Discovery and Characterization of Multiple Classes of Human CatSper Blockers
Sign Up to like & getrecommendations! Published in 2022 at "Chemmedchem"
DOI: 10.1002/cmdc.202000499
Abstract: The cation channel of sperm (CatSper) is a validated target for nonhormonal male contraception, but it lacks selective blockers, hindering studies to establish its role in both motility and capacitation. Via an innovative calcium uptake… read more here.
Keywords: discovery characterization; characterization multiple; catsper blockers; catsper ... See more keywords
Discovery and characterization of novel trans‐spliced products of human polyoma JC virus late transcripts from PML patients
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Cellular Physiology"
DOI: 10.1002/jcp.26219
Abstract: Although the human neurotropic polyomavirus, JC virus (JCV), was isolated almost a half century ago, understanding the molecular mechanisms governing its biology remains highly elusive. JCV infects oligodendrocytes and astrocytes in the central nervous system… read more here.
Keywords: pml patients; spliced products; late transcripts; coding regions ... See more keywords
Discovery and Characterization of a Novel Method for Effective Improvement of Cyclodextrin Yield and Product Specificity
Sign Up to like & getrecommendations! Published in 2019 at "Chemical Research in Chinese Universities"
DOI: 10.1007/s40242-019-8406-0
Abstract: Cyclodextrins(CDs) are widely used in food, pharmaceuticals, drug delivery, and chemical industries and in agriculture and environmental engineering. To improve the yield and selectivity of CDs, this work presented a facile, scalable and efficient enzymatic… read more here.
Keywords: product selectivity; yield product; yield; discovery characterization ... See more keywords
High-Throughput Discovery and Characterization of Human Transcriptional Effectors
Sign Up to like & getrecommendations! Published in 2020 at "Cell"
DOI: 10.1016/j.cell.2020.11.024
Abstract: Thousands of proteins localize to the nucleus; however, it remains unclear which contain transcriptional effectors. Here, we develop HT-recruit, a pooled assay where protein libraries are recruited to a reporter, and their transcriptional effects are… read more here.
Keywords: human transcriptional; characterization human; throughput discovery; transcriptional effectors ... See more keywords
Discovery and characterization of selective human sphingomyelin synthase 2 inhibitors.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.04.067
Abstract: Sphingomyelin synthase (SMS) is a membrane enzyme that catalyzes the synthesis of sphingomyelin, is required for the maintenance of plasma membrane microdomain fluidity, and has two isoforms: SMS1 and SMS2. Although these isoforms exhibit the… read more here.
Keywords: sms2 inhibitors; sms2; sphingomyelin synthase; sphingomyelin ... See more keywords
Rapid Discovery and Characterization of Synthetic Neutralizing Antibodies against Anthrax Edema Toxin.
Sign Up to like & getrecommendations! Published in 2019 at "Biochemistry"
DOI: 10.1021/acs.biochem.9b00184
Abstract: Anthrax, a lethal, weaponizable disease caused by Bacillus anthracis, acts through exotoxins that are primary mediators of systemic toxicity and also targets for neutralization by passive immunotherapy. The ease of engineering B. anthracis strains resistant… read more here.
Keywords: anthrax edema; discovery characterization; anthrax; antibody ... See more keywords
Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.0c00499
Abstract: Visceral leishmaniasis is responsible for up to 30,000 deaths every year. Current treatments have shortcomings that include toxicity and variable efficacy across endemic regions. Previously, we reported the discovery of GNF6702, a selective inhibitor of… read more here.
Keywords: proteasome inhibitor; inhibitor; proteasome; kinetoplastid selective ... See more keywords
Discovery and Characterization of the First Nonpeptide Antagonists for the Relaxin-3/RXFP3 System.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c00508
Abstract: The neuropeptide relaxin-3/RXFP3 system is involved in many important physiological processes such as stress responses, appetite control, and motivation for reward. To date, pharmacological studies of RXFP3 have been limited to peptide ligands. In this… read more here.
Keywords: discovery characterization; rxfp3 system; rxfp3; relaxin rxfp3 ... See more keywords
Discovery and Characterization of Synthesized and FDA-Approved Inhibitors of Clostridial and Bacillary Collagenases
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c00785
Abstract: In view of the worldwide antimicrobial resistance (AMR) threat, new bacterial targets and anti-infective agents are needed. Since important roles in bacterial pathogenesis have been demonstrated for the collagenase H and G (ColH and ColG)… read more here.
Keywords: bacillary collagenases; discovery characterization; clostridial bacillary; synthesized fda ... See more keywords
Discovery, Characterization, and Engineering of LvIC, an α4/4-Conotoxin That Selectively Blocks Rat α6/α3β4 Nicotinic Acetylcholine Receptors.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01786
Abstract: α6β4 nicotinic acetylcholine receptors (nAChRs) are expressed in the central and peripheral nervous systems, but their functions are not fully understood, largely because of a lack of specific ligands. Here, we characterized a novel α-conotoxin,… read more here.
Keywords: discovery characterization; acetylcholine receptors; nicotinic acetylcholine; lvic ... See more keywords
Discovery and Characterization of the Potent and Highly Selective (Piperidin-4-yl)pyrido[3,2- d]pyrimidine Based in Vitro Probe BAY-885 for the Kinase ERK5.
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01606
Abstract: The availability of a chemical probe to study the role of a specific domain of a protein in a concentration- and time-dependent manner is of high value. Herein, we report the identification of a highly… read more here.
Keywords: bay 885; probe; potent highly; characterization potent ... See more keywords