Medicinal chemistry
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Medicinal chemistry · Feb 2018
ReviewManaging Neuropathic Pain in Multiple Sclerosis: Pharmacological Interventions.
Multiple sclerosis (MS) is a chronic inflammatory demyelinating disease of the central nervous system (CNS). Of the plethora of motor and sensory disturbances experienced by sufferers, neuropathic pain is a highly prevalent and debilitating symptom, and at present remains extremely difficult to treat. Common forms of neuropathic pain seen in MS patients include central neuropathic pain, Lhermitte's phenomenon and trigeminal neuralgia, which are all speculated to arise from specific patterns of lesion formation. ⋯ Studies aimed at understanding the mechanisms underlying EAE-induced neuropathic pain and investigating the efficacy of novel pharmacological interventions at the animal level offer an exciting area of future research, and may inform future therapeutic options for MS-associated neuropathic pain.
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Medicinal chemistry · Jan 2017
ReviewApplication of Machine Learning Approaches for Protein-protein Interactions Prediction.
Proteomics endeavors to study the structures, functions and interactions of proteins. Information of the protein-protein interactions (PPIs) helps to improve our knowledge of the functions and the 3D structures of proteins. Thus determining the PPIs is essential for the study of the proteomics. ⋯ This review presents the application of machine learning approaches in predicting PPI. Many examples of success in identification and prediction in the area of PPI prediction have been discussed, and the PPIs research is still in progress.
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The approach to the axilla is an evolving paradigm, and recognition of the complexity of breast cancer (BC) biology is changing treatment options. The sentinel lymph node biopsy (SLNB) technique is based on the excision and histological examination of the axillary lymph nodes(s), which is assumed to be the first one draining from the primary tumor. SLNB can accurately stage the axilla, and several trials have shown that there are no significant differences in local recurrence and overall survival between patients treated with or without axillary node dissection (ALND) after a negative SLNB. ⋯ Micrometastatic disease can be safely managed with SLNB alone, and additional identification of micrometastases with immunohistochemistry does not affect disease-free survival or overall survival. An appropriate management of the axilla is crucial for the outcome of patients with early BC, and SLNB introduction into the clinical practice dramatically changed the surgical treatment, reducing morbidity without decreasing survival. A tailored approach should be suggested in each patient with BC, considering the biology of the tumor rather than nodal involvement.
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Oseltamivir (has known by its brand name 'Tamiflu') is a prodrug, requiring ester hydrolysis for conversion to the active form, Oseltamivir carboxylate. Oseltamivir was the first orally active neuraminidase inhibitor commercially developed by US based Gilead Sciences and is currently marketed by F. Hoffmann-La Roche (Roche). ⋯ Orally Oseltamivir is well tolerated and effective in treatment of influenza in adolescents and adults, including the elderly and patients with chronic cardiac and/or respiratory disease. Many of the pharmaceutical companies targeted Oseltamivir as a block buster molecule. In present review, we have tried to cover chemistry, mode of binding, total synthesis, current patent status, adverse effect and clinical status of Oseltamivir giving emphasis on medicinal chemistry aspect.
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Medicinal chemistry · May 2005
ReviewProtein phosphorylation and signal transduction modulation: chemistry perspectives for small-molecule drug discovery.
Protein phosphorylation has been exploited by Nature in profound ways to control various aspects of cell proliferation, differentiation, metabolism, survival, motility and gene transcription. Cellular signal transduction pathways involve protein kinases, protein phosphatases, and phosphoprotein-interacting domain (e.g., SH2, PTB, WW, FHA, 14-3-3) containing cellular proteins to provide multidimensional, dynamic and reversible regulation of many biological activities. ⋯ Noteworthy studies related to molecular genetics, signal transduction pathways, structural biology, and drug design for several of these therapeutic targets are highlighted. Some exemplary proof-of-concept lead compounds, clinical candidates and/or breakthrough medicines are further detailed to illustrate achievements as well as challenges in the generation, optimization and development of small-molecule inhibitors of protein kinases, protein phosphatases or phosphoprotein-interacting domain containing cellular proteins.