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Inhibitor molecules
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Transforming growth factor-β (TGF-β) is a cytokine with multiple functions, including cell growth regulation, extracellular matrix production, angiogenesis homeostasis adjustment and et al. TGF-β pathway activation promotes tumor metastasis/progression and mediates epithelial-mesenchymal transmission suppressing immunosurveillance in advanced tumors.
13p
vishanshan
27-06-2024
1
1
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Corrosion inhibitors are one of the practical and cost-effective way of preventing and inhibiting corrosion. An inhibitor's primary function includes creating a barrier by forming one or more molecular layers to protect against corrosive attacks. Organic molecules are one of the most popular, efficient, and practical corrosion inhibitors, and all studies demonstrate that organic compounds, preferentially those containing nitrogen (N), sulphur (S), and oxygen (O), have high inhibitory efficiency
28p
dianmotminh02
03-05-2024
2
1
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Ebook "Targeting protein-protein interactions by small molecules" comprehensively reviews the state-of-the-art strategies developed for protein-protein interaction (PPI) inhibitors, and highlights the success stories in new drug discovery and development. Consisting of two parts with twelve chapters, it demonstrates the design strategies and case studies of small molecule PPI inhibitors. The first part discusses various discovery strategies for small molecule PPI inhibitors, such as high throughput screening, hot spot-based design, computational approaches, and fragment-based design.
332p
tracanhphuonghoa1007
22-04-2024
4
2
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Immune checkpoint blockade (ICB) therapy has demonstrated considerable clinical benefit in several malignancies, but has shown favorable response in only a small proportion of cancer patients. Recent studies have shown that matrix metalloproteinases (MMPs) are highly associated with the microenvironment of tumors and immune cells. However, it is unknown whether MMPs are involved in immunotherapy.
19p
vibransone
28-03-2024
6
2
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Ebook "Therapy of viral infections (Topics in medicinal chemistry, Volume 15)" focuses on the one hand on recent developments of inhibitors against wellestablished drug targets and on the other hand new targets on either the virus or its host side are presented.
231p
manmanthanhla0201
26-02-2024
1
1
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Transporter associated with antigen processing 1 (TAP1) is a molecule involved in processing and presentation of major histocompatibility complex class I restricted antigens, including tumor-associated antigens. TAP1 participates in tumor immunity, and is aberrantly expressed in multiple cancer types.
17p
vischultz
20-10-2023
1
1
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Cancer cells express immunosuppressive molecules, such as programmed death ligands (PD-L)1 and PD-L2, enabling evasion from the host’s immune system. Cancer cells synthesize and secrete acetylcholine (ACh), acting as an autocrine or paracrine hormone to promote their proliferation, differentiation, and migration.
20p
visharma
20-10-2023
6
2
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Clear cell renal cell carcinoma (ccRCC) is the most common type of kidney cancer and is notorious for its resistance to both chemotherapy and small-molecule inhibitor targeted therapies. Subcellular targeted cancer therapy may thwart the resistance to produce a substantial effect.
9p
visharma
20-10-2023
3
2
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Dicarbonyl/L-xylulose reductase (DCXR) is an enzyme reducing dicarbonyl (-CO-) groups in single sugar molecules and participates in the sugar metabolism of several sugar metabolism cycles in different living organisms (humans, other animals, fungi, and microorganisms).
10p
vimulcahy
18-09-2023
9
3
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Design, synthesis, and in vitro antitumor activity of 6-aryloxyl substituted quinazoline derivatives
Quinazoline derivatives are a class of important antitumor drugs known as small molecule inhibitors that include epidermal growth factor receptor (EGFR) inhibitors. Based on the structure of poziotinib, a series of 6-aryloxyl substituted quinazoline derivatives were designed and synthesized. The molecular docking results suggested that compound 4m has different binding modes to the wild-type and mutated EGFR.
37p
lyhuyenthu
31-01-2023
3
2
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The inhibition effect of hydroxyethylcellulose (HEC) on 1018 c-steel corrosion in 3.5% NaCl solution was investigated by using potentiodynamic polarization, electrochemical frequency modulation (EFM) and electrochemical impedance spectroscopy (EIS) techniques.
