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Discovery of small molecule degraders for modulating cell cycle

Frontiers of Medicine   Pages 823-854 doi: 10.1007/s11684-023-1027-5

Abstract: The cell cycle is a complex process that involves DNA replication, protein expression, and cell division. Dysregulation of the cell cycle is associated with various diseases. Cyclin-dependent kinases (CDKs) and their corresponding cyclins are major proteins that regulate the cell cycle. In contrast to inhibition, a new approach called proteolysis-targeting chimeras (PROTACs) and molecular glues can eliminate both enzymatic and scaffold functions of CDKs and cyclins, achieving targeted degradation. The field of PROTACs and molecular glues has developed rapidly in recent years. In this article, we aim to summarize the latest developments of CDKs and cyclin protein degraders. The selectivity, application, validation and the current state of each CDK degrader will be overviewed. Additionally, possible methods are discussed for the development of degraders for CDK members that still lack them. Overall, this article provides a comprehensive summary of the latest advancements in CDK and cyclin protein degraders, which will be helpful for researchers working on this topic.

Keywords: PROTAC     molecular glue     degrader     cell cycle     CDK     cyclin    

Near-infrared benzodiazoles as small molecule environmentally-sensitive fluorophores

Frontiers of Chemical Science and Engineering 2022, Volume 16, Issue 1,   Pages 128-135 doi: 10.1007/s11705-021-2080-8

Abstract: The development of fluorophores emitting in the near-infrared spectral window has gained increased attention given their suitable features for biological imaging. In this work, we have optimised a general and straightforward synthetic approach to prepare a small library of near-infrared-emitting C-bridged nitrobenzodiazoles using commercial precursors. C-bridged benzodiazoles have low molecular weight and neutral character as important features that are not common in most near-infrared dyes. We have investigated their fluorescence response in the presence of a wide array of 60 different biomolecules and identified compound 3i as a potential chemosensor to discriminate between Fe2+ and Fe3+ ions in aqueous media.

Keywords: fluorescence     probes     iron     screening     library    

Recent advances of small-molecule fluorescent probes for detecting biological hydrogen sulfide

Frontiers of Chemical Science and Engineering 2022, Volume 16, Issue 1,   Pages 34-63 doi: 10.1007/s11705-021-2050-1

Abstract: It was recently revealed that H2S is also an endogenous signaling molecule that has important

Keywords: hydrogen sulfide     fluorescent probe     reducibility     nucleophilicity     copper sulfide precipitate     hydrogen polysulfides    

A pseudocapacitive molecule-induced strategy to construct flexible high-performance asymmetric supercapacitors

Frontiers of Chemical Science and Engineering 2023, Volume 17, Issue 9,   Pages 1208-1220 doi: 10.1007/s11705-023-2304-1

Abstract: we present an “advantage-complementary strategy” using sodium lignosulfonate as a pseudocapacitive molecule

Keywords: molecular synergy     pseudocapacitive lignosulfonate     flexible electronic devices     asymmetric supercapacitor     wide voltage windows    

Genetic biosensors for small-molecule products: Design and applications in high-throughput screening

Qingzhuo Wang,Shuang-Yan Tang,Sheng Yang

Frontiers of Chemical Science and Engineering 2017, Volume 11, Issue 1,   Pages 15-26 doi: 10.1007/s11705-017-1629-z

Abstract: Overproduction of small-molecule chemicals using engineered microbial cells has greatly reduced the productionSuch biosensors allow a high-throughput screening of the small-molecule products, and can be roughlyThis review summarizes the recent developments in the design and applications of biosensors for small-molecule

Keywords: biosensor     small molecule product     transcription factor     riboswitch     high-throughput screening    

Calculation of collision frequency function for aerosol particles in free molecule regime in presence

Xiaowei LUO, Yannick BENICHOU, Suyuan YU

Frontiers in Energy 2013, Volume 7, Issue 4,   Pages 506-510 doi: 10.1007/s11708-013-0275-5

Abstract: The collision frequency function for aerosol particles has already been calculated for the free moleculecollision frequency in the case of particles much smaller than the mean free path of the gas (free molecule

Keywords: aerosol particles     collision frequency function     coagulation    

Development of small-molecule viral inhibitors targeting various stages of the life cycle of emerging

Xiaohuan Wang, Peng Zou, Fan Wu, Lu Lu, Shibo Jiang

Frontiers of Medicine 2017, Volume 11, Issue 4,   Pages 449-461 doi: 10.1007/s11684-017-0589-5

Abstract: In this review, we summarize and discuss the latest progress in the development of small-molecule viralWe also discuss some general strategies for developing small-molecule viral inhibitors.

