Search Results - "Lv, Binhua"
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A Phase I, Randomized, Double-Blind, Placebo-Controlled, Single Ascending Dose, Multiple Ascending Dose and Food Effect Study to Evaluate the Tolerance, Pharmacokinetics of Jaktinib, a New Selective Janus Kinase Inhibitor in Healthy Chinese Volunteers
Published in Frontiers in pharmacology (14-12-2020)“…Jaktinib is a novel selective janus kinase 1/2 inhibitor. The phase I first-in-human study evaluated the tolerance and pharmacokinetics of jaktinib in healthy…”
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A novel anti-LAG-3/TIGIT bispecific antibody exhibits potent anti-tumor efficacy in mouse models as monotherapy or in combination with PD-1 antibody
Published in Scientific reports (09-05-2024)“…We report the generation of a novel anti-LAG-3/TIGIT bispecific IgG4 antibody, ZGGS15, and evaluated its anti-tumor efficacy in mouse models as monotherapy or…”
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Design, Synthesis, and Biological Evaluation of Deuterated C‑Aryl Glycoside as a Potent and Long-Acting Renal Sodium-Dependent Glucose Cotransporter 2 Inhibitor for the Treatment of Type 2 Diabetes
Published in Journal of medicinal chemistry (27-02-2014)“…SGLT2 inhibitors deuterated at sites susceptible to oxidative metabolism were found to have a slightly longer t max and half-life (t 1/2), dose-dependent…”
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Study on Typical Diarylurea Drugs or Derivatives in Cocrystallizing with Strong H‑Bond Acceptor DMSO
Published in ACS omega (02-03-2021)“…Diarylureas are widely used in self-assembly and supramolecular chemistry owing to their outstanding characteristics as both H-bond donors and acceptors…”
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Exploration of O-spiroketal C-arylglucosides as novel and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors
Published in Bioorganic & medicinal chemistry letters (15-12-2009)“…The novel spiro[isobenzofuran-1,2′-pyran] structure is proved to be an effective scaffold for diversification of SGLT2 inhibitors and a number of compounds…”
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C-Aryl glucosides substituted at the 4′-position as potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes
Published in Bioorganic & medicinal chemistry letters (01-08-2011)“…A series of C-aryl glucosides with various substituents at the 4′-position of the distal aryl ring have been synthesized and evaluated for inhibition of hSGLT1…”
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O-Spiro C-aryl glucosides as novel sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors
Published in Bioorganic & medicinal chemistry letters (01-10-2009)“…Two series of O-spiro C-aryl glucosides have been synthesized and evaluated for inhibition of hSGLT1 and hSGLT2. Two series of O-spiro C-aryl glucosides were…”
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ortho-Substituted C-aryl glucosides as highly potent and selective renal sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors
Published in Bioorganic & medicinal chemistry (15-06-2010)“…A series of ortho-substituted C-aryl glucosides have been synthesized and evaluated for inhibition of hSGLT1 and hSGLT2. A series of 2-substituted C-aryl…”
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Discovery of Potent SOS1 PROTACs with Effective Antitumor Activities against NCI-H358 Tumor Cells In Vitro/In Vivo
Published in Journal of medicinal chemistry (25-01-2024)“…Directly targeted KRAS inhibitors are now facing resistance problems, which might be partially solved by the combination of SOS1 inhibitors with KRAS…”
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ZGGS15, a Novel IgG4 Bispecific Monoclonal Antibody Targeting Both LAG-3 and Tigit, Demonstrates Outstanding Anti-Tumor Activity and Can be Used As Monotherapy or in Combination with Anti-PD-1 Antibodies for Cancer Immunotherapy
Published in Blood (02-11-2023)“…Background This study aims to evaluate the anti-tumor efficacy of ZGGS15, a novel IgG4 bispecific monoclonal antibody (BsAb) targeting TIGIT and LAG-3, for…”
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Abstract 1618: A highly selective and potent TLR8 agonist ZG0895 in preclinical studies of anti-tumor activities
Published in Cancer research (Chicago, Ill.) (04-04-2023)“…Abstract Toll-like receptor 8 (TLR8) recognizes ssRNA fragments from pathogens and initiate both innate and adaptive immune responses. TLR8 activation can…”
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Abstract 2790: Preclinical studies of ZG19018, a novel irreversible covalent inhibitor of KRAS G12C, for the treatment of advanced non-small cell lung cancer and other solid tumors
Published in Cancer research (Chicago, Ill.) (04-04-2023)“…Abstract Growing evidences of covalent irreversible inhibitors in clinical treatments of solid tumors with KRAS G12C mutation have recently emerged after…”
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Abstract 2323: ZGGS18, a bispecific drug candidate of anti-VEGF and TGFbeta-trap, inhibiting tumor proliferation and improving tumor microenvironment with I/O therapy
Published in Cancer research (Chicago, Ill.) (04-04-2023)“…Abstract ZGGS18 is a bifunctional fusion protein targeting both human vascular endothelial growth factor (VEGF) and transforming growth factor-β (TGF-β), which…”
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Abstract 6368: Preclinical pharmacology and safety studies of ZG005: an anti-PD-1/TIGIT bispecific mAb in a phase I clinical trial for advanced tumors
Published in Cancer research (Chicago, Ill.) (04-04-2023)“…Abstract ZG005 is a humanized anti-PD-1/TIGIT bispecific antibody that effectively blocks the binding between PD-1 and TIGIT, on immune cells, with their…”
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EGT1442, a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA(1c) levels in db/db mice and prolongs the survival of stroke-prone rats
Published in Pharmacological research (01-04-2011)“…Sodium glucose co-transporter 2 (SGLT2) is a renal type III integral membrane protein that co-transports sodium and glucose from filtrate to epithelium in the…”
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Conformationally Constrained Spiro C-Arylglucosides as Potent and Selective Renal Sodium-Dependent Glucose Co-transporter 2 (SGLT2) Inhibitors
Published in ChemMedChem (07-06-2010)“…Sodium glucose co‐transporter 2 (SGLT2) is an emerging target for the treatment of type 2 diabetes mellitus (DM2). Here, the synthesis and preliminary…”
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EGT1442, a potent and selective SGLT2 inhibitor, attenuates blood glucose and HbA 1c levels in db/db mice and prolongs the survival of stroke-prone rats
Published in Pharmacological research (2011)“…Sodium glucose co-transporter 2 (SGLT2) is a renal type III integral membrane protein that co-transports sodium and glucose from filtrate to epithelium in the…”
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