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Analysis of the crystal structures of
2024-11-11

Analysis of the crystal structures of LAPs from E. coli[29], bovine eye lens [30], Pseudomonas putida[27], tomato [31] and P. falciparum[32] revealed that the monomer of M17-family LAP is composed of two domains: the smaller, variable N-terminal domain and the larger, conserved C-terminal domain tha
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br Brain cell reactions Brain cells in common with
2024-11-11

Brain cell reactions Brain cells in common with all metabolic cells must contain chemically active primary compounds which spontaneously initiate and continue cell reactions under normal conditions of temperature and pressure (NTP). These compounds have been identified as monophosphoric and polyp
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In the late s Solvay Pharmaceuticals discontinued the Phase
2024-11-09

In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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br Materials and methods br
2024-11-09

Materials and methods Results and discussion Conclusion Amino-functionalized mesoporous TiO2-NH2 microparticles were used to immobilize ADA, followed by GLU cross-linking. The mesopores provided a natural microenvironment with sufficient room for the enzyme to efficiently perform its cataly
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In conclusion two novel series of furo pyrimidin amines
2024-11-09

In conclusion, two novel series of furo[2,3-]pyrimidin4-amines and 7-pyrrolo[2,3-]pyrimidin-4-amines which exhibit potent in vitro inhibitor activity against ACK1 have been identified and evaluated. 1,3-Dithiolane-substituted pyrrolopyrimidine displays excellent ACK1 cellular inhibition, good kinas
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br Conclusion There have been multiple clinical trials and p
2024-11-09

Conclusion There have been multiple clinical trials and pre-clinical studies that have tested the utility of 5ARIs in treating prostate disease, as summarized in Fig. 1. Inhibiting androgen action through the use of finasteride and dutasteride has been established as a valuable resource for physi
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br Clinical realities br Commentary on
2024-11-09

Clinical realities Commentary on uses of selective 17,20 lyase inhibitors If continued monitoring of these same parameters along with tracking of circulating ACTH in human trials confirms these new drugs are the long sought after 17,20 lyase inhibitors, then we may for the first time be able t
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br Structure of V ATPase V
2024-11-09

Structure of V-ATPase V-ATPase is a highly conserved multi-subunit enzyme that uses energy from ATP hydrolysis to transport protons across membranes [2], [3], [4]. It consists of two major functional domains, V1 and V0 (Fig. 1). The former has eight different subunits (A, B, C, D, E, F, G, and H)
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br Resection of DNA ends The highly conserved MRN
2024-11-09

Resection of DNA ends The highly conserved MRN/MRX complex (Mre11-Rad50-Nbs1 in metazoan; Mre11-Rad50-Xrs2 in yeast) and the Ku70/Ku80 heterodimer (hereafter referred to as Ku) are the first protein complexes to be recruited at DSBs [6]. The presence of Ku and MRN/MRX mediates the recruitment of
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In Rainey et al published the results of a
2024-11-09

In 2008, Rainey et al. published the results of a targeted compound library screen for potential inhibitors of the ATM kinase. In this study, the compound CP466722 was identified as a highly selective and rapidly reversible ATM inhibitor, which did not inhibit PI3K or related PIKK family members. Mo
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GABAB receptor is associated with brain
2024-11-09

GABAB receptor is associated with GDC-0879 and behavioral diseases, including epilepsy, spasticity, anxiety and neuropathic pain (Bettler et al., 2004, Bowery et al., 2002, Froestl, 2010). Baclofen, a clinical drug and selective GABAB receptor agonist, is used to treat muscle spasticity in patients
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br Author contribution br Acknowledgement br Introduction Si
2024-11-09

Author contribution Acknowledgement Introduction Since the initial finding of Gould et al. [1], showing the loss of dendritic spines in the hippocampus after ovariectomy and its rescue after treatment of the animals with estradiol, a tremendous number of studies have demonstrated a role of
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MMP is the most critical protease which is
2024-11-09

MMP9 is the most critical protease which is involved in the degradation of ECM. TIMP-1 is an important regulator in the synthesis and degradation of ECM [8,9]. Hepatic TIMP-1 expression significantly increases in patients with liver fibrosis [10]. Serum level of TIMP-1 expression is positively assoc
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br Antiangiogenic therapy in non small cell
2024-11-08

Antiangiogenic therapy in non-small cell lung cancer (NSCLC) Antiangiogenic targeted therapy is an area of active research in which numerous agents have been studied and have been shown to be effective for many tumor types including NSCLC. Angiogenesis is frequently upregulated in malignant solid
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Di ethylhexyl phthalate DEHP is one of the
2024-11-08

Di-(2-ethylhexyl) phthalate (DEHP) is one of the most widely used environmental chemicals in the production of polyvinyl chloride. After Glycopyrrolate synthesis into human body, DEHP can be converted to the metabolite mono-ethylhexyl phthalate (MEHP), which has higher toxicity than DEHP and can inf
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