Search Results - "Palmer, Stephen S."
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c-Jun NH2 -terminal kinase inhibitor bentamapimod reduces induced endometriosis in baboons: an assessor-blind placebo-controlled randomized study
Published in Fertility and sterility (01-03-2016)“…Objective To test the hypothesis that the c-Jun NH2 -terminal kinase (JNK) inhibitor (JNKI) bentamapimod (AS602801/PGL5001) can reduce induced endometriosis in…”
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Discovery and Development of Small Molecule Allosteric Modulators of Glycoprotein Hormone Receptors
Published in Frontiers in endocrinology (Lausanne) (14-09-2015)“…Glycoprotein hormones, follicle-stimulating hormone (FSH), luteinizing hormone (LH), and thyroid-stimulating hormone (TSH) are heterodimeric proteins with a…”
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3
Biomarkers in reproductive medicine: the promise, and can it be fulfilled?
Published in Fertility and sterility (15-03-2013)“…A biomarker can be used for early diagnosis of a disease, identification of individuals for disease prevention, as a potential drug target, or as a potential…”
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Pharmacological Characterization of Low Molecular Weight Biased Agonists at the Follicle Stimulating Hormone Receptor
Published in International journal of molecular sciences (12-09-2021)“…Follicle-stimulating hormone receptor (FSHR) plays a key role in reproduction through the activation of multiple signaling pathways. Low molecular weight (LMW)…”
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Follicle-Stimulating Hormone Induces Lipid Droplets via Gαi/o and β-Arrestin in an Endometrial Cancer Cell Line
Published in Frontiers in endocrinology (Lausanne) (03-02-2022)“…Follicle-stimulating hormone (FSH) and its G protein-coupled receptor, FSHR, represents a paradigm for receptor signaling systems that activate multiple and…”
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Follicle-stimulating Hormone Activates Extracellular Signal-regulated Kinase but Not Extracellular Signal-regulated Kinase Kinase through a 100-kDa Phosphotyrosine Phosphatase
Published in The Journal of biological chemistry (28-02-2003)“…In this report we sought to elucidate the mechanism by which the follicle-stimulating hormone (FSH) receptor signals to promote activation of the p42/p44…”
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Discovery and characterization of bromodomain 2–specific inhibitors of BRDT
Published in Proceedings of the National Academy of Sciences - PNAS (02-03-2021)“…Bromodomain testis (BRDT), a member of the bromodomain and extraterminal (BET) subfamily that includes the cancer targets BRD2, BRD3, and BRD4, is a validated…”
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Discovery of Highly Potent and BMPR2-Selective Kinase Inhibitors Using DNA-Encoded Chemical Library Screening
Published in Journal of medicinal chemistry (09-02-2023)“…The discovery of monokinase-selective inhibitors for patients is challenging because the 500+ kinases encoded by the human genome share highly conserved…”
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DNA-encoded chemistry technology yields expedient access to SARS-CoV-2 Mpro inhibitors
Published in Proceedings of the National Academy of Sciences - PNAS (07-09-2021)“…Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) has killed more than 4 million humans globally, but there is no bona fide Food and Drug…”
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Discovery of potent BET bromodomain 1 stereoselective inhibitors using DNA-encoded chemical library selections
Published in Proceedings of the National Academy of Sciences - PNAS (31-05-2022)“…SignificanceBET bromodomain inhibition is therapeutic in multiple diseases; however, pan-BET inhibitors have induced significant myelosuppression and…”
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Discovery of highly potent and ALK2/ALK1 selective kinase inhibitors using DNA-encoded chemistry technology
Published in Proceedings of the National Academy of Sciences - PNAS (19-11-2024)“…Activin receptor type 1 (ACVR1; ALK2) and activin receptor like type 1 (ACVRL1; ALK1) are transforming growth factor beta family receptors that integrate…”
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Reversible male contraception by targeted inhibition of serine/threonine kinase 33
Published in Science (American Association for the Advancement of Science) (24-05-2024)“…Men or mice with homozygous serine/threonine kinase 33 ( ) mutations are sterile owing to defective sperm morphology and motility. To chemically evaluate STK33…”
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Pharmacological and Functional Characterization of Novel EP and DP Receptor Agonists: DP1 Receptor Mediates Penile Erection in Multiple Species
Published in Journal of sexual medicine (01-02-2008)“…Despite the widespread use of prostaglandin E1 as an efficacious treatment for male erectile dysfunction for more than two decades, research on prostanoid…”
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Bentamapimod (JNK Inhibitor AS602801) Induces Regression of Endometriotic Lesions in Animal Models
Published in Reproductive sciences (Thousand Oaks, Calif.) (01-01-2016)“…Endometriosis is an estrogen (ER)-dependent gynecological disease caused by the growth of endometrial tissue at extrauterine sites. Current endocrine therapies…”
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A long-acting tumor necrosis factor alpha-binding protein demonstrates activity in both in vitro and in vivo models of endometriosis
Published in The Journal of pharmacology and experimental therapeutics (01-08-2010)“…Endometriosis is characterized by the presence of elevated proinflammatory cytokines such as tumor necrosis factor (TNF) alpha in the peritoneal cavity…”
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Relaxin Increases Secretion of Matrix Metalloproteinase-2 and Matrix Metalloproteinase-9 during Uterine and Cervical Growth and Remodeling in the Pig
Published in Endocrinology (Philadelphia) (01-09-2001)“…Matrix metalloproteinases are proteolytic enzymes that degrade the extracellular matrix and are essential for tissue remodeling. Uterine and cervical growth…”
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Discovery of new molecules for future treatment of infertility
Published in Reproductive biomedicine online (01-06-2005)“…The introduction of recombinant gonadotrophins for the treatment of infertility has been an important advance in improving the quality and consistency of…”
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Relaxin Increases Secretion of Tissue Inhibitor of Matrix Metalloproteinase-1 and -2 during Uterine and Cervical Growth and Remodeling in the Pig
Published in Endocrinology (Philadelphia) (01-01-2002)“…Remodeling of reproductive organs during pregnancy requires degradation and resynthesis of structural barriers to cell invasion. Matrix metalloproteinases…”
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DNA-encoded chemistry technology yields expedient access to SARS-CoV-2 M pro inhibitors
Published in Proceedings of the National Academy of Sciences - PNAS (07-09-2021)“…Significance SARS-CoV-2 has had a crippling impact on human life globally. Vaccine development has been used as a first-line strategy for COVID-19 prevention…”
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Fluorescence polarization assay and SDS-PAGE confirms matrilysin degrades fibronectin and collagen IV whereas gelatinase A degrades collagen IV but not fibronectin
Published in Connective tissue research (01-01-2001)“…Matrilysin and gelatinase A are hypothesized to have significant roles in uterine and ovarian function. However, proteolytic activity assays for these enzymes…”
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