Development of potent and selective inhibitors targeting the papain-like protease of SARS-CoV-2
Sign Up to like & getrecommendations! Published in 2021 at "Cell Chemical Biology"
DOI: 10.1016/j.chembiol.2021.04.020
Abstract: The COVID-19 pandemic has been disastrous to society and effective drugs are urgent needed. The papain-like protease domain (PLpro) of SARS-CoV-2 (SCoV2) is indispensable for viral replication and represents a putative target for pharmacological intervention.… read more here.
Keywords: development potent; potent selective; like protease; papain like ... See more keywords
Development of Potent Nanosized Isatin-isonicotinohydrazide Hybrid for Management of Mycobacterium Tuberculosis.
Sign Up to like & getrecommendations! Published in 2021 at "International journal of pharmaceutics"
DOI: 10.1016/j.ijpharm.2021.121369
Abstract: Inspired by the antitubercular activity of isoniazid (INH) and 5-bromoisatin, isatin-INH hybrid (WF-208) has been synthesized as a potent agent against multidrug-resistant (MDR) and extensively drug-resistant (XDR) strains of M. tuberculosis. In silico molecular docking… read more here.
Keywords: development potent; potent nanosized; tuberculosis; compound ... See more keywords
Development of Potent Immune Modulators Targeting Stimulator of Interferon Genes Receptor.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01795
Abstract: Stimulator of interferon genes (STING) is an endoplasmic reticulum-membrane protein that plays important roles in cancer immunotherapy by activating innate immune responses. We designed and synthesized STING modulators and characterized compounds 4a and 4c that… read more here.
Keywords: development potent; potent immune; stimulator interferon; interferon ... See more keywords
Development of Potent and Selective Antagonists for the UTP-Activated P2Y4 Receptor.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b00030
Abstract: P2Y4 is a Gq protein-coupled receptor activated by uridine-5'-triphosphate (UTP), which is widely expressed in the body, e.g., in intestine, heart, and brain. No selective P2Y4 receptor antagonist has been described so far. Therefore, we… read more here.
Keywords: receptor; development potent; potent selective; p2y4 receptor ... See more keywords
Development of Potent and Selective Janus Kinase 2/3 Directing PG-PROTACs.
Sign Up to like & getrecommendations! Published in 2022 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.1c00650
Abstract: Aberrant activation of the JAK-STAT signaling pathway has been implicated in the pathogenesis of a range of hematological malignancies and autoimmune disorders. Here we describe the design, synthesis, and characterization of JAK2/3 PROTACs utilizing a… read more here.
Keywords: protacs; kinase directing; selective janus; development potent ... See more keywords
Osteocytes regulate neutrophil development through IL-19: A potent cytokine for neutropenia treatment.
Sign Up to like & getrecommendations! Published in 2021 at "Blood"
DOI: 10.1182/blood.2020007731
Abstract: Osteocytes are the most abundant (90-95%) cells in bone and have emerged as an important regulator of hematopoiesis, but their role in neutrophil development and the underlying mechanisms remain unclear. Interleukin (IL)-19 produced predominantly by… read more here.
Keywords: development potent; potent cytokine; neutropenia treatment; neutrophil development ... See more keywords
Development of potent reversible selective inhibitors of butyrylcholinesterase as fluorescent probes
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.2210/pdb6rua/pdb
Abstract: Brain butyrylcholinesterase (BChE) is an attractive target for drugs designed for the treatment of Alzheimer’s disease (AD) in its advanced stages. It also potentially represents a biomarker for pr... read more here.
Keywords: development potent; selective inhibitors; potent reversible; inhibitors butyrylcholinesterase ... See more keywords