IDH mutations in glioma and acute myeloid leukemia

L Dang, S Jin, SM Su - Trends in molecular medicine, 2010 - cell.com
The systematic sequencing of glioblastoma multiforme (GBM) genomes has identified the
recurrent mutation of IDH1, a gene encoding NADP+-dependent isocitrate dehydrogenase 1 …

Rhodanine as a privileged scaffold in drug discovery

T Tomasic, LP Masic - Current Medicinal Chemistry, 2009 - ingentaconnect.com
Rhodanines, thiazolidine-2, 4-diones and pseudothiohydantoins have become a very
interesting class of heterocyclic compounds since the introduction of various glitazones and …

Cell-based assays for high-throughput screening

WF An, N Tolliday - Molecular biotechnology, 2010 - Springer
Cell-based assays represent approximately half of all high-throughput screens currently
performed. Here, we review in brief the history and status of high-throughput screening …

Target identification in chemical genetics: the (often) missing link

L Burdine, T Kodadek - Chemistry & biology, 2004 - cell.com
Target Identification in Chemical Genetics: Chemistry & Biology Skip to Main Content
Advertisement Cell Chemical Biology This journal offers authors two options (open access or …

Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation

RA Ward, C Brassington, AL Breeze… - Journal of medicinal …, 2012 - ACS Publications
Lactate dehydrogenase A (LDHA) catalyzes the conversion of pyruvate to lactate, utilizing
NADH as a cofactor. It has been identified as a potential therapeutic target in the area of …

Fragment-based lead discovery: a chemical update

DA Erlanson - Current opinion in biotechnology, 2006 - Elsevier
Fragment-based lead discovery constructs drug leads from small molecular fragments. In
theory, this is a highly efficient method for drug discovery, and the technique has become …

Small-molecule inhibitors of human LDH5

C Granchi, I Paterni, R Rani… - Future medicinal …, 2013 - Taylor & Francis
The latest findings on the role played by human LDH5 (h LDH5) in the promotion of
glycolysis in invasive tumor cells indicates that this enzyme subtype is a promising …

Fragment growing and linking lead to novel nanomolar lactate dehydrogenase inhibitors

A Kohlmann, SG Zech, F Li, T Zhou… - Journal of medicinal …, 2013 - ACS Publications
Lactate dehydrogenase A (LDH-A) catalyzes the interconversion of lactate and pyruvate in
the glycolysis pathway. Cancer cells rely heavily on glycolysis instead of oxidative …

Estimating protein− ligand binding affinity using high-throughput screening by NMR

MD Shortridge, DS Hage, GS Harbison… - Journal of …, 2008 - ACS Publications
Many of today's drug discovery programs use high-throughput screening methods that rely
on quick evaluations of protein activity to rank potential chemical leads. By monitoring …

Antibacterial drug discovery and structure-based design

JJ Barker - Drug Discovery Today, 2006 - Elsevier
Bacterial resistance continues to develop and pose a significant threat, both in hospitals
and, more recently, in the community. A focus on other therapeutic areas by the larger …