Lei Tian

Dr. Lei Tian

orcid

Research Focus & Metrics

Academic Career Length

7Years (2020-Present)

(Calculated once Scilit publication data is synced: current year − year of first publication + 1)

Representative Publications

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13 February 2023 in Molecules
Verified
Journal Article
Open access
PDF file
ZSZhenfeng Shi
Zhenfeng Shi
JZJie Zhang
Jie Zhang
LTLei Tian
Lei Tian
LXLiang Xin
Liang Xin
Chengyuan LiangChengyuan Liang
Chengyuan Liang
MLMin Li
Min Li
Due to the overuse of antibiotics, bacterial resistance has markedly increased to become a global problem and a major threat to human health. Fortunately, in recent years, various new antibiotics have been developed through both improvements to traditional antibiotics and the discovery of antibiotics with novel mechanisms with the aim of addressing the decrease in the efficacy of traditional antibiotics. This manuscript reviews the antibiotics that have been approved for marketing in the last 20 years with an emphasis on the antibacterial properties, mechanisms, structure–activity relationships (SARs), and clinical safety of these antibiotics. Furthermore, the current deficiencies, opportunities for improvement, and prospects of antibiotics are thoroughly discussed to provide new insights for the design and development of safer and more potent antibiotics.

8 February 2021 in Organic Chemistry Frontiers
Verified
Journal Article
Closed access
PDF file
JNJiang Nan*
Jiang Nan*
QMQiong Ma
Qiong Ma
JYJiacheng Yin
Jiacheng Yin
Chengyuan LiangChengyuan Liang
Chengyuan Liang
LTLei Tian
Lei Tian
YMYangmin Ma
Yangmin Ma
A rhodium(III)-catalyzed formal C–H [5 + 1] cyclization of 2-pyrrolyl/indolylanilines with vinylene carbonate has been explored towards the potent assembly of diverse 4-methylpyrrolo[1,2-a]quinoxalines. This established protocol is characterized by an exceedingly simple reaction system, and excellent functional group toleration and yields. Most importantly, entirely distinct from documented [4 + 2] cyclization conversions, herein, the emerging vinylene carbonate firstly presents as a C1 synthon to realize [5 + 1] annulation and shows new chemical reactivity. Biological studies indicate that these prepared products are promising candidates in terms of their antibacterial activity.

16 September 2022 in Biomedicine & Pharmacotherapy
Verified
Journal Article
Open access
ZSZhenfeng Shi
Zhenfeng Shi
JLJifang Liu
Jifang Liu
LTLei Tian
Lei Tian
JLJingyi Li
Jingyi Li
YGYue Gao
Yue Gao
Chengyuan LiangChengyuan Liang
Chengyuan Liang
Due to the complexity and particularity of cancer cell microenvironments, redox responsive drug delivery systems (DDSs) for cancer therapy have been extensively explored. Compared with widely reported cancer treatment systems based on disulfide bonds, diselenide bonds have better redox properties and greater anticancer efficiency. In this review, the significance and application of diselenide bonds in DDSs are summarized, and the stimulation sensitivity of diselenide bonds is comprehensively reported. The potential and prospects for the application of diselenide bonds in next-generation anticancer drug treatment systems are extensively discussed.

1 April 2022 in Biomedicine & Pharmacotherapy
Verified
Journal Article
Open access
JXJuan Xia
Juan Xia
NHNan Hui
Nan Hui
LTLei Tian
Lei Tian
Chengyuan LiangChengyuan Liang
Chengyuan Liang
JZJie Zhang
Jie Zhang
KWKun Wang
Kun Wang
In recent years, with improvements in treatments for heart failure (HF), the survival period of patients has been extended. However, the emergence of some patients with repeated hospitalizations due to their worsening conditions and low survival rates followed. Currently, few drugs are available for such patients. Vericiguat was first drug approved for the treatment of symptomatic patients with chronic HF with reduced ejection fraction (HFrEF) to reduce the occurrence of worsening HF. This article provides comprehensive information about vericiguat in terms of drug design and development, structure-activity relationship (SAR), synthesis, pharmacological efficacy, and clinical practice. In addition, insights into the current vericiguat trials and treatments of HF are also discussed.

3 August 2022 in Molecules
Verified
Journal Article
Open access
PDF file
CSChunyang Shi
Chunyang Shi
YMYangmin Ma
Yangmin Ma
LTLei Tian
Lei Tian
JLJingyi Li
Jingyi Li
GQGuaiping Qiao
Guaiping Qiao
Chengyuan LiangChengyuan Liang
Chengyuan Liang
Inappropriate and disproportionate antibiotic use contributes immensely to the development of antibiotic resistance in bacterial species associated with food contamination. Therefore, alternative strategies to treat multidrug-resistant (MDR) bacterial infections are urgently needed. In this study, verbascoside was shown to exhibit excellent antibacterial activity and synergistic effects in combination with cell wall synthesis-inhibiting antibiotics, indicating that it can be used as an adjuvant to restore or increase the activity of antibiotics against resistant pathogens. In a mechanistic study, higher concentrations of verbascoside resulted in a longer lag phase and a lower specific exponential-phase growth rate of bacteria. Furthermore, verbascoside exerted its antimicrobial activity through multiple mechanisms, including cell membrane dysfunction, biofilm eradication and changes in cell morphology. The promising antibacterial activity and in vitro safety assessment results suggested that verbascoside can be used as a food additive for fresh meat preservation. Treatment with medium and high doses of verbascoside caused significant bacterial death in meat samples, slowed the spoilage rate, and extended the shelf life. Collectively, verbascoside is expected to be useful as an antibiotic adjuvant to prevent or treat resistant bacteria-related infections and an alternative novel antimicrobial additive in the food industry.

22 March 2026 in ChemMedChem
Verified
Journal Article
Open access
PDF file
CTChao Tang
Chao Tang
BTBin Tian
Bin Tian
BZBingxing Zhang
Bingxing Zhang
YZYunfei Zhang
Yunfei Zhang
CKChanghua Ke
Changhua Ke
LTLei Tian
Lei Tian
Vepdegestrant (ARV‐471) is an orally bioavailable, proteolysis‐targeting chimera (PROTAC)‐based estrogen receptor (ER) degrader and is among the most clinically advanced ER‐targeting PROTAC degraders, identified through a rational medicinal chemistry optimization campaign. It is being developed as an oral small‐molecule endocrine therapy for advanced or metastatic ER‐positive, human epidermal growth factor receptor 2 (HER2)‐negative breast cancer, with particular relevance for tumors harboring ESR1 mutations. On June 6, 2025, Arvinas and Pfizer submitted a New Drug Application (NDA) for vepdegestrant to the U.S. Food and Drug Administration (FDA), representing an important step in the clinical translation of PROTAC technology. This review summarizes the design, synthesis, degradation mechanism, preclinical pharmacology, and clinical development of vepdegestrant and discusses the broader implications and future prospects of oral PROTAC‐based ER degraders in breast cancer therapy.