Indole Inhibitors of Human Nonpancreatic Secretory Phospholipase A2. 1. Indole-3-acetamides

…, ER McKinney, ED Mihelich, JL Olkowski… - Journal of medicinal …, 1996 - ACS Publications
Phospholipases (PLAs) produce rate-limiting precursors in the biosynthesis of various types
of biologically active lipids involved in inflammatory processes. Increased levels of human …

Indole Inhibitors of Human Nonpancreatic Secretory Phospholipase A2. 3. Indole-3-glyoxamides

…, ER McKinney, ED Mihelich, JL Olkowski… - Journal of medicinal …, 1996 - ACS Publications
The preceding papers of this series detail the development of functionalized indole-3-acetamides
as inhibitors of hnps-PLA 2 . We describe here the extension of the structure−activity …

Indole Inhibitors of Human Nonpancreatic Secretory Phospholipase A2. 2. Indole-3-acetamides with Additional Functionality

…, ER McKinney, ED Mihelich, JL Olkowski… - Journal of medicinal …, 1996 - ACS Publications
As reported in our previous paper, a series of indole-3-acetamides which possessed
potency and selectivity as inhibitors of human nonpancreatic secretory phospholipase A 2 (hnps-…

Neuroprotection mediated by glutamate carboxypeptidase II (NAALADase) inhibition requires TGF-β

AG Thomas, W Liu, JL Olkowski, Z Tang, Q Lin… - European journal of …, 2001 - Elsevier
Inhibition of glutamate carboxypeptidase (GCP) II (EC 3.4.17.21), also termed N-acetylated
alpha-linked acidic dipeptidase (NAALADase), has been shown to protect against ischemic …

Neuroprotection afforded by NAAG and NAALADase inhibition requires glial cells and metabotropic glutamate receptor activation

AG Thomas, JL Olkowski, BS Slusher - European journal of pharmacology, 2001 - Elsevier
N-acetylated-α-linked-acidic-dipeptidase (NAALADase or glutamate carboxypeptidase II)
cleaves the neuropeptide N-acetyl-aspartyl-glutamate (NAAG) to glutamate and N-acetyl-…

N-acetylated α-linked acidic dipeptidase converts N-acetylaspartylglutamate from a neuroprotectant to a neurotoxin

AG Thomas, JJ Vornov, JL Olkowski, AT Merion… - … of Pharmacology and …, 2000 - ASPET
We previously reported that inhibition of the brain enzymeN-acetylated α-linked acidic
dipeptidase (NAALADase; glutamate carboxypeptidase II) robustly protects cortical neurons from …

D-phe-pro-p-amidinobenzylamine: A potent and highly selective thrombin inhibitor

…, DS Gifford-Moore, ND Jones, JL Olkowski… - Bioorganic & Medicinal …, 1996 - Elsevier
The design, synthesis, and enzyme inhibitory profile of D-Phe-Pro-p-Amidinobenzylamine
are presented. This compound has inhibitory activity equivalent to D-Phe-Pro-Arg-H, two …

Serine protease selectivity of the thrombin inhibitor D-Phe-Pro-agmatine and its homologs

…, DS Gifford-Moore, ND Jones, JL Olkowski… - Bioorganic & Medicinal …, 1995 - Elsevier
Analogs of D-Phe-Pro-Agmatine were assayed for inhibititory activity versus thrombin, trypsin,
plasmin, n-tPA and urokinase. The X-ray structure of the thrombin/D-Phe-Pro-Agmatine co-…

Use of identical assay conditions for cocaine analog binding and dopamine uptake to identify potential cocaine antagonists

BS Slusher, CW Tiffany, JL Olkowski… - Drug and alcohol …, 1997 - Elsevier
The addictive and euphorogenic properties of cocaine are thought to result from inhibition of
the dopamine transporter (DAT). Recent evidence suggests that dopamine and cocaine …

Toxicity induced by a polyglutamated folate analog is attenuated by NAALADase inhibition

AG Thomas, JL Olkowski, JJ Vornov, BS Slusher - Brain research, 1999 - Elsevier
Folates have been shown to be neurotoxic and convulsive. Endogenously, folates exist in
the brain in a polyglutamated form with 1–7 terminal glutamates (approx. 1 μM). The brain …