8p
vihermione
06-01-2023
9
2
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The therapeutic armamentarium in multiple myeloma has been significantly broadened by proteasome inhibitors, highly efficient means in controlling of multiple myeloma. Despite the developments of therapeutic regimen in treatment of multiple myeloma, still the complete remission requires a novel therapeutic strategy with significant differences in outcomes.
10p
vikolindagrabar
27-07-2022
8
2
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Glioblastoma (GBM) is the most common primary malignant brain tumor in adults exhibiting infiltration into surrounding tissues, recurrence, and resistance to therapy. GBM infiltration is accomplished by many deregulated factors such as cell adhesion molecules (CAMs), which are membrane proteins that participate in cell-cell and cell-ECM interactions to regulate survival, proliferation, migration, and stemness.
12p
visusanwojcicki
28-06-2022
7
2
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Isatin, 1H -indoline-2,3-dione, an endogenous compound, is also a synthetically versatile molecule that possesses a diversity of biological activities including anticonvulsant, antibacterial, antifungal, antiviral, anticancer, and cytotoxic properties. Based on the promising cytotoxic activity studies on N -substituted isatin derivatives, a series of 18 derivatives of 2-(2,3-dioxo-2,3-dihydro-1H -indol-1-yl)-N -phenylacetamide were designed, synthesized, and characterized according to their analytical and spectral data.
9p
langthannam
29-12-2021
11
1
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The M2 protein of the influenza A virus, responsible for flu, is a homotetramer transmembrane protein, forming a transmembrane ion channel, where His 37s act as pH sensors and Trp 41s and Asp 44s act as channel gates. Opening of this channel leads to transfer of virus RNA into the human host. Thus, blocking this transfer is an important pharmaceutical strategy to stop infection. As a result of viral drug resistance, commercially available channel inhibitors, rimantadine (RIM) and amantadine (AMA), are not as effective as they used to be.
17p
tudichquannguyet
29-11-2021
13
1
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A total of 63 newly synthesized compounds were screened in terms of PARP inhibition by cellular PARylation assay in the HeLa cell line. It was found that 19 compounds significantly inhibited the H2O2 -induced cellular PARylation. The chemosensitizer effect of these compounds in cancer cells treated with doxorubicin (doxo) was investigated. It was found that the combination of potent PARP inhibitors with doxo potentiated a cytotoxic effect, similar to that of olaparib.
26p
tudichquannguyet
29-11-2021
6
0
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The excessive activity of acetylcholinesterase enzyme (AChE) causes different neuronal problems, especially dementia and neuronal cell deaths. Food and Drug Administration (FDA) approved drugs donepezil, rivastigmine, tacrine and galantamine are AChE inhibitors and in the treatment of Alzheimer’s disease (AD) these drugs are currently prescribed. However, these inhibitors have various adverse side effects. Therefore, there is a great need for the novel selective AChE inhibitors with fewer adverse side effects for the effective treatment.
15p
tudichquannguyet
29-11-2021
15
1
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The molecular features characteristics provided by the 3D-QSAR contour plots were quite useful for designing and improving the activity of acetylcholinesterase of this class. Based on these findings, a new series of 1,2,3-triazole based derivatives were designed, among which compound A1 with the highest predictive activity was subjected to detailed molecular docking and compared to the most active compound.
14p
tudichquannguyet
29-11-2021
10
1
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Neuroblastoma (NB) patients with MYCN amplification or overexpression respond poorly to current therapies and exhibit extremely poor clinical outcomes. PI3K-mTOR signaling-driven deregulation of protein synthesis is very common in NB and various other cancers that promote MYCN stabilization.
13p
vimahuateng
26-11-2021
4
1
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Bioinformatic analyses have suggested their upregulation in leukemia/lymphoma, thymoma, pancreas, glioma, and glioblastoma, and downregulation in cervical, uterine, rectum, and colon cancers. However, every cancer type includes, at least, a subtype with high MEIS expression. In addition, studies have highlighted that MEIS proteins and associated factors may function as diagnostic or therapeutic biomarkers for various diseases.
28p
thiencuuchu
27-11-2021
7
1
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