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更新于：2025-05-07

L3MBTL3

更新于：2025-05-07

基本信息

别名

H-l(3)mbt-like protein 3、KIAA1798、l(3)mbt-like 3 (Drosophila)

+ [8]

简介

Is a negative regulator of Notch target genes expression, required for RBPJ-mediated transcriptional repression (PubMed:29030483). It recruits KDM1A to Notch-responsive elements and promotes KDM1A-mediated H3K4me demethylation (PubMed:29030483). Involved in the regulation of ubiquitin-dependent degradation of a set of methylated non-histone proteins, including SOX2, DNMT1 and E2F1. It acts as an adapter recruiting the CRL4-DCAF5 E3 ubiquitin ligase complex to methylated target proteins (PubMed:29691401, PubMed:30442713). Required for normal maturation of myeloid progenitor cells (By similarity).

关联

项与 L3MBTL3 相关的药物

UNC1679

靶点

L3MBTL3

作用机制

L3MBTL3 inhibitors

在研机构-

原研机构

The University of North Carolina at Chapel Hill

在研适应症-

非在研适应症-

最高研发阶段无进展

首次获批国家/地区-

首次获批日期1800-01-20

UNC1215

靶点

L3MBTL3

作用机制

L3MBTL3 inhibitors

在研机构-

原研机构

The University of North Carolina at Chapel Hill

在研适应症-

非在研适应症

肿瘤

最高研发阶段无进展

首次获批国家/地区-

首次获批日期1800-01-20

100 项与 L3MBTL3 相关的临床结果

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100 项与 L3MBTL3 相关的转化医学

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0 项与 L3MBTL3 相关的专利（医药）

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项与 L3MBTL3 相关的文献（医药）

2025-03-20·Nucleic Acids Research

Cooperation of a polymerizing SAM domain and an intrinsically disordered region enables full SAMD1 function on chromatin

Article

作者: Geller, Merle ; Nist, Andrea ; Simon, Clara ; Liefke, Robert ; Huber, Theresa ; Xu, Jingfei ; Wang, Zhanxin ; Rohner, Iris ; Cao, Yinghua ; Stiewe, Thorsten ; Wei, Pengshuai ; Stielow, Bastian ; Jeude, Lea Marie

AbstractTranscription factors orchestrate gene expression through a myriad of complex mechanisms, encompassing collaborations with other transcription factors and the formation of multimeric complexes. The chromatin-binding protein SAMD1 [sterile alpha motif (SAM) domain-containing protein 1] binds to unmethylated CpG-rich DNA utilizing its N-terminal winged-helix (WH) domain. Additionally, its C-terminal SAM domain, which mediates interactions with itself and with L3MBTL3, is crucial for chromatin binding. The precise role of the SAM domain in this process remains unclear. Using structural analyses, we elucidated the distinct homopolymerization modes within the SAM domains of L3MBTL3 and SAMD1, alongside their heterodimerization architecture. Interestingly, SAMD1 necessitates not only the WH and SAM domain but also a proline/alanine-rich intrinsically disordered region (IDR) for efficient chromatin binding. The IDR is essential for the ability of SAMD1 to form large polymers, with its functionality determined by integrity rather than the specific sequence. Mutagenesis studies underscore the critical role of arginines within the IDR for polymerization, chromatin binding, and the biological function of SAMD1. These findings propose a model in which structured and unstructured regions of SAMD1 cooperate in a coordinated fashion to facilitate chromatin binding. This work provides new insights into the diverse mechanisms transcription factors employ to interact with chromatin and regulate gene expression.

2025-01-01·Journal of Molecular Modeling

Investigation of a novel Schiff base Catena-((μ6-(E)-2-((4-methoxy-2-oxidobenzylidene)ammonio)ethane-1-sulfonato potassium as a potential antibacterial agent

Article

作者: Poyraz, Emine Berrin ; Yılmaz, Sümeyye Kırkıncı ; Dege, Necmi ; Ağar, Ayşen Alaman ; Aşkar, Şinasi ; Sıdden, Chinnasami

CONTEXTSchiff bases, which have intriguing properties in many areas, have been studied extensively in recent years due to their structural properties and biological activities. In this research, a novel water-soluble Schiff base complex, Catena-((μ₆-(E)-2-((4-methoxy-2-oxidobenzylidene) ammonio) ethane-1-sulfonato potassium, C₁₀H₁₄KNO₆S (CMOAESP), was synthesized by a one-step condensation reaction of 2-hydroxy-4-methoxy benzaldehyde and taurine with the yield of 65%, 0.333 g. Spectral analysis of water-soluble crude product showed equilibria keto-enol tautomerism, by a resulting Zwitterionic form of the structure. The ADMET prediction showed that the CMOAESP obeys Lipinski's rule and was in bioavability range. The molecular docking results showed an inhibition ability for 1JIJ and MBT1 proteins which play an important role in antibacterial studies. The experimental end theoretical calculations were in a good agreement that CMOASP has inhibition efficiency against Escherichia coli and has inhibition at high concentrations against Staphylococcaceae aureus.METHODSThe WinGX software system SHELXS direct technique was used to solve the structure, and SHELXL full-matrix least-squares approach on F² was used to refine the results. The Gaussian 09W program was used to carry out the DFT calculations. The gap values for CMOAESP were calculated by using the B3LYP/6- 311 + + G(d,p) method in order to predict its reactivities and behaviors in the gas phase. The frontier orbitals, LUMO and HOMO together with some global parameters as electronegativity (μ), chemical potential (χ), hardness (η), electrophilicity index (ω), and softness (S) values were predicted from DFT calculations.

2023-02-01·Heliyon

L3MBTL3 is induced by HIF-1α and fine tunes the HIF-1α degradation under hypoxia in vitro

Article

作者: Wang, Di ; Lai, Dongming ; Wang, Mengdong ; Lang, Yue ; Tang, Jun ; Zhang, Rui ; Xiao, Chenglu ; Shao, Anwen

HIF-1α plays a crucial part in hypoxia response by transcriptionally upregulating genes to adapt the hypoxic condition. HIF-1α is under severe cellular control as its exceptional activation is always associated with tumorigenesis and tumor progression. Here, we report L3MBTL3 serves as a novel negative regulator of HIF-1α. It is upregulated during hypoxia and acts as a transcriptional target of HIF-1α. In the nuclei, L3MBTL3 makes an interaction with HIF-1α and promotes its ubiquitination and degradation. These findings indicate L3MBTL3 forms a negative feedback loop with HIF-1α in vitro to dampen the hypoxic response.

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