Search Results - "Lubbers, Laura"
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Precision medicine for genetic epilepsy on the horizon: Recent advances, present challenges, and suggestions for continued progress
Published in Epilepsia (Copenhagen) (01-10-2022)“…The genetic basis of many epilepsies is increasingly understood, giving rise to the possibility of precision treatments tailored to specific genetic…”
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Estradiol and ERβ agonists enhance recognition memory, and DPN, an ERβ agonist, alters brain monoamines
Published in Neurobiology of learning and memory (01-11-2010)“…► Estradiol enhances recognition memory. ► Estrogen enhancements in memory rely on estrogen receptor (ER) beta. ► DPN, an ER beta agonist, alters monoaminergic…”
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3
Transcriptional Architecture of the Primate Neocortex
Published in Neuron (Cambridge, Mass.) (22-03-2012)“…Genome-wide transcriptional profiling was used to characterize the molecular underpinnings of neocortical organization in rhesus macaque, including cortical…”
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4
Silencing Myostatin Using Cholesterol-conjugated siRNAs Induces Muscle Growth
Published in Molecular therapy. Nucleic acids (02-08-2016)“…Short interfering RNAs (siRNAs) are a valuable tool for gene silencing with applications in both target validation and therapeutics. Many advances have…”
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Antiepileptogenesis and disease modification: Progress, challenges, and the path forward—Report of the Preclinical Working Group of the 2018 NINDS‐sponsored antiepileptogenesis and disease modification workshop
Published in Epilepsia open (01-06-2021)“…Epilepsy is one of the most common chronic brain diseases and is often associated with cognitive, behavioral, or other medical conditions. The need for…”
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Applicability of in vitro-in vivo translation of cathepsin K inhibition from animal species to human with the use of free-drug hypothesis
Published in Naunyn-Schmiedeberg's archives of pharmacology (01-04-2017)“…The correlation of in vitro inhibition of cathepsin K (CatK) activity and in vivo suppression of collagen I biomarkers was examined with three selective CatK…”
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A team science approach for the preclinical and clinical characterization and biomarker development for post‐traumatic epilepsy
Published in Epilepsia open (01-09-2023)“…Objective Post‐traumatic epilepsy (PTE) is an acquired epilepsy that develops in the months or years following a traumatic brain injury (TBI) and can lead to…”
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Nuclear and Extranuclear Estrogen Binding Sites in the Rat Forebrain and Autonomic Medullary Areas
Published in Endocrinology (Philadelphia) (01-07-2008)“…Immunocytochemical studies have shown that nuclear and extranuclear estrogen receptors (ERs) are present in several extrahypothalamic brain regions. The goal…”
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Preclinical evaluation of [11C]L‐235 as a radioligand for Positron Emission Tomography cathepsin K imaging in bone
Published in Journal of labelled compounds & radiopharmaceuticals (01-04-2021)“…The cathepsin K (CatK) enzyme is abundantly expressed in osteoclasts, and CatK inhibitors have been developed for the treatment of osteoporosis. In our effort…”
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Determination of in Vivo Enzyme Occupancy Utilizing Inhibitor Dissociation Kinetics
Published in Journal of the American Chemical Society (09-09-2015)“…During drug discovery, assessment of in vivo target occupancy by therapeutic candidates is often required for predicting clinical efficacy. Current strategies…”
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Transposition of three amino acids transforms the human metabotropic glutamate receptor (mGluR)-3-positive allosteric modulation site to mGluR2, and additional characterization of the mGluR2-positive allosteric modulation site
Published in The Journal of pharmacology and experimental therapeutics (01-07-2008)“…Glutamate is a major neurotransmitter in the central nervous system, and abnormal glutamate neurotransmission has been implicated in many neurological…”
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Estrogen receptor (ER) subtype agonists alter monoamine levels in the female rat brain
Published in The Journal of steroid biochemistry and molecular biology (01-11-2010)“…We assessed the effects of subtype-selective ER agonists on monoamine levels in discrete regions of the female rat brain. Ovariectomized (ovx) rats were…”
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Suppression of cathepsin K biomarker in synovial fluid as a free-drug–driven process
Published in Journal of circulating biomarkers (01-01-2019)“…Cathepsin K (CatK) inhibitors exhibited chondroprotective and pain-reducing effects in animal models, however, improvements were relatively modest at dose…”
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A team science approach to discover novel targets for infantile spasms (IS)
Published in Epilepsia open (01-03-2021)“…Infantile spasms (IS) is a devastating epilepsy syndrome that typically begins in the first year of life. Symptoms consist of stereotypical spasms,…”
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Proof-of-concept Studies for siRNA-mediated Gene Silencing for Coagulation Factors in Rat and Rabbit
Published in Molecular therapy. Nucleic acids (01-01-2015)“…The present study aimed at establishing feasibility of delivering short interfering RNA (siRNA) to target the coagulation cascade in rat and rabbit, two…”
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Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists
Published in Bioorganic & medicinal chemistry letters (01-08-2010)“…Medicinal chemistry efforts have identified a quinolinone class of potent NPSR antagonists that readily cross the blood–brain barrier. Optimization efforts…”
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Differential Mass Spectrometry of Rat Plasma Reveals Proteins That Are Responsive to 17β-Estradiol and a Selective Estrogen Receptor Modulator PPT
Published in Journal of proteome research (03-10-2008)“…Estrogens are a class of steroid hormones that interact with two related but distinct nuclear receptors, estrogen receptor (ER) α and β. To identify potential…”
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MK-7128, a novel CB1 receptor inverse agonist, improves scopolamine-induced learning and memory deficits in mice
Published in Behavioural pharmacology (01-04-2011)“…Cannabinoid receptors (CBRs) play an important role in a variety of physiological functions and have been considered drug targets for obesity and psychiatric…”
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PISA, A novel pharmacodynamic assay for assessing poly(ADP-ribose) polymerase (PARP) activity in situ
Published in Journal of pharmacological and toxicological methods (01-05-2010)“…Poly ADP-ribose polymerase (PARP) maintains genomic integrity by repairing DNA strand breaks, however over-activation of PARP following neural tissue injury is…”
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Estrogen Receptor β Messenger Ribonucleic Acid Expression in the Forebrain of Proestrous, Pregnant, and Lactating Female Rats
Published in Endocrinology (Philadelphia) (01-05-2003)“…Estrogen receptor (ER)β is present in hypothalamic and limbic neurons of female rat brains, but little is known about its regulation under physiological…”
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