Keywords: emerging and re-emerging viruses     small-molecule inhibitor     coronavirus     Ebola virus     Zika virus     life cycle    

Small-molecule anti-COVID-19 drugs and a focus on China’s homegrown mindeudesivir (VV116)

Frontiers of Medicine doi: 10.1007/s11684-023-1037-3

Abstract: So far, a few small-molecule antiviral drugs, including nirmatrelvir–ritonavir (Paxlovid), remdesivirregarding the pharmacological mechanism and therapeutic effects focusing on mindeudesivir and other small-molecule

Keywords: COVID-19     antiviral drugs     mindeudesivir    

Design of nanocarriers for efficient cellular uptake and endosomal release of small molecule and nucleic

Vaibhav Mundra, Ram I. Mahato

Frontiers of Chemical Science and Engineering 2014, Volume 8, Issue 4,   Pages 387-404 doi: 10.1007/s11705-014-1457-3

Abstract: There are many challenges in developing efficient and target specific delivery systems of small molecule

Keywords: nanocarrier     cellular uptake     endosomal release     nucleic acid drug    

Calculation of Bond-length, Bond-energy and Force Constant of Hydrogen Molecule by Classical Mechanics

Chen Jing

Strategic Study of CAE 2003, Volume 5, Issue 6,   Pages 39-43

Abstract: belong in fact, to statistic regularity, and imply a macro-time scale is used, therefore in hydrogen moleculeBased on the overlap of electron cloud, the ground state hydrogen molecule structural parameters arecalculated with the classical mechanics, and the hydrogen molecule bond-length Re, bonding-energyIn this calculation, hydrogen molecule chemical bonding model is concise and has clear physical meaning

Keywords: hydrogen molecule     bond-length     bond-energy     force constant    

A small-molecule pan-HER inhibitor alone or in combination with cisplatin exerts efficacy against nasopharyngeal

Frontiers of Medicine 2023, Volume 17, Issue 2,   Pages 275-289 doi: 10.1007/s11684-022-0945-y

Abstract: The abnormal activation of HER family kinase activity is closely related to the development of human malignancies. In this study, we used HER kinases as targets for the treatment of nasopharyngeal carcinoma (NPC) and explored the anti-tumor effects of the novel pan-HER inhibitor HM781-36B, alone or in combination with cisplatin. We found that HER family proteins were positively expressed in tumor tissues of some NPC patients, and the high levels of those proteins were significantly related to poor prognosis. HM781-36B inhibited NPC in vitro and in vivo. HM781-36B exerted synergistic effects with cisplatin on inhibiting proliferation and promoting apoptosis of NPC cells. In NPC xenograft models in nude mice, HM781-36B and cisplatin synergistically inhibited tumor growth. Downregulating the activity of HER family proteins and their downstream signaling pathways and regulating tumor microenvironment may explain the synergistic anti-tumor effects of HM781-36B and cisplatin. In conclusion, our study provides evidence for HER family proteins as prognostic biomarkers and potential therapeutic targets for NPC. The pan-HER inhibitor HM781-36B alone or in combination with cisplatin represents promising therapeutic effects for the treatment of NPC patients, which provides a new idea for the comprehensive treatment of NPC.

