LIVIVO - The Search Portal for Life Sciences

zur deutschen Oberfläche wechseln
Advanced search

Search results

Result 1 - 10 of total 29

Search options

  1. Article: Merging Humans and Neuroprosthetics through Regenerative Peripheral Nerve Interfaces.

    Tian, Yucheng / Vaskov, Alex K / Adidharma, Widya / Cederna, Paul S / Kemp, Stephen W P

    Seminars in plastic surgery

    2024  Volume 38, Issue 1, Page(s) 10–18

    Abstract: Limb amputations can be devastating and significantly affect an individual's independence, leading to functional and psychosocial challenges in nearly 2 million people in the United States alone. Over the past decade, robotic devices driven by neural ... ...

    Abstract Limb amputations can be devastating and significantly affect an individual's independence, leading to functional and psychosocial challenges in nearly 2 million people in the United States alone. Over the past decade, robotic devices driven by neural signals such as neuroprostheses have shown great potential to restore the lost function of limbs, allowing amputees to regain movement and sensation. However, current neuroprosthetic interfaces have challenges in both signal quality and long-term stability. To overcome these limitations and work toward creating bionic limbs, the Neuromuscular Laboratory at University of Michigan Plastic Surgery has developed the Regenerative Peripheral Nerve Interface (RPNI). This surgical construct embeds a transected peripheral nerve into a free muscle graft, effectively amplifying small peripheral nerve signals to provide enhanced control signals for a neuroprosthetic limb. Furthermore, the RPNI has the potential to provide sensory feedback to the user and facilitate neuroprosthesis embodiment. This review focuses on the animal studies and clinical trials of the RPNI to recapitulate the promising trajectory toward neurobionics where the boundary between an artificial device and the human body becomes indistinct. This paper also sheds light on the prospects of the improvement and dissemination of the RPNI technology.
    Language English
    Publishing date 2024-02-06
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 2077828-4
    ISSN 1535-2188
    ISSN 1535-2188
    DOI 10.1055/s-0044-1779028
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 4383: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  2. Article ; Online: Drug development and potential targets for Cushing's syndrome.

    Wei, Wei / Xu, Qianqian / Wu, Liuyi / Gong, Guangyue / Tian, Yucheng / Huang, Huidan / Li, Zhiyu

    European journal of medicinal chemistry

    2024  Volume 270, Page(s) 116333

    Abstract: Cushing's syndrome (CS) is a complex disorder characterized by the excessive secretion of cortisol, with Cushing's disease (CD), particularly associated with pituitary tumors, exhibiting heightened morbidity and mortality. Although transsphenoidal ... ...

    Abstract Cushing's syndrome (CS) is a complex disorder characterized by the excessive secretion of cortisol, with Cushing's disease (CD), particularly associated with pituitary tumors, exhibiting heightened morbidity and mortality. Although transsphenoidal pituitary surgery (TSS) stands as the primary treatment for CD, there is a crucial need to optimize patient prognosis. Current medical therapy serves as an adjunctive measure due to its unsatisfactory efficacy and unpredictable side effects. In this comprehensive review, we delve into recent advances in understanding the pathogenesis of CS and explore therapeutic options by conducting a critical analysis of potential drug targets and candidates. Additionally, we provide an overview of the design strategy employed in previously reported candidates, along with a summary of structure-activity relationship (SAR) analyses and their biological efficacy. This review aims to contribute valuable insights to the evolving landscape of CS research, shedding light on potential avenues for therapeutic development.
    MeSH term(s) Humans ; Cushing Syndrome/drug therapy ; Cushing Syndrome/etiology ; Pituitary ACTH Hypersecretion/complications ; Pituitary ACTH Hypersecretion/drug therapy ; Drug Delivery Systems ; Drug Development ; Hydrocortisone/therapeutic use
    Chemical Substances Hydrocortisone (WI4X0X7BPJ)
    Language English
    Publishing date 2024-03-22
    Publishing country France
    Document type Journal Article ; Review
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2024.116333
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.B 784: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  3. Article ; Online: The discovery of potent USP2/USP8 dual-target inhibitors for the treatment of breast cancer via structure guided optimization of ML364.

    Tian, Yucheng / Liu, Kang / Wu, Dongdong / Wu, Liuyi / Xu, Qianqian / Wei, Wei / Li, Zhiyu / Du, Qianming / Bian, Jinlei

    European journal of medicinal chemistry

    2024  Volume 268, Page(s) 116275

    Abstract: USP2 and USP8 are crucial in the development and progression of breast cancer, primarily through the stabilization of protein substrates such as Her2 and ERα. The dual-target inhibitor ML364, targeting both USP2 and USP8, has garnered significant ... ...

