Search Results - "Ebetino, Frank H."
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The relationship between the chemistry and biological activity of the bisphosphonates
Published in Bone (New York, N.Y.) (01-07-2011)“…Abstract The ability of bisphosphonates ((HO)2 P(O)CR1 R2 P(O)(OH)2 ) to inhibit bone resorption has been known since the 1960s, but it is only recently that a…”
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Real-Time Impedance-Based Monitoring of the Growth and Inhibition of Osteomyelitis Biofilm Pathogen Staphylococcus aureus Treated with Novel Bisphosphonate-Fluoroquinolone Antimicrobial Conjugates
Published in International journal of molecular sciences (19-01-2023)“…Osteomyelitis is a limb- and life-threatening orthopedic infection predominantly caused by biofilms. Bone infections are extremely challenging to treat…”
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The Molecular Mechanism of Nitrogen-Containing Bisphosphonates as Antiosteoporosis Drugs
Published in Proceedings of the National Academy of Sciences - PNAS (16-05-2006)“…Osteoporosis and low bone mass are currently estimated to be a major public health risk affecting > 50% of the female population over the age of 50. Because of…”
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Rescue bisphosphonate treatment of alveolar bone improves extraction socket healing and reduces osteonecrosis in zoledronate-treated mice
Published in Bone (New York, N.Y.) (01-06-2019)“…Bisphosphonate (BP)-related osteonecrosis of the jaw, previously known as BRONJ, now referred to more broadly as medication-related osteonecrosis of the jaw…”
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Influence of bone affinity on the skeletal distribution of fluorescently labeled bisphosphonates in vivo
Published in Journal of bone and mineral research (01-04-2012)“…Bisphosphonates are widely used antiresorptive drugs that bind to calcium. It has become evident that these drugs have differing affinities for bone mineral;…”
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Bisphosphonate drugs have actions in the lung and inhibit the mevalonate pathway in alveolar macrophages
Published in eLife (30-12-2021)“…Bisphosphonates drugs target the skeleton and are used globally for the treatment of common bone disorders. Nitrogen-containing bisphosphonates act by…”
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Hydroxychloroquine and a low antiresorptive activity bisphosphonate conjugate prevent and reverse ovariectomy-induced bone loss in mice through dual antiresorptive and anabolic effects
Published in Bone Research (05-09-2024)“…Osteoporosis remains incurable. The most widely used antiresorptive agents, bisphosphonates (BPs), also inhibit bone formation, while the anabolic agent,…”
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Fluorescent Bisphosphonate and Carboxyphosphonate Probes: A Versatile Imaging Toolkit for Applications in Bone Biology and Biomedicine
Published in Bioconjugate chemistry (17-02-2016)“…A bone imaging toolkit of 21 fluorescent probes with variable spectroscopic properties, bone mineral binding affinities, and antiprenylation activities has…”
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Bisphosphonate use in the horse: what is good and what is not?
Published in BMC veterinary research (24-06-2019)“…Bisphosphonates (BPs) are a family of molecules characterized by two key properties: their ability to bind strongly to bone mineral and their inhibitory…”
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Efficacy of Bisphosphonate-Conjugated Sitafloxacin in a Murine Model of S. aureus Osteomyelitis: Evidence of "Target & Release" Kinetics and Killing of Bacteria Within Canaliculi
Published in Frontiers in cellular and infection microbiology (24-06-2022)“…infection of bone is difficult to eradicate due to its ability to colonize the osteocyte-lacuno-canalicular network (OLCN), rendering it resistant to…”
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Synthesis of a Bone-Targeted Bortezomib with In Vivo Anti-Myeloma Effects in Mice
Published in Pharmaceutics (10-09-2018)“…Multiple myeloma (MM) is the most common cancer affecting the bone and bone marrow and remains incurable for most patients; novel therapies are therefore…”
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Inhibition of Protein Prenylation by Bisphosphonates Causes Sustained Activation of Rac, Cdc42, and Rho GTPases
Published in Journal of bone and mineral research (01-05-2006)“…N‐BPs, which inhibit bone resorption by preventing prenylation of small GTPases, unexpectedly cause the accumulation of GTP‐bound, unprenylated Rho family…”
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How Do Bisphosphonates Inhibit Bone Metastasis In Vivo
Published in Neoplasia (New York, N.Y.) (01-07-2010)“…Bisphosphonates are potent inhibitors of osteoclast-mediated bone resorption and have demonstrated clinical utility in the treatment of patients with…”
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Evidence of bisphosphonate-conjugated sitafloxacin eradication of established methicillin-resistant S. aureus infection with osseointegration in murine models of implant-associated osteomyelitis
Published in Bone Research (18-10-2023)“…Eradication of MRSA osteomyelitis requires elimination of distinct biofilms. To overcome this, we developed bisphosphonate-conjugated sitafloxacin (BCS,…”
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The Pharmacological Profile of a Novel Highly Potent Bisphosphonate, OX14 (1‐Fluoro‐2‐(Imidazo‐[1,2‐α]Pyridin‐3‐yl)‐Ethyl‐Bisphosphonate)
Published in Journal of bone and mineral research (01-09-2017)“…ABSTRACT Bisphosphonates are widely used in the treatment of clinical disorders characterized by increased bone resorption, including osteoporosis, Paget's…”
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A Bisphosphonate With a Low Hydroxyapatite Binding Affinity Prevents Bone Loss in Mice After Ovariectomy and Reverses Rapidly With Treatment Cessation
Published in JBMR plus (01-04-2021)“…ABSTRACT Bisphosphonates (BPs) are a mainstay of osteoporosis treatment; however, concerns about bone health based on oversuppression of remodeling remain…”
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Fluorescent risedronate analogue 800CW-pRIS improves tooth extraction-associated abnormal wound healing in zoledronate-treated mice
Published in Communications medicine (05-09-2022)“…Background Bisphosphonate-related osteonecrosis of the jaw (BRONJ) is a rare but serious side effect of nitrogen-containing bisphosphonate drugs (N-BPs)…”
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Development of Bisphosphonate-Conjugated Antibiotics to Overcome Pharmacodynamic Limitations of Local Therapy: Initial Results with Carbamate Linked Sitafloxacin and Tedizolid
Published in Antibiotics (Basel) (17-06-2021)“…The use of local antibiotics to treat bone infections has been questioned due to a lack of clinical efficacy and emerging information about Staphylococcus…”
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Synthesis, Chiral High Performance Liquid Chromatographic Resolution and Enantiospecific Activity of a Potent New Geranylgeranyl Transferase Inhibitor, 2-Hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic Acid
Published in Journal of medicinal chemistry (13-05-2010)“…3-(3-Pyridyl)-2-hydroxy-2-phosphonopropanoic acid (3-PEHPC, 1) is a phosphonocarboxylate (PC) analogue of 2-(3-pyridyl)-1-hydroxyethylidenebis(phosphonic acid)…”
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