability developed using an extensive nonredundant data set

A Krasowski, D Muthas, A Sarkar… - Journal of chemical …, 2011 - ACS Publications
Judging if a protein is able to bind orally available molecules with high affinity, ie if a protein
is druggable, is an important step in target assessment. In order to derive a structure-based …

[HTML][HTML] Chemical synthesis, molecular modelling, and evaluation of anticancer activity of some pyrazol-3-one Schiff base derivatives

SM Bensaber, HA Allafe, NB Ermeli… - Medicinal Chemistry …, 2014 - Springer
A series of twelve pyrazol-3-one Schiffs base derivatives (5–17) were designed and
synthesized by microwave-assisted chemical synthesis. Their purity was confirmed by …

Crystal structure of human thymidine phosphorylase in complex with a small molecule inhibitor

RA Norman, ST Barry, M Bate, J Breed, JG Colls… - Structure, 2004 - cell.com
Human thymidine phosphorylase (HTP), also known as platelet-derived endothelial cell
growth factor (PD-ECGF), is overexpressed in certain solid tumors where it is linked to poor …

Designing prodrugs and bioprecursors

CG Wermuth - The practice of medicinal chemistry, 2008 - Elsevier
Publisher Summary The bioavailability of molecules exclusively screened through in vitro
assays can be low. In vivo administration is limited to the parenteral route, and their clinical …