    Abstract USP2 and USP8 are crucial in the development and progression of breast cancer, primarily through the stabilization of protein substrates such as Her2 and ERα. The dual-target inhibitor ML364, targeting both USP2 and USP8, has garnered significant interest in recent research. In this study, we developed a series of ML364 derivatives using ligand-based drug design strategies. The standout compound, LLK203, demonstrated enhanced inhibitory activity, showing a 4-fold increase against USP2 and a 9-fold increase against USP8, compared to the parent molecule. In MCF-7 breast cancer cells, LLK203 effectively degraded key proteins involved in cancer progression and notably inhibited cell proliferation. Moreover, LLK203 exhibited potent in vivo efficacy in the 4T1 homograft model, while maintaining a low toxicity profile. These results underscore the potential of LLK203 as a promising dual-target inhibitor of USP2/USP8 for breast cancer treatment.
    MeSH term(s) Humans ; Female ; Breast Neoplasms/drug therapy ; Breast Neoplasms/metabolism ; MCF-7 Cells ; Cell Proliferation ; Ubiquitin Thiolesterase ; Endopeptidases/metabolism ; Endosomal Sorting Complexes Required for Transport/pharmacology
    Chemical Substances USP2 protein, human (EC 3.4.19.12) ; Ubiquitin Thiolesterase (EC 3.4.19.12) ; USP8 protein, human (EC 3.4.19.12) ; Endopeptidases (EC 3.4.-) ; Endosomal Sorting Complexes Required for Transport
    Language English
    Publishing date 2024-02-24
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2024.116275
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.B 784: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  4. Article ; Online: Ultrathin Aerogel Micro/Nanofiber Membranes with Hierarchical Cellular Architecture for High-Performance Warmth Retention.

    Tian, Yucheng / Wang, Sai / Yang, Ming / Liu, Shude / Yu, Jianyong / Zhang, Shichao / Ding, Bin

    ACS nano

    2023  Volume 17, Issue 24, Page(s) 25439–25448

    Abstract: A low temperature environment poses significant challenges to the global economy and public health. However, the existing cold-protective materials still struggle with the trade-off between thickness and thermal resistance, resulting in poor thermal-wet ... ...

    Abstract A low temperature environment poses significant challenges to the global economy and public health. However, the existing cold-protective materials still struggle with the trade-off between thickness and thermal resistance, resulting in poor thermal-wet comfort and limited personal cold protection performance. Here, a scalable strategy, based on electrospinning and solution casting, is developed to create aerogel micro/nanofiber membranes with a hierarchical cellular architecture by manipulating the phase separation of the charged jets and of the spreading casting solution. The integration of interconnected nanopores (30-60 nm), ultrafine fiber diameter, and high porosity, enables the aerogel micro/nanofiber membranes with lightweight, ultrathin thickness (∼0.5 mm), and superior warmth retention performance with ultralow thermal conductivity of 14.01 mW m
    Language English
    Publishing date 2023-12-10
    Publishing country United States
    Document type Journal Article
    ISSN 1936-086X
    ISSN (online) 1936-086X
    DOI 10.1021/acsnano.3c08930
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

    Inter-library loan at ZB MED

    Your chosen title can be delivered directly to ZB MED Cologne location if you are registered as a user at ZB MED Cologne.

  5. Article ; Online: Neuromuscular implants: Interfacing with skeletal muscle for improved clinical translation of prosthetic limbs.

    Quinn, Kiara N / Tian, Yucheng / Budde, Ryan / Irazoqui, Pedro P / Tuffaha, Sami / Thakor, Nitish V

    Muscle & nerve

    2023  Volume 69, Issue 2, Page(s) 134–147

    Abstract: After an amputation, advanced prosthetic limbs can be used to interface with the nervous system and restore motor function. Despite numerous breakthroughs in the field, many of the recent research advancements have not been widely integrated into ... ...

