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During the course of our ACK inhibitor program
2025-02-21
During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of ident
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Renal cell carcinoma RCC accounts for more than
2025-02-21
Renal cell carcinoma (RCC) accounts for more than 12,000 cancer deaths in the United States (Jemal et al., 2003). The current treatment includes surgical resection followed by interleukin-2 or Interferon-α treatment. Some patients experience distant metastatic lesions of RCC. In the last 5 years, re
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Carbenoxolone Another open question is whether GABA and ACh
2025-02-21
Another open question is whether GABA and ACh are released from the same synaptic vesicles, or even the same presynaptic terminals. Multi-transmitter neurons may either function through co-release, in which multiple neurotransmitters are packaged into the same presynaptic terminal and are therefore
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br Trauma and ACEs screening the past present
2025-02-21
Trauma and ACEs screening: the past, present, and future Traditionally, allopathy’s biomedical model has utilized an etic perspective; the outsiders’ view of the problem. Development of diagnostic screening tools requires an etic approach, which relies heavily on a completely objective perspectiv
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br AD and COX LOX
2025-02-21
AD and COX/5-LOX pharmacology Early studies on the role of cyclooxygenases in AD were inspired by epidemiological data suggesting that COX inhibitors such as nonsteroidal anti-inflammatory drugs (NSAIDs) could be beneficial in AD patients (Lucca et al., 1994, McGeer et al., 1990). This line of re
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br Acknowledgments br Introduction Hypospadias is a common
2025-02-21
Acknowledgments Introduction Hypospadias is a common congenital malformation in males, in which the urethral orifice is found on the ventral side of the penis as a result of incomplete fusion of urethral folds. The mean prevalence in per 10,000 live births from 1910 to 2013 were: Europe 19.9,
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During preparation of this manuscript some studies investiga
2025-02-21
During preparation of this manuscript, some studies investigating effects of Sunitinib on Axl activity in renal cancer have been published [44], [45], [46], [47]. However, there are several important considerations to take into account interpreting results of these studies. First, Sunitinib doses th
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In this paper we describe the formation
2025-02-21
In this paper, we describe the formation of a structure-based pharmacophore which lead to the discovery of several hydrophobic, yet non-lipid inhibitors of ATX. These compounds docked within the same volume occupied by the initial non-lipid inhibitors of ATX used to build the pharmacophore. Violatio
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Polyphenols like flavonoids have the potential to penetrate
2025-02-21
Polyphenols like flavonoids have the potential to penetrate into lipid bilayers which is vital for enabling protection against oxidation. Rosmarinic ATP luminescence assay is a natural polyphenol antioxidant isolated from Sphaeranthus amaranthoides. Polyphenols can inhibit the propagation of lipid
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br Introduction Cadmium is a
2025-02-21
Introduction Cadmium is a major component of heavy metal pollution. Phytoremediation is considered to be the more effective method for recovering contaminated soil [[1], [2], [3], [4]] via cadmium absorption, transport, and accumulation. Several cadmium-associated proteins have previously been we
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Among the most important Ca regulatory mechanisms are the
2025-02-21
Among the most important Ca regulatory mechanisms are the Plasma Membrane Calcium ATPase (PMCA) and Sarcoplasmic Reticulum Calcium ATPase (SERCA). These pumps belong to the family of P-ATPases, which share the formation of an acid-stable phosphorylated intermediate as part of their reaction cycle. P
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Thus phosphorylation of p was used to measure the intracellu
2025-02-21
Thus, phosphorylation of p38 was used to measure the intracellular potency of ASK1 inhibitors. In this assay, HEK293/AP-1luc Apoptosis inducer expressing human full-length ASK1 were incubated with compound for 18 h and then lysed and the level of phospho-p38 was quantified using the HTRF assay [33]
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br Acknowledgments br Introduction Cancer is a deadly diseas
2025-02-21
Acknowledgments Introduction Cancer is a deadly disease of uncontrolled cell division and has the potential to invade or spread to other parts of the body and affects normal functioning of the vital organs. Nowadays cancer is considered as leading cause of human death in all over the world and
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In the current study SA was
2025-02-21
In the current study, SA was assessed to confirm the safety of CS addition to erythrocytes SA as well as SA elicits antioxidant action. It has been reported that, ROS induced desialylation by depletion of SA content from cell surfaces (Pawluczyk et al., 2014, Harisa, 2015). Therefore, significant de
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br Method of literature search br
2025-02-21
Method of literature search Disclosures Acknowledgment The authors thank and acknowledge Mrs. Jaini Parekh, BFA, for illustrating the diagram in Figure 1. An overview of angiogenesis Angiogenesis is a biological process through which there is the formation of new blood vessels from pre-