• BI 2536 Our previous studies found that some steroid mimetic

  2024-12-13

  

  Our previous studies found that some steroid mimetic structures such as stilbene, biphenyl, naphthalene and benzothiophene rings were suitable for lipophilic moieties of 17,20-lyase inhibitors, and several inhibitors obtained using a steroid A, C-ring mimetic approach have already been published. Du

• The combination of Aurora kinase inhibitors with

  2024-12-13

  

  The combination of Aurora kinase inhibitors with standard chemotherapeutics or radiotherapeutics are currently in progress, such as AZD1152 plus radiotherapy in various solid cancer models. In addition, Azzariti et al. found that AZD1152-HQPA enhanced oxaliplatin and gemcitabine effectiveness in the

• Herbal medicines have been used

  2024-12-13

  

  Herbal medicines have been used to treat various types of diseases and disorders for thousands of years worldwide (Li and Brown, 2009). Natural products have been the remedy of cancer chemotherapy for the past several decades. Anisomeles indica (L.) Kuntze. (Labiatae), commonly known as 'yu-chen-tsa

• Although the LB domains of mGlu receptors have not been

  2024-12-13

  

  Although the LB2 domains of mGlu receptors have not been shown to form an extensive interface during activation, they do draw closer to each other, as demonstrated in crystal structures (Kunishima et al., 2000, Muto et al., 2007, Tsuchiya et al., 2002) and by FRET analysis (Doumazane et al., 2013, V

• The protective role of HMW

  2024-12-13

  

  The protective role of HMW-HA in inflammatory diseases and pulmonary damage led us to investigate whether PM2.5-induced ALI could be attenuated by HMW-HA and the underlying mechanisms. In this study, we used a rat model to evaluate the effect of HMW-HA on pulmonary histology, lung inflammation, oxid

• br Materials and methods br Results and discussion

  2024-12-13

  

  Materials and methods Results and discussion During recent years, recombinant ASK1 has been obtained by expensive baculovirus-insect cell 69 2 systems [20], [27]. In the present study, we constructed recombinant ASK1 and expressed in active form at high level in E. coli. Human ASK1 catalytic

• Songbirds are outstanding models in

  2024-12-13

  

  Songbirds are outstanding models in the study of vocal communication (Maney and Pinaud, 2011). Following the pioneering studies of William H. Thorpe and Peter Marler on the development of song in chaffinches (Fringilla coelebs) and white-crowned sparrows (Zonotrichia leucophrys) (Marler, 2004; Thorp

• Apelin induced G i activation has

  2024-12-13

  

  Apelin induced Gαi activation has been demonstrated as a benefiting effect on cardiac contractility [12], [38], [39], and a vasodilator activity that protects against angiotensin-II-induced cardiovascular fibrosis and atheroma [40], [41]. In contrast, stretch causes hypertrophy through diminishing G

• br Apelin Discovered in apelin

  2024-12-13

  

  Apelin Discovered in 1998, apelin was initially identified as the sole endogenous ligand for the APJ receptor (Tatemoto et al., 1998). Apelin-77 (pre-pro-apelin) is the precursor for various pharmacologically active apelin isoforms (e.g. apelin-12, -13, -17 and 36), and it shares 75–95% sequence

• Another interesting aspect of neutralizing

  2024-12-13

  

  Another interesting aspect of neutralizing AP-1 is the inhibition of interactions between AP-1 and Smad proteins, which synergize to activate the TGF-β1-responsive genes involved in hypertrophic growth of the heart muscle and in the development of cardiac fibrosis. Through preventing AP-1 activation

• br Nanoparticle Conjugated Topoisomerase Inhibitors The safe

  2024-12-13

  

  Nanoparticle-Conjugated Topoisomerase Inhibitors The safety and efficacy of topotecan administered as LDM or MTD have been evaluated in several preclinical studies and a few clinical trials whose results showed that there can be significant adverse effects likely precluding its use in patients [5

• Kidney contributes importantly to the long term

  2024-12-13

  

  Kidney contributes importantly to the long-term blood pressure control via regulating sodium homeostasis. Renal proximal tubule (RPT) is one of the most critical segments for sodium reabsorption within kidney and therefore involved in blood pressure adjustment. This process is regulated by numerous

• Pathogen infected macrophages release exosomes associating w

  2024-12-12

  

  Pathogen-infected epacadostat release exosomes associating with pathogen-associated molecular patterns (PAMPs) such as LPS and lipoprotein derived from microorganisms [29,30]. Exosomes released by bacterially infected, but not uninfected, macrophages stimulate macrophages to release inflammatory med

• br Introduction The structural similarities

  2024-12-12

  

  Introduction The structural similarities between puromycin (1, Fig. 1) and the aminoacyl adenyl terminal of aminoacyl–tRNA allow it to terminate the protein synthesis process by causing premature release of a polypeptide from the ribosome [1], [2]. Tremendous progress in the study of puromycin an

• Voreloxin Hydrochloride Imatinib was first approved for the

  2024-12-12

  

  Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h

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