    Abstract After an amputation, advanced prosthetic limbs can be used to interface with the nervous system and restore motor function. Despite numerous breakthroughs in the field, many of the recent research advancements have not been widely integrated into clinical practice. This review highlights recent innovations in neuromuscular implants-specifically those that interface with skeletal muscle-which could improve the clinical translation of prosthetic technologies. Skeletal muscle provides a physiologic gateway to harness and amplify signals from the nervous system. Recent surgical advancements in muscle reinnervation surgeries leverage the "bio-amplification" capabilities of muscle, enabling more intuitive control over a greater number of degrees of freedom in prosthetic limbs than previously achieved. We anticipate that state-of-the-art implantable neuromuscular interfaces that integrate well with skeletal muscle and novel surgical interventions will provide a long-term solution for controlling advanced prostheses. Flexible electrodes are expected to play a crucial role in reducing foreign body responses and improving the longevity of the interface. Additionally, innovations in device miniaturization and ongoing exploration of shape memory polymers could simplify surgical procedures for implanting such interfaces. Once implanted, wireless strategies for powering and transferring data from the interface can eliminate bulky external wires, reduce infection risk, and enhance day-to-day usability. By outlining the current limitations of neuromuscular interfaces along with potential future directions, this review aims to guide continued research efforts and future collaborations between engineers and specialists in the field of neuromuscular and musculoskeletal medicine.
    MeSH term(s) Artificial Limbs ; Muscle, Skeletal ; Electrodes
    Language English
    Publishing date 2023-12-21
    Publishing country United States
    Document type Journal Article ; Review
    ZDB-ID 438353-9
    ISSN 1097-4598 ; 0148-639X
    ISSN (online) 1097-4598
    ISSN 0148-639X
    DOI 10.1002/mus.28029
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 1449: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)
    Zs.MO 551: Show issues

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  6. Article ; Online: Impacts of dibutyl phthalate on bacterial community composition and carbon and nitrogen metabolic pathways in a municipal wastewater treatment system.

    Wang, Jian / Tian, Yucheng / Wei, Jian / Lyu, Chunjian / Yu, Huibin / Song, Yonghui

    Environmental research

    2023  Volume 223, Page(s) 115378

    Abstract: Dibutyl phthalate (DBP) is a typical toxic and hazardous pollutant in pharmaceutical wastewater, affecting the metabolism of microbial flora, leading to decreased treatment efficiency, and deteriorated effluent quality in municipal wastewater treatment ... ...

    Abstract Dibutyl phthalate (DBP) is a typical toxic and hazardous pollutant in pharmaceutical wastewater, affecting the metabolism of microbial flora, leading to decreased treatment efficiency, and deteriorated effluent quality in municipal wastewater treatment plants (WWTPs). This study conducted a long-term experiment with 6 operational stages in a pilot-scale A
    MeSH term(s) Dibutyl Phthalate/toxicity ; Waste Disposal, Fluid ; Nitrogen/metabolism ; Carbon ; RNA, Ribosomal, 16S ; Bacteria/genetics ; Bacteria/metabolism ; Metabolic Networks and Pathways ; Water Purification ; Pharmaceutical Preparations ; Bioreactors/microbiology ; Sewage/microbiology
    Chemical Substances Dibutyl Phthalate (2286E5R2KE) ; Nitrogen (N762921K75) ; Carbon (7440-44-0) ; RNA, Ribosomal, 16S ; Pharmaceutical Preparations ; Sewage
    Language English
    Publishing date 2023-01-26
    Publishing country Netherlands
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 205699-9
    ISSN 1096-0953 ; 0013-9351
    ISSN (online) 1096-0953
    ISSN 0013-9351
    DOI 10.1016/j.envres.2023.115378
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 726: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (1.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  7. Article: Merging Humans and Neuroprosthetics through Regenerative Peripheral Nerve Interfaces

    Tian, Yucheng / Vaskov, Alex K. / Adidharma, Widya / Cederna, Paul S. / Kemp, Stephen W.P.

    Seminars in Plastic Surgery

    (Michigan Special Issue: 60 Years of Michigan Plastic Surgery)

    2024  Volume 38, Issue 01, Page(s) 10–18

    Abstract: Limb amputations can be devastating and significantly affect an individual's independence, leading to functional and psychosocial challenges in nearly 2 million people in the United States alone. Over the past decade, robotic devices driven by neural ... ...

