Voxelotor (GBT440), a first‐in‐class hemoglobin oxygen‐affinity modulator, has promising and reassuring preclinical and clinical data
Sign Up to like & getrecommendations! Published in 2018 at "American Journal of Hematology"
DOI: 10.1002/ajh.25042
Abstract: Voxelotor, a first-in-class drug, is currently being studied for the treatment of sickle cell disease in the United States and Europe that has received Breakthrough Therapy Designation (BTD) by the Food and Drug Administration (FDA)… read more here.
Keywords: hemoglobin; affinity; voxelotor; first class ... See more keywords
The Interregional Migration of Human Capital: The Case of “First-Class” University Graduates in China
Sign Up to like & getrecommendations! Published in 2021 at "Applied Spatial Analysis and Policy"
DOI: 10.1007/s12061-021-09401-7
Abstract: Human capital has been acknowledged as a key driver for innovation, thereby promoting regional economic development in the knowledge era. University graduates from China’s “first-class” universities—the top 42 universities, included in the “double first-class” initiative,… read more here.
Keywords: university; human capital; migration; first class ... See more keywords
Discovery of first-in-class imidazothiazole-based potent and selective ErbB4 (HER4) kinase inhibitors.
Sign Up to like & getrecommendations! Published in 2021 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2021.113674
Abstract: This article reports on novel imidazothiazole derivatives as first-in-class potent and selective ErbB4 (HER4) inhibitors. There are no other reported selective inhibitors of this kinase in the literature, that's why they are considered as first-in-class.… read more here.
Keywords: potent selective; kinase; selective erbb4; first class ... See more keywords
MRI findings are associated with time to return to play in first class cricket fast bowlers with side strain in Australia and England.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of science and medicine in sport"
DOI: 10.1016/j.jsams.2019.05.020
Abstract: OBJECTIVES To investigate the reliability of reporting and relationship between MRI parameters at injury and time to return to play (RTP) in first class cricket fast bowlers with side strain in Australia and England. DESIGN… read more here.
Keywords: time; rtp; fast bowlers; first class ... See more keywords
Understanding first-class passengers' luxury value perceptions in the US airline industry
Sign Up to like & getrecommendations! Published in 2018 at "Tourism Management Perspectives"
DOI: 10.1016/j.tmp.2018.07.001
Abstract: Abstract This study explored the importance of luxury value in the context of first-class flights. More specifically, it was proposed the role of luxury value in the formation of outcome variables. In addition, the moderating… read more here.
Keywords: first class; class passengers; luxury value;
Identification of First-in-Class Inhibitors of Kallikrein-Related Peptidase 6 That Promote Oligodendrocyte Differentiation.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c02175
Abstract: Multiple sclerosis (MS) is an autoimmune demyelinating disease of the central nervous system (CNS) that causes severe motor, sensory, and cognitive impairments. Kallikrein-related peptidase (KLK)6 is the most abundant serine protease secreted in the CNS,… read more here.
Keywords: kallikrein related; related peptidase; identification first; differentiation ... See more keywords
First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53
Sign Up to like & getrecommendations! Published in 2021 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.1c00605
Abstract: MINA53 is a JmjC domain 2-oxoglutarate-dependent oxygenase that catalyzes ribosomal hydroxylation and is a target of the oncogenic transcription factor c-MYC. Despite its anticancer target potential, no small-molecule MINA53 inhibitors are reported. Using ribosomal substrate… read more here.
Keywords: class inhibitors; mina53; oxygenase; first class ... See more keywords
Discovery of First-in-Class Peptidomimetic Neurolysin Activators Possessing Enhanced Brain Penetration and Stability.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00759
Abstract: Peptidase neurolysin (Nln) is an enzyme that functions to cleave various neuropeptides. Upregulation of Nln after stroke has identified the enzyme as a critical endogenous cerebroprotective mechanism and validated target for the treatment of ischemic… read more here.
Keywords: discovery; neurolysin; brain penetration; nln ... See more keywords
Discovery of the First-in-Class G9a/GLP Covalent Inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00652
Abstract: The highly homologous protein lysine methyltransferases G9a and GLP, which catalyze mono- and dimethylation of histone H3 lysine 9 (H3K9), have been implicated in various human diseases. To investigate functions of G9a and GLP in… read more here.
Keywords: glp; discovery first; first class; covalent ... See more keywords
Discovery and Development of First-in-Class ACKR3/CXCR7 Superagonists for Platelet Degranulation Modulation.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01198
Abstract: The atypical chemokine receptor 3 (ACKR3), formerly known as CXC-chemokine receptor 7 (CXCR7), has been postulated to regulate platelet function and thrombus formation. Herein, we report the discovery and development of first-in-class ACKR3 agonists, which… read more here.
Keywords: discovery development; platelet degranulation; cxcr7; first class ... See more keywords
Discovery of the First-in-Class Intestinal Restricted FXR and FABP1 Dual Modulator ZLY28 for the Treatment of Nonalcoholic Fatty Liver Disease.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01918
Abstract: The prevalence of nonalcoholic steatohepatitis (NASH) is increasing rapidly worldwide, and NASH has become a serious problem for human health. Recently, the selective activation of the intestinal farnesoid X receptor (FXR) was considered as a… read more here.
Keywords: class intestinal; restricted fxr; first class; intestinal restricted ... See more keywords