Multiple folate enzyme inhibition: mechanism of a novel pyrrolopyrimidine-based antifolate LY231514 (MTA)

C Shih, LL Habeck, LG Mendelsohn, VJ Chen… - Advances in enzyme …, 1998 - Elsevier
Since the late 1950 s, extensive research efforts have been devoted to the discovery and
development of antifolate antimetabolites as chemotherapeutic agents for the management of …

LY231514, a pyrrolo [2, 3-d] pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes

…, LS Gossett, SB Gates, WC MacKellar, LL Habeck… - Cancer research, 1997 - AACR
N-[4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]-benzoyl]-l-glutamic
acid (LY231514) is a novel pyrrolo[2,3-d]pyrimidine-based antifolate currently undergoing …

Enzyme inhibition, polyglutamation, and the effect of LY231514 (MTA) on purine biosynthesis.

LG Mendelsohn, C Shih, VJ Chen, LL Habeck… - Seminars in …, 1999 - europepmc.org
The pyrrolopyrimidine-based antifolate, N-¿ 4-[2-(2-amino-3, 4-dihydro-4-oxo-7H-pyrrolo [2,
3-d] pyrimidin-5-yl) ethyl] benzoyl¿ glutamic acid, LY231514 (MTA) has demonstrated …

The role of dietary folate in modulation of folate receptor expression, folylpolyglutamate synthetase activity and the efficacy and toxicity of lometrexol

LG Mendelsohn, SB Gates, LL Habeck… - Advances in enzyme …, 1996 - Elsevier
We have studied the molecular effects of a LFD in a murine model in order to better define the
biochemical changes associated with folate deficiency. In addition, we have demonstrated …

[PDF][PDF] Substrate specificity of mammalian folylpolyglutamate synthetase for 5, 10-dideazatetrahydrofolate analogs.

LL Habeck, LG Mendelsohn, C Shih, EC Taylor… - Molecular …, 1995 - Citeseer
The metabolism of 5, 1 0-dideazatetrahydrofolate(DDATHF [lometrexol]) to polyglutamate
derivatives by folylpoly-y-gluta-mate synthetase(FPGS) plays a central role in the activity of this …

A novel class of monoglutamated antifolates exhibits tight-binding inhibition of human glycinamide ribonucleotide formyltransferase and potent activity against solid …

LL Habeck, TA Leitner, KA Shackelford, LS Gossett… - Cancer research, 1994 - AACR
… The pentaglutamate of Lometrexol had an ll-fold higher affinity for recombinant monofunctional
hGARFT than Lometrexol. Other groups have reported approximately 100-fold higher …

Characterization of folate receptor from normal and neoplastic murine tissue: influence of dietary folate on folate receptor expression.

…, LG Mendelsohn, KA Shackelford, LL Habeck… - Clinical cancer research …, 1996 - AACR
Membrane-associated folate receptors (FRs) have been detected in many mammalian species,
and multiple isoforms have been identified. The pharmacological properties of FRs from …

vir genes influence conjugal transfer of the Ti plasmid of Agrobacterium tumefaciens

SB Gelvin, LL Habeck - Journal of Bacteriology, 1990 - Am Soc Microbiol
Mutation of the genes virA, virB, virC, and virG of the Agrobacterium tumefaciens octopine-type
Ti plasmid pTiR10 was found to cause a 100- to 10,000-fold decrease in the frequency of …

Multiple copies of virG allow induction of Agrobacterium tumefaciens genes and T-DNA processing at alkaline pH.

CN Liu, TR Steck, LL Habeck, JA Meyer, SB Gelvin - 1993 - cabidigitallibrary.org
It is reported that several vir genes of the octopine-type Ti (tumour-inducing) plasmid pTiA6
of A. tumefaciens can be induced to high levels by acetosyringone in both minimal and rich …

Subdomains of the octopine synthase upstream activating element direct cell-specific expression in transgenic tobacco plants.

H Kononowicz, YE Wang, LL Habeck… - The Plant Cell, 1992 - academic.oup.com
Previous work has shown that the octopine synthase (ocs) gene encoded by the Agrobacterium
tumefaciens Ti-plasmid contains an upstream activating sequence necessary for its …