Pad4 Inhibitor

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Pad4 Inhibitor 的研究
PubMed
PAD4 and Its Inhibitors in Cancer Progression and Prognosis
The systemic spread of malignancies and the risk of cancer-associated thrombosis are major clinical challenges in cancer therapy worldwide. As an important post-translational modification enzyme, peptidyl arginine deiminase 4 (PAD4) could mediate the citrullination of protein in different components...
作者: Di Zhu
已发布: 2022/11/08
Keywords: NETosis; P…
ScienceDirect
Peptidylarginine deiminases 4 as a promising target in drug discovery
Peptidylarginine deaminase 4 (PAD4) is a crucial post-translational modifying enzyme catalyzing the conversion of arginine into citrulline residues, and mediating the formation of neutrophil extracellular traps (NETs). PAD4 plays a vital role in the occurrence and development of cardiovascular disea...
已发布: 2021/12/15
Cited By: 0
Keywords: NETs; Citru…
PubMed
GSK484, an inhibitor of peptidyl arginine deiminase 4, increases the radiosensitivity of colorectal cancer and inhibits neutrophil extracellular traps
Introduction: Colorectal cancer (CRC) is the third most common malignancy and a major cause of cancer-related deaths. Peptidyl arginine deiminase 4 (PAD4 or PADI4) is expressed in neutrophils that, when activated, can drive the formation of neutrophil extracellular traps (NETs). PAD4 has been found ...
作者: Binbin Wang
已发布: 2023/9
Keywords: Colorectal …
PubMed
A Novel Peptidylarginine Deiminase 4 (PAD4) Inhibitor BMS-P5 Blocks Formation of Neutrophil Extracellular Traps and Delays Progression of Multiple Myeloma
Multiple myeloma is a plasma cell malignancy, which grows in the bone marrow (BM). The major population of cells in the BM is represented by neutrophils and they can form neutrophil extracellular traps (NET). Here, we investigated whether multiple myeloma cells induce NET formation and whether targe...
作者: Marina Li
已发布: 2020/7
Keywords: National In…
ScienceDirect
Topical Perspectives Identification of novel PAD4 inhibitors based on a pharmacophore model derived from transition state coordinates
1.4 Protein arginine deiminases 4 (PAD4) is an attractive target for the development of novel and selective inhibitors of Rheumatoid Arthritis (RA). F-amidine is known as mechanism-based inhibitor targeting PAD4 and used as inactivators by covalently modifying the active site Cys645. To identify nov...
已发布: 2017/03/01
Cited By: 0
Keywords: Protein argi…
nih.gov
https://pmc.ncbi.nlm.nih.gov › articles
Structure–Activity Relationship of PAD4 Inhibitors and Their Role …
Protein arginine deiminase 4 (PAD4) plays an important role in cancer progression by participating in gene regulation, protein modification, and neutrophil extracellular trap (NET) formation. Many reversible and irreversible PAD4 inhibitors have ...
- Protein arginine deiminase 4 …
  Importantly, the discovery of a role for PAD4 in p53 regulated transcription …
- PAD4 and Its Inhibitors in …
  In this review, we describe PAD4 involvement in gene regulation, protein …
- GSK484, an inhibitor of pepti…
  This study is aimed at exploring the role of PAD4 inhibitor (GSK484) in NET …
- Inhibition of PAD4 activity is …
  PAD4 has been strongly implicated in the pathogenesis of autoimmune, …
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ACS Publications
https://pubs.acs.org › doi
Novel Peptidylarginine Deiminase Type 4 …
2022年9月6日 · The present application describes a series of novel compounds as PAD4 inhibitors for the treatment of rheumatoid arthritis, systemic lupus erythematous, …
标记:
Enzyme inhibitor
Cancer
PAD4 inhibitor的图片

