Inside the biochemical pathways of thymidylate synthase perturbed by anticancer drugs: Novel strategies to overcome cancer chemoresistance

L Taddia, D D'Arca, S Ferrari, C Marraccini… - Drug Resistance …, 2015 - Elsevier
Our current understanding of the mechanisms of action of antitumor agents and the precise
mechanisms underlying drug resistance is that these two processes are directly linked …

Antifolate inhibitors of thymidylate synthase as anticancer drugs

A Jarmula - Mini reviews in medicinal chemistry, 2010 - ingentaconnect.com
Inhibitors of thymidylate synthase (TS) play an essential role in the pharmacological
management of several tumors. Two antifolates, Raltitrexed and Pemetrexed, are licensed …

Future potential of thymidylate synthase inhibitors in cancer therapy

NL Lehman - Expert opinion on investigational drugs, 2002 - Taylor & Francis
Thymidylate synthase (TS) catalyses the de novo synthesis of deoxythymidylate and is a key
rate-limiting enzyme of DNA synthesis. The primary site of action of the classic antifolate …

Thymidylate synthase inhibitors as anticancer agents: from bench to bedside

E Chu, MA Callender, MP Farrell… - Cancer chemotherapy and …, 2003 - Springer
Thymidylate synthase (TS) is a folate-dependent enzyme that catalyzes the reductive
methylation of 2′-deoxyuridine-5′-monophosphate to 2′-deoxythymidine-5 …

The means to an end of tumor cell resistance to chemotherapeutic drugs targeting thymidylate synthase: shoot the messenger

RW Berg, PJ Ferguson, JM DeMoor… - Current drug …, 2002 - ingentaconnect.com
Thymidylate synthase (TS) is an essential enzyme in de novo synthesis of thymidylate, and
is required for DNA synthesis and cell proliferation in the absence of exogenous thymidine …

Folate-based thymidylate synthase inhibitors in cancer chemotherapy

Y Takemura, AL Jackman - Anti-cancer drugs, 1997 - journals.lww.com
Understanding the relationship between chemical structure and biological properties of
folate analogs, particularly their Interactions with the target enzymes, transport proteins and …

Standing the test of time: targeting thymidylate biosynthesis in cancer therapy

PM Wilson, PV Danenberg, PG Johnston… - Nature reviews Clinical …, 2014 - nature.com
Over the past 60 years, chemotherapeutic agents that target thymidylate biosynthesis and
the enzyme thymidylate synthase (TS) have remained among the most-successful drugs …

Thymidylate synthase structure, function and implication in drug discovery

MP Costi, S Ferrari, A Venturelli, S Calo… - Current medicinal …, 2005 - ingentaconnect.com
Recent methodologies applied to the drug discovery process, such as genomics and
proteomics, have greatly implemented our basic understanding of drug action and are giving …

Thymidylate synthase and drug resistance

GJ Peters, CL Van der Wilt, B Van Triest… - European Journal of …, 1995 - Elsevier
Thymidylate synthase is an important target for both fluorinated pyrimidines and for new
folate analogues. Resistance to 5-fluorouracil (5FU) can be related to insufficient inhibition …

A novel approach to thymidylate synthase as a target for cancer chemotherapy

Q Li, C Boyer, JY Lee, HM Shepard - Molecular Pharmacology, 2001 - ASPET
Tumor cell resistance to fluoropyrimidines and other inhibitors of thymidylate synthase (TS)
is a serious problem often associated with increased intracellular TS. Clinically, another …