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Steroid sulfatase: molecular biology, regulation, and inhibition.
TLDR
The development of potent STS inhibitors will allow investigation of the role of this enzyme in physiological and pathological processes, and one such inhibitor, 667 COUMATE, has entered a phase I trial in postmenopausal women with breast cancer. Expand
Regulation of calcium signalling in T lymphocytes by the second messenger cyclic ADP-ribose
TLDR
The presence, causal relation and biological significance of the major constituents of the cADPR/calcium-signalling pathway in human T cells are shown. Expand
cGMP mobilizes intracellular Ca2+ in sea urchin eggs by stimulating cyclic ADP-ribose synthesis
TLDR
A novel action of 3',5'-cyclic guanosine monophosphate (cGMP) is demonstrated in stimulating the synthesis of cADPR from β-NAD+ by activating its synthetic enzyme ADP-ribosyl cyclase9–11 in sea urchin eggs and egg homogenates. Expand
Pharmacokinetics and efficacy of 2-methoxyoestradiol and 2-methoxyoestradiol-bis-sulphamate in vivo in rodents
TLDR
The resistance to metabolism shown by 2-MeOE2bisMATE and its ability to inhibit tumour growth in vivo suggest that this compound should have considerable potential for development as a novel anticancer drug. Expand
Nicotinic Acid Adenine Dinucleotide Phosphate (Naadp+) Is an Essential Regulator of T-Lymphocyte Ca2+-Signaling
TLDR
Microinjection of a self-inactivating concentration of NAADP+ completely abolished subsequent stimulation of Ca2+-signaling via the T cell receptor/CD3 complex, indicating that a functional NAadP+ Ca2-release system is essential for T-lymphocyte Ca2+. Expand
Estrone sulfamates: potent inhibitors of estrone sulfatase with therapeutic potential.
Characterization of cyclic adenosine diphosphate-ribose-induced Ca2+ release in T lymphocyte cell lines.
TLDR
The identity of this endogenous material was further confirmed by its ability to release Ca2+ in saponin-permeabilized Jurkat T cells and the presence of endogenous cADPr was analyzed directly by HPLC. Expand
Inhibition of steroid sulphatase activity by tricyclic coumarin sulphamates
TLDR
Surprisingly, in vivo 6615 COUMATE proved to be the most active drug, inhibiting rat liver E1-STS activity by 23 and 94% when assayed 24 h after administration of the 0.1 and 1 mg/kg doses. Expand
Regulation of steroid sulphatase expression and activity in breast cancer
TLDR
Investigation of the regulation of STS mRNA expression in cultured breast tissue fibroblasts and MCF-7 cells suggests that TNFalpha and IL-6 may increase STS activity via a post-translational modification of the enzyme or by increasing substrate availability. Expand
Phase I Study of STX 64 (667 Coumate) in Breast Cancer Patients: The First Study of a Steroid Sulfatase Inhibitor
TLDR
STX64 is a potent, well-tolerated STS inhibitor that inhibits STS activity in PBLs and tumor tissues and causes significant decreases in serum concentrations of steroids with estrogenic properties. Expand
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