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The AMPKß2 (AMP-activated protein kinase) isoform promotes glycemic homeostasis through an insulin-independent mechanism. Many glucose "importers" such as SC4 act as AMPK activators, but their prolonged consumption is associated with undesirable effects. Objetive: in this work, molecular docking was used to analyze the possible interaction between sapogenins and AMPK. Methods: the preparation of the protein blanks, preparation of the ligands and molecular coupling have been carried out. Results: the results showed that eight sapogenins present in Chenopodium quinoa interact at the same binding site as SC4 corresponding to the ADaM site of AMPK. These interactions scored ΔG values ranging from -6.2 to -7.7 kcal/mol, with Serjanic acid being the sapogenin with the lowest ΔG. The addition of hydrophilic groups such as -OH and -COOH in the chemical structure of Serjanic acid improved its binding affinity to the AMPKß2 isoform opening the possibility of generating semi-synthetic drugs from natural compounds with higher biological activity and better specificity.. [ABSTRACT FROM AUTHOR]

Copyright of Chinese Journal of Oil Crop Sciences is the property of Oil Crops Research Institute of Chinese Academy of Agricultural Sciences and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

There is an important activity of 4-thiazolidinone derivatives on the active site of protein kinases of the parasite Toxoplasma gondii. The calcium-dependent protein kinase CDPK1 is an important object of study, due to its activity in host cell invasion and parasite motility. Twelve structural modifications with alkyl, aromatic and bumpedkinase substitutions at position 3 of the 2-hydrazono-4-thiazolidinone derivative were proposed. A molecular docking and ADME-T properties study was carried out, where derivatives 8A, 2B and 3C presented low binding energy scores (-9.51, -9.19, -10.58) Kcal/mol respectively, a good toxicological profile and no violation of Lipinski's rules being candidates for synthesis for in vivo evaluation. [ABSTRACT FROM AUTHOR]

Copyright of Ginecología y Obstetricia de México is the property of Federacion Mexicana de Ginecologia y Obstetricia and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Two-component signaling circuits (TCS) allow bacteria to detect environmental cues and to produce adaptive responses. These signaling systems are based on autophosphorylation and phosphoryl-group transfers between histidine and aspartate containing sensor kinase and response regulator proteins. Upon reception of a specific stimulus the sensor kinase protein autophosphorylates, by either an inter- or intra-molecular reaction, and transphosphorylates its cognate response regulator, which, typically, acts as a transcriptional regulator, thereby triggering physiological responses. Frequently, in the absence of the stimulus, the sensor kinase proteins are responsible for the dephosphorylation of their cognate response regulators. Furthermore, a group of sensor kinases have additional functional domains that are involved in a forward phosphorelay for signal transmission and in a reverse phosphorelay for signal decay. As is the case of the autophosphorylation reaction, the phosphoryl-group transfers involved in the forward and reverse phosphorelay can occur either intra- or inter-molecularly. In this review, we highlight some important features of bacterial TCS, with special emphasis on the autophosphorylation and phosphoryl-group transfer events. [ABSTRACT FROM AUTHOR]

Introduction: Alzheimer's disease (AD) is a progressive neurodegenerative disorder related to dementia and cognitive impairment. The research into potential therapies has shifted towards the inhibition of both α amyloid and tau aggregates. Objective: To update the research in the development of therapeutic strategies for AD based on the PαA and tau study. Method: PubMed database was used to search the required information using the related keywords. Immunohistochemistry was performed on AD brain tissue sections. Results: Due to its pathological relevance, the main research for the therapeutic strategies in AD are based on Aα and tau as following: decreasing Aα formation, reducing Aα levels, immunotherapy to Aα and tau, interfering or disrupting Aα and tau aggregates, inhibiting and activating kinase and phosphatase activity respectively, and stabilizing microtubules. Discussion and conclusion: the PαA formation and aggregation as well as the posttranslational modifications of tau that promotes its aggregation have shown to be key mechanisms for the AD onset, hence, to prevent the evolution of the disease it is essential to inhibit these processes in the early stages of the onset, but, these strategies have caused side effects blocking important physiological functions, thus leading to research approaches such as the inhibition of the aggregation of both PαA and tau, that seems to be the most efficient therapeutic strategy for AD. [ABSTRACT FROM AUTHOR]

Myotonic dystrophy type I or Steinert's disease is a multisystemic disease of autosomal dominant genetic origin, generated by an alteration at trinucletotide CTG expansion located in the 3' end of the gene DPKM (myotonic dystrophy protein kinase) on chromosome 19q13.3 with alterations in skeletal muscle, heart, eye, endocrine and, mainly, neurological. It has four clinical forms; its diagnosis is based on genetic studies, clinical data and electromyography. So far the treatment is just symptomatic and there are many ongoing studies of genetic translocations. This paper reports the case of a family with the Steinert's disease where six members were deceased secondary to the clinical manifestations of this disease. [ABSTRACT FROM AUTHOR]

Copyright of Revista Ciencias de la Salud is the property of Colegio Mayor de Nuestra Senora del Rosario and its content may not be copied or emailed to multiple sites or posted to a listserv without the copyright holder's express written permission. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)

Since 2003, the term orthotriccia has been used to define the application of shock waves in the therapy of musculoskeletal disorders. A shock wave (SW) is an acoustic or sonic wave producing its maximal pressure in few nanoseconds (ns). SW generates a high positive (>Mpa) and a negative pressure (5-10 Mpa) (Mpa=megapascal); having a short rise of 20-120 ns and a short pulse duration (5 ns). In contrast to ultrasound waves, SW have a low frequency and poor energy absorption by living tissues. SW travel trough soft and homogeneous tissues at 1.500 m/s speed experimenting low distortion. SW applied to bone tissue can stimulate its neoformation by increasing the activity of mitogen activated protein kinase (MAPK), signal regulated kinase (EPK) and P38 kinase; all of them involved in the mechanical stimulation of osteoblastic and chondrogenic growth and differentiation. Two neurophysiological models try to explain the analgesic mechanism of SW in orthopedics: the "control gate theory" and "hyperstimulation mediated analgesia" described in this review article. [ABSTRACT FROM AUTHOR]