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Author

Yuanwei Chen

Other affiliations: Chinese Academy of Sciences
Bio: Yuanwei Chen is an academic researcher from Sichuan University. The author has contributed to research in topics: Enzalutamide & Androgen receptor. The author has an hindex of 14, co-authored 40 publications receiving 676 citations. Previous affiliations of Yuanwei Chen include Chinese Academy of Sciences.

Papers
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Journal ArticleDOI
TL;DR: The preliminary data suggests that PROTAC-oriented CDK2/9 degradation is potentially an effective therapeutic approach.

61 citations

Journal ArticleDOI
TL;DR: EGT1442 showed favorable properties both in vitro and in vivo and could be beneficial to the management of type 2 diabetic patients and could help to promote normalization of blood glucose without hypoglycemia in the setting of type 1 diabetes.

59 citations

Patent
22 Aug 2008
TL;DR: In this paper, compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT are provided. And the authors also provide pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by sGLT inhibition.
Abstract: Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

57 citations

Patent
22 May 2007
TL;DR: In this article, compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT are provided. And the authors also provide pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by sGLT inhibition.
Abstract: Provided are compounds having an inhibitory effect on sodium-dependent glucose cotransporter SGLT. The invention also provides pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions which are affected by SGLT inhibition.

57 citations

Journal ArticleDOI
TL;DR: S GLT2 inhibitors deuterated at sites susceptible to oxidative metabolism were found to have a slightly longer tmax and half-life, dose-dependent increase in urinary glucose excretion in rats, and slightly superior effects on UGE in dogs while retaining similar in vitro inhibitory activities against hSGLT2.
Abstract: SGLT2 inhibitors deuterated at sites susceptible to oxidative metabolism were found to have a slightly longer tmax and half-life (t1/2), dose-dependent increase in urinary glucose excretion (UGE) in rats, and slightly superior effects on UGE in dogs while retaining similar in vitro inhibitory activities against hSGLT2. In particular, deuterated compound 41 has the potential to be a robust long-acting antidiabetic agent.

56 citations


Cited by
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Journal ArticleDOI
TL;DR: A personal review of advances in the genetics, molecular biology, biochemistry, biophysics, and structure of SGLTs, including cotransporters for sugars, anions, vitamins, and short-chain fatty acids.
Abstract: There are two classes of glucose transporters involved in glucose homeostasis in the body, the facilitated transporters or uniporters (GLUTs) and the active transporters or symporters (SGLTs). The ...

1,082 citations

DOI
20 Sep 2000
TL;DR: Thiazolidinediones(TDs)是一类新型的胰岛素抵抗治疗药物动物及临床实验证实TDs通过激活核受体过氧化物酶体增
Abstract: Thiazolidinediones(TDs)是一类新型的胰岛素抵抗治疗药物。动物及临床实验证实TDs通过激活核受体过氧化物酶体增殖物激活受体-γ(PPAR-γ)显著增加胰岛素敏感性,改善胰岛β-细胞功能,降低血糖和胰岛素水平,缓解高血压及脂代谢紊乱,对2型糖尿病大血管和微血管病变亦具有保护作用。临床使用耐受性好,低血糖发生率低。但其中的Troglitazone具有明显的肝脏毒性。

688 citations

Journal ArticleDOI
TL;DR: The next few years will be critical for NP-driven lead discovery, and a concerted effort is required to identify new biologically active pharmacophores and to progress these and existing compounds through pre-clinical drug development into clinical trials.

456 citations

Journal ArticleDOI
TL;DR: Advances in the application of hydrogen isotopes in the life sciences are described and 3 H, in particular, has seen an increase in utilization, especially in pharmaceutical drug discovery.
Abstract: Hydrogen isotopes are unique tools for identifying and understanding biological and chemical processes. Hydrogen isotope labelling allows for the traceless and direct incorporation of an additional mass or radioactive tag into an organic molecule with almost no changes in its chemical structure, physical properties, or biological activity. Using deuterium-labelled isotopologues to study the unique mass-spectrometric patterns generated from mixtures of biologically relevant molecules drastically simplifies analysis. Such methods are now providing unprecedented levels of insight in a wide and continuously growing range of applications in the life sciences and beyond. Tritium (3 H), in particular, has seen an increase in utilization, especially in pharmaceutical drug discovery. The efforts and costs associated with the synthesis of labelled compounds are more than compensated for by the enhanced molecular sensitivity during analysis and the high reliability of the data obtained. In this Review, advances in the application of hydrogen isotopes in the life sciences are described.

394 citations

Journal ArticleDOI
TL;DR: This Perspective provides an overview of the recent developments of deuteration, with a focus on deuterated clinical candidates, and highlights both opportunities and challenges of this strategy.
Abstract: The use of deuteration in medicinal chemistry has exploded in the past years, and the FDA has recently approved the first deuterium-labeled drug. Precision deuteration goes beyond the pure and simple amelioration of the pharmacokinetic parameters of a drug and might provide an opportunity when facing problems in terms of metabolism-mediated toxicity, drug interactions, and low bioactivation. The use of deuterium is even broader, offering the opportunity to lower the degree of epimerization, reduce the dose of coadministered boosters, and discover compounds where deuterium is the basis for the mechanism of action. Nevertheless, designing, synthesizing, and developing a successful deuterated drug is far from straightforward, and the translation from concept to practice is often unpredictable. This Perspective provides an overview of the recent developments of deuteration, with a focus on deuterated clinical candidates, and highlights both opportunities and challenges of this strategy.

341 citations