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| 1 | Ganglioside GD3 synthase(GD3S),a novel cancer drug target显示文摘Gangliosides are a class of important glycosphingolipids containing sialic acid that are widely distributed on the outer surface of cells and are abundantly distributed in brain tissue. Disialoganglioside with three glycosyl groups(GD3) and disialoganglioside with two glycosyl groups(GD2) are markedly increased in pathological conditions such as cancers and neurodegenerative diseases. GD3 and GD2 were found to play important roles in cancers by mediating cell proliferation, migration, invasion, adhesion,angiogenesis and in preventing immunosuppression of tumors. GD3 synthase(GD3S) is the regulatory enzyme of GD3 and GD2 synthesis, and is important in tumorigenesis and the development of cancers.The study of GD3S as a drug target may be of great significance for the discovery of new drugs for cancer treatment. This review will describe the gangliosides and their roles in physiological and pathological conditions; the roles of GD3 and GD2 in cancers; the expression, functions and mechanisms of GD3S,and its potential as a drug target in cancers. | Jinyi Liu Xiangjin Zheng Xiaocong Pang Li Li Jinhua Wang Cui Yang Guanhua Du | 2018 | Acta Pharmaceutica Sinica B2018，8，5： | 4 |
| 2 | Pharmacokinetic study of gallocatechin-7-gallate from Pithecellobium clypearia Benth. in rats显示文摘The pharmacokinetic profile of gallocatechin-7-gallate(J10688)was studied in rats after intravenous administration.Male and female Sprague-Dawley(SD)rats received 1,3,and 10 mg/kg(i.v.)of J10688 and plasma drug concentrations were determined by a high performance liquid chromatography-mass spectrometry(LC–MS)method.The pharmacokinetic software Data Analysis System(Version 3.0)was used to calculate the pharmacokinetic parameters.For different i.v.doses of J10688,the mean peak plasma concentration(C_0)values ranged from 11.26 to 50.82 mg/L,and mean area under the concentration-time curve(AUC_(0–t))values ranged from 1.75 to 11.80(mg h/L).J10688 lacked dosedependent pharmacokinetic properties within doses between 1 and 10 mg/kg,based on the power model.The method developed in this study was sensitive,precise,and stable.The pharmacokinetic properties of J10688 in SD rats were shown to have rapid distribution and clearance values.These pharmacokinetic results may contribute to an improved understanding of the pharmacological actions of J10688. | Chao Li Xiaowei Song Junke Song Xiaocong Pang Zhe Wang Ying Zhao Wenwen Lian Ailin Liu Guanhua Du | 2016 | Acta Pharmaceutica Sinica B2016，6，1： | 4 |
| 3 | Targeting integrin pathways:mechanisms and advances in therapy显示文摘Integrins are considered the main cell-adhesion transmembrane receptors that play multifaceted roles as extracellular matrix(ECM)-cytoskeletal linkers and transducers in biochemical and mechanical signals between cells and their environment in a wide range of states in health and diseases.Integrin functions are dependable on a delicate balance between active and inactive status via multiple mechanisms,including protein-protein interactions,conformational changes,and trafficking.Due to their exposure on the cell surface and sensitivity to the molecular blockade,integrins have been investigated as pharmacological targets for nearly 40 years,but given the complexity of integrins and sometimes opposite characteristics,targeting integrin therapeutics has been a challenge.To date,only seven drugs targeting integrins have been successfully marketed,including abciximab,eptifibatide,tirofiban,natalizumab,vedolizumab,lifitegrast,and carotegrast.Currently,there are approximately 90 kinds of integrin-based therapeutic drugs or imaging agents in clinical studies,including small molecules,antibodies,synthetic mimic peptides,antibody-drug conjugates(ADCs),chimeric antigen receptor(CAR)T-cell therapy,imaging agents,etc.A serious lesson from past integrin drug discovery and research efforts is that successes rely on both a deep understanding of integrin-regulatory mechanisms and unmet clinical needs.Herein,we provide a systematic and complete review of all integrin family members and integrin-mediated downstream signal transduction to highlight ongoing efforts to develop new therapies/diagnoses from bench to clinic.In addition,we further discuss the trend of drug development,how to improve the success rate of clinical trials targeting integrin therapies,and the key points for clinical research,basic research,and translational research. | Xiaocong Pang Xu He Zhiwei Qiu Hanxu Zhang Ran Xie Zhiyan Liu Yanlun Gu Nan Zhao Qian Xiang Yimin Cui | 2023 | Signal Transduction and Targeted Therapy2023，8，2： | 3 |
| 4 | Recombinant human ACE2: potential therapeutics of SARS-CoV-2 infection and its complication显示文摘Dear Editor,Since December 2019,severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)has caused a pneumonia outbreak in Wuhan city,China,followed by global spread[1,2].As of 9 April,2020,millions of confirmed cases of SARS-CoV-2 infection have been reported,and the global death toll of SARS-CoV-2 infection has surged to tens of thousands of victims,making it a public health emergency of international concern(PHEIC).However,no specific antiviral drug or vaccine for SARS-CoV-2 treatment exists.The high infectivity and the increasing fatality of SARS-CoV-2 highlight the demand for drug discovery.SARS-CoV-2 is closely related to severe acute respiratory syndrome coronavirus(SARS-CoV)[2].Full-genome sequencing analysis indicated that SARS-CoV-2 shares a high-sequence identity with SARS-CoV[3].The spike protein(S-protein)of coronaviruses interacts with cell receptors to mediate viral entry into target cells[4].Additional evidence suggests that both SARS-CoV and SARS-CoV-2 employ angiotensin-converting enzyme 2(ACE2)as the entry receptor and that the receptor-binding domain(RBD)of the S-protein directly binds to ACE2,triggering endocytosis of virus particles[5,6,7].A recent study suggested that the binding affinity between ACE2 and the RBD of SARS-CoV-2 is 10–20 times stronger than that with the RBD of SARS-CoV[5],which likely explains the increased infectivity of SARS-CoV-2. | Xiaocong Pang Yimin Cui Yizhun Zhu | 2020 | Acta Pharmacologica Sinica2020，41，9： | 0 |
| 5 | Discovery of C19-9 as a novel non-RGD inhibitor of αvβ3 to overcome enzalutamide resistance in castration-resistant prostate cancer显示文摘Dear Editor,The integrinαvβ3 receptor is a promising target for anticancer therapy.1,2 However,there are no effective marketed treatments targetingαvβ3.One possible limitation of Arginine-Glycine-Aspartic(RGD)-mimeticαvβ3 antagonists has been shown to cause partial agonism,which could induce major conformational changes that trigger paradoxical cell adhesion and angiogenesis. | Xiaocong Pang Xiaojiao Sun Yanlun Gu Xu He Kan Gong Song Song Jixin Zhang Jie Xia Zhenming Liu Yimin Cui | 2023 | Signal Transduction and Targeted Therapy2023，8，3： | 0 |
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