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Consideration of the rate of product
2024-05-17

Consideration of the rate of product formation at different substrate concentrations and estimation of Michaelis-Menten parameters gives some insight into the possible mechanisms underlying the observed decreases in enzyme activity. Estimates based on two-substrate concentrations lack precision and
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A key building block in MT SGL is the
2024-05-17

A key building block in MT-SGL is the computation of the proximal operator in (12) when is the multi-task sparse group lasso regularizer given byFor MT-SGL, the iterates x ≡ Θ are matrices, and the proximal operator is computed at z ≡ Z = Θ + α(Θ − Θ). For the loss function L(·) corresponding to Ga
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For the first series we decided to verify
2024-05-17

For the first series we decided to verify the effects induced, on the ALR2 inhibitory properties, of an additional steric hindrance on the carbon in α position with respect to the carboxylic group, by introducing a methyl group (R2=Me). Therefore, we synthesized a series of new α-alanine derivatives
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br Introduction Diabetes mellitus DM
2024-05-17

Introduction Diabetes mellitus (DM) is a chronic metabolic disorder characterized by elevated levels of glucose in the blood. Type 1 diabetes is characterized by insufficient insulin production and needs a daily administration of insulin. Actually, no prevention is known for Type 1 diabetes. Type
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For the first series we decided to verify
2024-05-17

For the first series we decided to verify the effects induced, on the ALR2 inhibitory properties, of an additional steric hindrance on the carbon in α position with respect to the carboxylic group, by introducing a methyl group (R2=Me). Therefore, we synthesized a series of new α-alanine derivatives
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Within the PARP family TIPARP is most evolutionarily conserv
2024-05-17

Within the PARP family, TIPARP is most evolutionarily conserved with PARP12 (ARTD12) and PARP13 (ARTD13) [27,28,41]. All three proteins contain at least one RNA-type CCCH zinc finger domain, a poly-ADP-ribose binding WWE domain and a PARP catalytic domain (Fig. 1). PARP13 is catalytically inactive,
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br Hypothesis The hypothesis is that AhR in skin diseases
2024-05-17

Hypothesis The hypothesis is that AhR in skin diseases could be an objective of study for future dermatological therapies. Both stimulation and inhibition of the receptor might have significant influences on neoplastic or inflammatory skin diseases. However, at present the functions of AhR are un
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The inflammatory cytokine IL is an additional
2024-05-17

The inflammatory cytokine IL-6 is an additional factor that has been hypothesized to contribute to epinephrine-mediated repression of drug detoxifying proteins such as CYP3A4 (Aninat et al., 2008). Indeed, this CYP is well-known to be repressed by IL-6 (Dickmann et al., 2011) and epinephrine has pre
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br ACK inhibitors Since ACK activation
2024-05-17

ACK1 inhibitors Since ACK1 activation is correlated with poor prognosis in various cancers, strong efforts are being directed by multiple groups towards developing highly potent and specific small molecule inhibitors targeting the ACK1 kinase. At least eight small molecule kinase inhibitors have
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At present drugs that specifically inhibit YAP activity
2024-05-17

At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhib
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IC values were obtained for an expanded
2024-05-16

IC50 values were obtained for an expanded version of the fragment library using the previously described mobility shift assay. Subsequently, Ki values were estimated from IC50 values to allow better comparison of the activity against targets which were measured at different substrate concentrations
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It was previously demonstrated that dissociation
2024-05-16

It was previously demonstrated that dissociation of the V-ATPase in response to glucose depletion in yeast requires an intact microtubular network [28] and a catalytically active enzyme [29]. Interestingly, mutations in the non-homologous region of the catalytic subunit A are able to block dissociat
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Recently competitive inhibitors of arginase have been develo
2024-05-16

Recently, competitive inhibitors of arginase have been developed which have greater specificity for the enzyme. Initial development of these compounds involved determination of the crystal structure of arginase. Christianson and colleagues found that a binuclear manganese cluster was required for ca
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br Economics consequences of antibiotic resistance
2024-05-16

Economics consequences of antibiotic resistance in a SICU In the era of cost-containment, surgeons also need to consider the economic impact of antibiotic resistance in the surgical patient. Antibiotic-resistant infections are more difficult to treat, are more costly and more likely to be fatal t
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Introduction Antimicrobial resistance is a growing
2024-05-16

Introduction Antimicrobial resistance is a growing health threat worldwide that has been associated with incorrect prescription and overuse of prostaglandin receptor [1]. Considering that physicians play a central role in antibiotic usage, a better understanding of their prescribing behaviours and
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