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Topic Review
Therapeutic Antibodies Targeting Glycosylation
We generated a platform for designing optimized functional therapeutic antibodies against cancer glycans. The target tumor-associated carbohydrate antigen is commonly expressed in colon and pancreatic cancers. We developed a system for selection of potent antibodies by yeast surface display against this carbohydrate antigen, then showed that elite clones have potent affinity, specificity, cancer cell binding, and therapeutic efficacy. These tools have broad utility for manipulating and engineering antibodies against carbohydrate antigens, and provide major innovative avenues of research in the field of cancer therapy and diagnostics.
  • 975
  • 20 Oct 2020
Topic Review
Synthesis of Medicinally Relevant N-Heterocycles
N-heterocycles, both saturated and unsaturated, are ubiquitous biologically active molecules that are extremely appealing scaffolds in drug discovery programs. Although classical synthetic methods have been developed to access many relevant N-heterocyclic scaffolds, representing well-established and reliable routes, some do not meet the needs of sustainability. In this context, several advances have been made towards the sustainable synthesis of N-heterocycles.
  • 969
  • 12 Oct 2021
Topic Review
Relevance of Crystal Forms in the Pharmaceutical Field
The existence of multiple crystal forms of an active pharmaceutical ingredients (API) is relevant not only for the selection of the best solid material to carry through the various stages of drug development, including the choice of dosage and of excipients suitable for drug development and marketing, but also in terms of intellectual property protection and/or extension. This is because the physico-chemical properties, such as solubility, dissolution rate, thermal stability, processability, etc., of the solid API may depend, sometimes dramatically, on the crystal form, with important implications on the drug’s ultimate efficacy.
  • 968
  • 26 Aug 2022
Topic Review
MGluRI and ErbB Receptors
It is well-appreciated that phosphorylation is an essential post-translational mechanism of regulation for several proteins, including group 1 metabotropic glutamate receptors (mGluRI), mGluR1 and mGluR5 subtypes. While contributions of various serine/threonine protein kinases on mGluRI modulation have been recognized, the functional role of tyrosine kinases (TKs) is less acknowledged. Here, we describe current evidence on the modulatory roles of the ErbB tyrosine kinases receptors - activated by the neurotrophic factors neuregulins (NRGs) - on mGluRI function. Available evidence suggests that mGluRI activity is tightly dependent on ErbB signaling, and that ErbB's modulation profoundly influences mGluRI-dependent effects on neurotransmission, neuronal excitability, synaptic plasticity, and learning and memory processes. 
  • 966
  • 13 Nov 2020
Topic Review
De Novo Synthesized Estradiol
The estrogen estradiol is a potent neuroactive steroid that may regulate brain structure and function. Although the eff ects of estradiol have been historically associated with gonadal secretion, the discovery that this steroid may be synthesized within the brain has expanded this traditional concept. Indeed, it is accepted that de novo synthesized estradiol in the nervous system (nE2) may modulate several aspects of neuronal physiology, including synaptic transmission and plasticity, thereby influencing a variety of behaviors. These modulations may be on a time scale of minutes via non-classical and often membrane-initiated mechanisms or hours and days by classical actions on gene transcription. Besides the high level, recent investigations in the cerebellum indicate that even a low aromatase expression can be related to the fast nE2 eff ect on brain functioning. These pieces of evidence point to the importance of an on-demand and localized nE2 synthesis to rapidly contribute to regulating synaptic transmission. This review is geared at exploring a new scenario for the impact of estradiol on brain processes as it emerges from the nE2 action on cerebellar neurotransmission and cerebellum-dependent learning.
  • 967
  • 30 Oct 2020
Topic Review
Flecainide
Flecainide is an IC antiarrhythmic drug approved in 1984 from Food and Drug Administration for the suppression of sustained ventricular tachycardia and later for acute cardioversion of atrial fibrillation (AF) and for sinus rhythm maintenance. It is categorized as a Vaughn-Williams Class IC agent based upon its properties of causes a strong degree of sodium channel blockage with slowing cardiac conduction and a minimal effect on ventricular repolarization. Currently, flecainide is mostly used for sinus rhythm maintenance in atrial fibrillation patients without structural cardiomyopathy although recent studies enrolling different patient population demonstrated a good effectiveness and safety profile. 
  • 965
  • 13 Nov 2021
Topic Review
Polysaccharide-Based Materials
Polysaccharide-based materials created by physical processes have received considerable attention for biomedical applications. 
  • 964
  • 20 May 2021
Topic Review
PPIs' Drug Dosage Forms Development - Formulation Challenges
Proton Pump Inhibitors, also known as PPIs, belong to a group of antisecretory drugs. Since their introduction to pharmacotherapy, PPIs have been widely used in the treatment of numerous diseases manifested by excessive secretion of gastric acid. There are still unmet needs regarding their availability for patients of all age groups. Their poor stability hinders the development of formulations in which dose can be easily adjusted.
  • 961
  • 31 Oct 2022
Topic Review
Targeted Alpha Therapy
This article discusses the therapeutic advantages of Targeted Alpha Therapy (TAT), including the short and highly ionizing path of α-particle emissions; the ability of TAT to complement and provide superior efficacy over existing forms of radiotherapy; and the physical decay properties and radiochemistry of common α-emitters, including 225Ac, 213Bi, 224Ra, 212Pb, 227Th, 223Ra, 211At.
  • 961
  • 12 Jan 2021
Topic Review
Ischemia and Reperfusion
Ischemia and reperfusion (I/R) causes a reduction in arterial blood supply to tissues, followed by the restoration of perfusion and consequent reoxygenation. The reestablishment of blood flow triggers further damage to the ischemic tissue through reactive oxygen species (ROS) accumulation, interference with cellular ion homeostasis, and inflammatory responses to cell death. In normal conditions, ROS mediate important beneficial responses. When their production is prolonged or elevated, harmful events are observed with peculiar cellular changes. In particular, during I/R, ROS stimulate tissue inflammation and induce NLRP3 inflammasome activation. The mechanisms underlying the activation of NLRP3 are several and not completely elucidated. It was recently shown that NLRP3 might sense directly the presence of ROS produced by normal or malfunctioning mitochondria or indirectly by other activators of NLRP3. Aim of the present review is to describe the current knowledge on the role of NLRP3 in some organs (brain, heart, kidney, and testis) after I/R injury, with particular regard to the role played by ROS in its activation. Furthermore, as no specific therapy for the prevention or treatment of the high mortality and morbidity associated with I/R is available, the state of the art of the development of novel therapeutic approaches is illustrated.
  • 961
  • 03 Nov 2020
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