• Annexin A ANXA a member of annexin superfamily

  2022-04-02

  

  Annexin A7 (ANXA7), a member of annexin superfamily, is a Ca2+- and phospholipid-binding protein and possesses GTPase activity [5,6]. The ANXA7 gene is located on human chromosome 10q21, where multiple potential tumor suppressor genes exist. Homozygous ANXA7 (−/−) knockout mice showed a lethal pheno

• br Conflict of interest statement br

  2022-04-02

  

  Conflict of interest statement Acknowledgments The authors would like to thank Dr. Linda Console-Bram for her editing of this review, Valentina Lucchesi for help with the figures, and acknowledge funding from NIH/NIDA (DA023204). Introduction G protein-coupled receptor 55 (GPR55) has emerg

• The treatment target which aims at diagnosing of

  2022-04-02

  

  The “90-90-90 treatment target” which aims at diagnosing 90% of HIV-infected individuals, treating 90% of those diagnosed and achieve viral suppression for 90% of treated individuals, is a key strategy to achieve one of the sustainable development goals (SDG) of ending AIDS as a public health threat

• The occurrence of MDR in cancer patients undergoing

  2022-04-01

  

  The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer MS023 in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems including the rhabdo

• DIG-11-dUTP mg br Materials and methods br Results br Discus

  2022-04-01

  

  Materials and methods Results Discussion Heart hypertrophy is initially physiological to compensate for the loss of heart functions. However, sustained stresses lead to a pathological status, in which myocardium becomes stiffened by interstitial fibrosis and thereby diastolic dysfunction in

• If some of the experimentally

  2022-04-01

  

  If some of the experimentally determined tRNAGlu identity elements are unique to E. coli, then there also must be some unique phylum-specific residues in the corresponding GluRS (E. coli in particular, and proteobacteria in general) as well. In this paper we focus on identifying such residues in E.

• With the advent of genome sequencing hexokinase

  2022-04-01

  

  With the advent of genome sequencing, hexokinase gene sequences are now available from a far greater number of vertebrate species, as well as from diverse non-vertebrate animal species. As indicated above, searches of vertebrate genome sequences revealed the existence of a novel fifth member of the

• GKRP binds to the inactive super open conformation of GCK

  2022-04-01

  

  GKRP binds to the inactive, super-open conformation of GCK, acting as a competitive inhibitor of glucose association with the enzyme (Fig. 3) [45]. Upon formation of the inhibitory complex with GKRP, GCK is sequestered into the hepatocyte nucleus [48]. The detailed mechanism by which GKRP mediates t

• Analogous to all GPCRs the GLP

  2022-04-01

  

  Analogous to all GPCRs, the GLP-1R transduces signals from the outside of the cell to the inside by allosterically converting a ligand-binding event to activation of intracellular effectors. The GLP-1R couples to several intracellular effectors and this pleiotropic coupling is physiologically releva

• heat shock protein inhibitors Two pathways have emerged to e

  2022-04-01

  

  Two pathways have emerged to explain the beneficial metabolic effect of Roux-en-Y bypass [Fig. 3]. Firstly, the rapid delivery of nutrients to the distal small intestine and bowel might up-regulate secretion of a physiological stimulus that improves glucose homeostasis. As such, GLP-1 represents an

• Natural products are a diverse and interesting source

  2022-04-01

  

  Natural products are a diverse and interesting source for the discovery of new lead structures (Newman and Cragg, 2016). After a successful era of natural product research, many pharmaceutical companies stopped their investment in natural product-driven drug discovery in the 1990s. The reason behind

• In stark contrast to this

  2022-04-01

  

  In stark contrast to this study, Zhang and colleagues demonstrated that FFA4, along with FFA1, play roles in suppressing cell proliferation and promoting apoptosis in CRC rat 4 treated with omega-3 PUFA [53]. In this study design, in vivo CRC was induced in mice upon treatment with the genotoxic co

• JNJ-26481585 br Clinical development of FGFR inhibitors in

  2022-04-01

  

  Clinical development of FGFR inhibitors in breast cancer The rationale to explore the role of FGFR inhibitors in patients with breast cancer comes from a variety of sources. These include genomic aberrations frequently identified in the FGF/FGFR pathway in breast cancer, the increased sensitivity

• A general synthesis of the tetrazole

  2022-04-01

  

  A general synthesis of the tetrazole is shown in . First, a magnesium-halogen exchange reaction quenched with DMF afforded benzo[]thiophene-5-carbaldehyde , which was further decorated with a bromine at the 3-position (). A Suzuki reaction with -tolylboronic HU 308 followed by reduction of the ald

• br Conclusion Discovery of an ideal orally active

  2022-04-01

  

  Conclusion Discovery of an ideal orally active antithrombotic drug has remained elusive till date. Research efforts in this direction led to the discovery of numerous coagulation enzyme inhibitors including various thrombin and FXa inhibitors. Several preclinical studies have highlighted the impo

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