    Series title Michigan Special Issue: 60 Years of Michigan Plastic Surgery
    Abstract Limb amputations can be devastating and significantly affect an individual's independence, leading to functional and psychosocial challenges in nearly 2 million people in the United States alone. Over the past decade, robotic devices driven by neural signals such as neuroprostheses have shown great potential to restore the lost function of limbs, allowing amputees to regain movement and sensation. However, current neuroprosthetic interfaces have challenges in both signal quality and long-term stability. To overcome these limitations and work toward creating bionic limbs, the Neuromuscular Laboratory at University of Michigan Plastic Surgery has developed the Regenerative Peripheral Nerve Interface (RPNI). This surgical construct embeds a transected peripheral nerve into a free muscle graft, effectively amplifying small peripheral nerve signals to provide enhanced control signals for a neuroprosthetic limb. Furthermore, the RPNI has the potential to provide sensory feedback to the user and facilitate neuroprosthesis embodiment. This review focuses on the animal studies and clinical trials of the RPNI to recapitulate the promising trajectory toward neurobionics where the boundary between an artificial device and the human body becomes indistinct. This paper also sheds light on the prospects of the improvement and dissemination of the RPNI technology.
    Keywords regenerative peripheral nerve interface ; neuroprosthetics ; sensory feedback ; clinical neural engineering
    Language English
    Publishing date 2024-02-01
    Publisher Thieme Medical Publishers, Inc.
    Publishing place Stuttgart ; New York
    Document type Article
    ZDB-ID 2077828-4
    ISSN 1536-0067 ; 1535-2188
    ISSN (online) 1536-0067
    ISSN 1535-2188
    DOI 10.1055/s-0044-1779028
    Database Thieme publisher's database

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 4383: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  8. Article ; Online: Impacts of dibutyl phthalate on biological municipal wastewater treatment in a pilot-scale A2/O-MBR system

    Wang, Jian / Tian, Yucheng / Wei, Jian / Yu, Huibin / Lyu, Chunjian / Song, Yonghui

    Chemosphere. 2022 Dec., v. 308 p.136559-

    2022  

    Abstract: Dibutyl phthalate (DBP) is a typical contaminant in pharmaceutical wastewater with strong bio-depressive properties which potentially affects the operation of municipal wastewater treatment systems. Based on a year-round monitoring of the quality of ... ...

    Abstract Dibutyl phthalate (DBP) is a typical contaminant in pharmaceutical wastewater with strong bio-depressive properties which potentially affects the operation of municipal wastewater treatment systems. Based on a year-round monitoring of the quality of influent and effluent of a full-scale pharmaceutical wastewater treatment plant in Northeast China, the DBP was found to be the representative pollutant and its concentration in the effluent ranged 4.28 ± 0.93 mg/L. In this study, the negative effects of DBP on a pilot-scale A²/O-MBR system was investigated. When the influent DBP concentration reached 8.0 mg/L, the removals of chemical oxygen demand (COD) and total nitrogen (TN) were significantly inhabited (P < 0.01), with the effluent concentration of 54.7 ± 2.6 mg/L and 22.8 ± 3.7 mg/L, respectively. The analysis of pollutant removal characteristics of each process unit showed that DBP had the most significant effects on the removals of COD and TN in the anoxic tank. The α- and β-diversity in the system decreased significantly when the influent DBP concentration reached 8.0 mg/L. The impacts of DBP on known nitrifying bacteria, such as Nitrospira, and phosphorus accumulating organisms (PAOs), such as Cadidatus Accumulibacter, were not remarkable. Whereas, DBP negatively affected the proliferation of key denitrifying bacteria, represented by Simplicispira, Dechloromonas and Acinetobacter. This study systematically revealed the impacts of DBP on the pollutants removal performance and the bacterial community structure of the biological municipal wastewater treatment process, which would provide insights for understanding the potential impacts of residues in treated pharmaceutical wastewater on biological municipal wastewater treatment.
    Keywords Acinetobacter ; Dechloromonas ; bacterial communities ; chemical oxygen demand ; community structure ; denitrification ; dibutyl phthalate ; municipal wastewater ; phosphorus ; pollutants ; pollution control ; total nitrogen ; wastewater treatment ; China ; Dibutyl phthalate (DBP) ; A2/O-MBR ; Pharmaceutical wastewater residues ; Microbial community structure
    Language English
    Dates of publication 2022-12
    Publishing place Elsevier Ltd
    Document type Article ; Online
    ZDB-ID 120089-6
    ISSN 1879-1298 ; 0045-6535 ; 0366-7111
    ISSN (online) 1879-1298
    ISSN 0045-6535 ; 0366-7111
    DOI 10.1016/j.chemosphere.2022.136559
    Database NAL-Catalogue (AGRICOLA)

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 2540: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  9. Article ; Online: Impacts of dibutyl phthalate on biological municipal wastewater treatment in a pilot-scale A

    Wang, Jian / Tian, Yucheng / Wei, Jian / Yu, Huibin / Lyu, Chunjian / Song, Yonghui

    Chemosphere

    2022  Volume 308, Issue Pt 3, Page(s) 136559

    Abstract: Dibutyl phthalate (DBP) is a typical contaminant in pharmaceutical wastewater with strong bio-depressive properties which potentially affects the operation of municipal wastewater treatment systems. Based on a year-round monitoring of the quality of ... ...