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abcam.com
GSK484, PAD4 inhibitor (CAS 1652591-81-5) (ab223598) | Abcam
researchgate.net
Synthesis and characterization of more potent PAD4 inhibitors. A,... | Download Scientific Diagram
frontiersin.org
Frontiers | The role of protein arginine deiminase 4-dependent neutrophil extracellular traps ...
pubs.acs.org
Novel Peptidylarginine Deiminase Type 4 (PAD4) Inhibitors | ACS Medicinal Chemistry Letters
onlinelibrary.wiley.com
PAD4 takes charge during neutrophil activation: Impact of PAD4 mediated NET formation on immune ...
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nih.gov
https://pmc.ncbi.nlm.nih.gov › articles
Protein arginine deiminase 4 (PAD4): …
Importantly, the discovery of a role for PAD4 in p53 regulated transcription utilized a recently described PAD4 inhibitor that was developed in our lab . This compound, denoted Cl-amidine, …
MDPI
https://www.mdpi.com
Structure–Activity Relationship of PAD4 Inhibitors and Their Role …
2024年2月28日 · In this review, we summarize the structure–activity relationships of newly investigated PAD4 inhibitors to bring researchers up to speed by guiding and describing new …
标记:
Enzyme inhibitor
Immunotherapy
PubMed
https://pubmed.ncbi.nlm.nih.gov
PAD4 and Its Inhibitors in Cancer Progression and Prognosis
2022年11月8日 · In this review, we describe PAD4 involvement in gene regulation, protein citrullination, and NET formation. We also discuss its potential role in cancer and cancer …
标记:
Pad4 Inhibitor
Cancer Research
Pad4 Enzyme
ScienceDirect
https://www.sciencedirect.com › science › article › pii
Peptidylarginine deiminases 4 as a promising target in drug …
2021年12月15日 · More and more efforts are devoted to developing highly efficient and selective PAD4 inhibitors via high-throughput screening, structure-based drug design and structure …
标记:
Chao Yang, Zhen-Zhen Dong, Jing Zhang, Dehong Teng, Xinzhi Luo, Dan Li, Yingtang Zhou
其他用户还问了以下问题
What are pad inhibitors?
Due to their potential role in human disease, the interest in identifying PAD inhibitors is high. In recent years, several PAD inhibitors have been described, but most of these compounds are relatively weak (Figure 5). For example, taxol and benzoyl- NG -asymmetrical dimethyl-Arg are high μM to mM PAD4 inhibitors [41, 55].
Protein arginine deiminase 4 (PAD4): current understanding and future
pmc.ncbi.nlm.nih.gov
What are PAD4 inhibitors & how do they work?
As mentioned above, PAD4 inhibitors are able to inhibit the expression of genes, such as PD1 and LAG3, which are potential immune checkpoint inhibitors, and their ability to inhibit tumor progression can be enhanced in combination with anti-CTLA-4 and anti-PD-1 antibodies.
Structure–Activity Relationship of PAD4 Inhibitors and Their Role in
mdpi.com
Are PAD4 inhibitors effective in treating rheumatoid arthritis and lupus erythematous?
The present application describes a series of novel compounds as PAD4 inhibitors for the treatment of rheumatoid arthritis, systemic lupus erythematous, antiphospholipid antibody syndrome, small vessels vasculitis, colitis, thrombosis, atherosclerosis, sepsis, diabetes, and certain types of cancer.
Novel Peptidylarginine Deiminase Type 4 (PAD4) Inhibitors
pubs.acs.org
What is PAD4 inhibitor 19?
Mydel et al. discovered a novel PAD4 inhibitor 19, which remarkably suppressed histone citrullination . 19 prevented the formation of NETs and blocked DNA release from neutrophils induced by PMA (phorbol 12 myristate 13 acetate). In general, 19 showed better PAD4 inhibitory activity than 2.
Peptidylarginine deiminases 4 as a promising target in drug discovery
sciencedirect.com
Are PAD4 inhibitors reversible?
Reversible (Non-Covalent) PAD4 Inhibitors The great degree of structural conservation of the PAD active site across all isoforms complicates the design of inhibitors specific to PAD4 isoforms. Simultaneous inhibition of multiple PAD isoforms is undesirable because each isoform is involved in a different biological pathway .
Structure–Activity Relationship of PAD4 Inhibitors and Their Role in
mdpi.com
What are the best PAD4 inhibitors?
For example, taxol and benzoyl- NG -asymmetrical dimethyl-Arg are high μM to mM PAD4 inhibitors [41, 55]. In contrast, our lab has successfully developed highly potent PAD4 inactivators (Figure 5) [47, 56]. The best two compounds, i.e. F-amidine and Cl-amidine, incorporate a haloacetamidine warhead in place of a substrate guanidinium group.
Protein arginine deiminase 4 (PAD4): current understanding and future
pmc.ncbi.nlm.nih.gov
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PubMed
https://pubmed.ncbi.nlm.nih.gov
GSK484, an inhibitor of peptidyl arginine deiminase 4 ... - PubMed
2023年5月19日 · This study is aimed at exploring the role of PAD4 inhibitor (GSK484) in NET formation and radioresistance in CRC. Methods: Reverse transcriptase quantitative …
标记:
Pad4 Inhibitor
Colorectal cancer
Neutrophil extracellular traps
nih.gov
https://pmc.ncbi.nlm.nih.gov › articles
Inhibition of PAD4 activity is sufficient to disrupt mouse and …
PAD4 has been strongly implicated in the pathogenesis of autoimmune, cardiovascular and oncological diseases, through clinical genetics and gene disruption in mice. Novel, selective …
标记:
PAD4
Necessity and sufficiency
Nature
https://www.nature.com › articles
Antibody discovery identifies regulatory mechanisms of protein …
2024年2月2日 · Small-molecule PAD4 inhibitors were developed and found to be effective in alleviating RA phenotypes in mouse models, indicating the relevance of PAD4 in RA pathology …
标记:
PAD4
Nature Chemical Biology
American Association for Cancer Research
https://aacrjournals.org › ...
A Novel Peptidylarginine Deiminase 4 …
2020年7月2日 · BMS-P5 is a potent selective pharmacological inhibitor of PAD4 (Supplementary Table S1) and was used to evaluate the effect of PAD4 inhibition on multiple myeloma …
标记:
Pad4 Inhibitor
Multiple Myeloma
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Structure–Activity Relationship of PAD4 Inhibitors and Their Role …

Protein arginine deiminase 4 …

PAD4 and Its Inhibitors in …

GSK484, an inhibitor of pepti…

Inhibition of PAD4 activity is …

Novel Peptidylarginine Deiminase Type 4 …

PAD4 inhibitor的图片

Protein arginine deiminase 4 (PAD4): …

Structure–Activity Relationship of PAD4 Inhibitors and Their Role …

PAD4 and Its Inhibitors in Cancer Progression and Prognosis

Peptidylarginine deiminases 4 as a promising target in drug …

Protein arginine deiminase 4 (PAD4): current understanding and future

Structure–Activity Relationship of PAD4 Inhibitors and Their Role in

Novel Peptidylarginine Deiminase Type 4 (PAD4) Inhibitors

Peptidylarginine deiminases 4 as a promising target in drug discovery

Structure–Activity Relationship of PAD4 Inhibitors and Their Role in

Protein arginine deiminase 4 (PAD4): current understanding and future

GSK484, an inhibitor of peptidyl arginine deiminase 4 ... - PubMed

Inhibition of PAD4 activity is sufficient to disrupt mouse and …

Antibody discovery identifies regulatory mechanisms of protein …

A Novel Peptidylarginine Deiminase 4 …

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