Keywords: epidermal growth factor receptor     ErbB receptors     HM781-36B     nasopharyngeal carcinoma     molecular targeted therapy     cisplatin    

Bright future of polymerizing small-molecule acceptors in realizing high performance all-polymer solar

Qi Chen1 , Cen Zhang1 , Lingwei Xue1,2 , Zhi-Guo Zhang1

Frontiers of Chemical Science and Engineering 2022, Volume 16, Issue 10,   Pages 1526-1529 doi: 10.1007/s11705-022-2161-3

Recent advances in small molecule fluorescent probes for simultaneous imaging of two bioactive molecules

Yongqing Zhou, Xin Wang, Wei Zhang, Bo Tang, Ping Li

Frontiers of Chemical Science and Engineering 2022, Volume 16, Issue 1,   Pages 4-33 doi: 10.1007/s11705-021-2041-2

Abstract: Single organic molecule fluorescent probes have been successively developed to simultaneously monitor

Keywords: bioactive molecules     fluorescent probes     in living cells and in vivo     review    

Single-Molecule Methods for Characterizing Different DNA Higher-Order Structures Review

Yonglin Liu, Tianyuan Bian, Yan Liu, Zhimin Li, Yufeng Pei, Jie Song

Engineering 2023, Volume 24, Issue 5,   Pages 277-292 doi: 10.1016/j.eng.2022.10.009

Abstract: Single-molecule methods are powerful tools for observing the behavior of individual molecules and probingIn this review, we introduce single-molecule methods, including single-molecule detection and manipulationWe conclude by providing a new perspective on the combination of DNA nanotechnology and single-molecule

Keywords: Single-molecule methods     DNA structure     Mechanical properties     Conformational transitions    

ECRG4: a new potential target in precision medicine

Xin Qin, Ping Zhang

Frontiers of Medicine 2019, Volume 13, Issue 5,   Pages 540-546 doi: 10.1007/s11684-018-0637-9

Abstract: 4 ( ), which is initially known as a new candidate tumor suppressor gene, is emerging as a sentinel molecule

Keywords: ECRG4     tumor suppressor gene     sentinel molecule     precision medicine     cell senescence     epithelium homeostasis    

Title Author Date Type Operation

Discovery of small molecule degraders for modulating cell cycle

Journal Article

Near-infrared benzodiazoles as small molecule environmentally-sensitive fluorophores

Journal Article

Recent advances of small-molecule fluorescent probes for detecting biological hydrogen sulfide

Journal Article

A pseudocapacitive molecule-induced strategy to construct flexible high-performance asymmetric supercapacitors

Journal Article

Genetic biosensors for small-molecule products: Design and applications in high-throughput screening

Qingzhuo Wang,Shuang-Yan Tang,Sheng Yang

Journal Article

Calculation of collision frequency function for aerosol particles in free molecule regime in presence

Xiaowei LUO, Yannick BENICHOU, Suyuan YU

Journal Article

Development of small-molecule viral inhibitors targeting various stages of the life cycle of emerging

Xiaohuan Wang, Peng Zou, Fan Wu, Lu Lu, Shibo Jiang

Journal Article

Small-molecule anti-COVID-19 drugs and a focus on China’s homegrown mindeudesivir (VV116)

Journal Article

Design of nanocarriers for efficient cellular uptake and endosomal release of small molecule and nucleic

Vaibhav Mundra, Ram I. Mahato

Journal Article

Calculation of Bond-length, Bond-energy and Force Constant of Hydrogen Molecule by Classical Mechanics

Chen Jing

Journal Article

A small-molecule pan-HER inhibitor alone or in combination with cisplatin exerts efficacy against nasopharyngeal

Journal Article

Bright future of polymerizing small-molecule acceptors in realizing high performance all-polymer solar

Qi Chen1 , Cen Zhang1 , Lingwei Xue1,2 , Zhi-Guo Zhang1

Journal Article

Recent advances in small molecule fluorescent probes for simultaneous imaging of two bioactive molecules

Yongqing Zhou, Xin Wang, Wei Zhang, Bo Tang, Ping Li

Journal Article

Single-Molecule Methods for Characterizing Different DNA Higher-Order Structures

Yonglin Liu, Tianyuan Bian, Yan Liu, Zhimin Li, Yufeng Pei, Jie Song

Journal Article

ECRG4: a new potential target in precision medicine

Xin Qin, Ping Zhang

Journal Article