    Abstract Dibutyl phthalate (DBP) is a typical contaminant in pharmaceutical wastewater with strong bio-depressive properties which potentially affects the operation of municipal wastewater treatment systems. Based on a year-round monitoring of the quality of influent and effluent of a full-scale pharmaceutical wastewater treatment plant in Northeast China, the DBP was found to be the representative pollutant and its concentration in the effluent ranged 4.28 ± 0.93 mg/L. In this study, the negative effects of DBP on a pilot-scale A
    MeSH term(s) Bacteria ; Bioreactors/microbiology ; Denitrification ; Dibutyl Phthalate ; Environmental Pollutants ; Nitrogen ; Pharmaceutical Preparations ; Phosphorus ; Sewage/microbiology ; Waste Disposal, Fluid ; Waste Water/chemistry ; Water Purification
    Chemical Substances Environmental Pollutants ; Pharmaceutical Preparations ; Sewage ; Waste Water ; Dibutyl Phthalate (2286E5R2KE) ; Phosphorus (27YLU75U4W) ; Nitrogen (N762921K75)
    Language English
    Publishing date 2022-09-19
    Publishing country England
    Document type Journal Article
    ZDB-ID 120089-6
    ISSN 1879-1298 ; 0045-6535 ; 0366-7111
    ISSN (online) 1879-1298
    ISSN 0045-6535 ; 0366-7111
    DOI 10.1016/j.chemosphere.2022.136559
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.A 2540: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

  10. Article ; Online: Design and optimization of selective and potent CDK9 inhibitors with flavonoid scaffold for the treatment of acute myeloid leukemia.

    Wu, Tizhi / Yu, Bin / Gong, Weihong / Zhang, Jing / Yu, Sixian / Tian, Yucheng / Zhao, Tengteng / Li, Zhiyu / Wang, Jubo / Bian, Jinlei

    European journal of medicinal chemistry

    2023  Volume 259, Page(s) 115711

    Abstract: Acute myeloid leukemia (AML) is a prevalent hematological tumor associated with a high morbidity and mortality rate. CDK9, functioning as a pivotal transcriptional regulator, facilitates transcriptional elongation through phosphorylation of RNA ... ...

    Abstract Acute myeloid leukemia (AML) is a prevalent hematological tumor associated with a high morbidity and mortality rate. CDK9, functioning as a pivotal transcriptional regulator, facilitates transcriptional elongation through phosphorylation of RNA polymerase II, which further governs the protein levels of Mcl-1 and c-Myc. Therefore, CDK9 has been considered as a promising therapeutic target for AML treatment. Here, we present the design, synthesis, and evaluation of CDK9 inhibitors bearing a flavonoid scaffold. Among them, compound 21a emerged as a highly selective CDK9 inhibitor (IC
    MeSH term(s) Humans ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/therapeutic use ; Flavonoids/pharmacology ; Flavonoids/therapeutic use ; Myeloid Cell Leukemia Sequence 1 Protein/metabolism ; Leukemia, Myeloid, Acute/pathology ; Apoptosis ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/therapeutic use ; Cell Line, Tumor ; Cyclin-Dependent Kinase 9/metabolism
    Chemical Substances Antineoplastic Agents ; Flavonoids ; Myeloid Cell Leukemia Sequence 1 Protein ; Protein Kinase Inhibitors ; Cyclin-Dependent Kinase 9 (EC 2.7.11.22) ; CDK9 protein, human (EC 2.7.11.22)
    Language English
    Publishing date 2023-08-09
    Publishing country France
    Document type Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2023.115711
    Database MEDical Literature Analysis and Retrieval System OnLINE

    More links

    Kategorien

    In stock of ZB MED Cologne/Königswinter

    Zs.B 784: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

    Order via subito

    This service is chargeable due to the Delivery terms set by subito. Orders including an article and supplementary material will be classified as separate orders. In these cases, fees will be demanded for each order.

To top