Iwao Ojima
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Iwao Ojima
Iwao Ojima (born June 5, 1945, in Japan) is a Japanese-American chemist and university distinguished professor at the State University of New York at Stony Brook (Stony Brook University). He has been widely recognized for his seminal contributions to a range of chemical research at the multifaceted interfaces of chemical synthesis and life sciences. As rare accomplishments, he has received four National Awards from the American Chemical Society in four different fields of research. He is also serving as the director of the Institute of Chemical Biology and Drug Discovery (ICB&DD), as well as the president of the Stony Brook Chapter of the National Academy of Inventors. Biography Ojima was born in Yokohama, Japan, in 1945 and educated at the University of Tokyo, Japan (B.S. 1968, Ph.D. 1973).  Before coming to the U.S. as an associate professor at the State University of New York at Stony Brook in 1983, he worked at the Sagami Institute of Chemical Research in Japan, first as a re ...
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Ernest Guenther Award
The Ernest Guenther Award in the Chemistry of Natural Products is an American Chemical Society (ACS) award in the field of the chemistry of natural products. The purpose of the award is to recognize and encourage outstanding achievements in the analysis, structure elucidation, and chemical synthesis of natural products, with special consideration given to the independence of thought and originality. The award is granted regardless of race, gender, age, religion, ethnicity, nationality, sexual orientation, gender expression, gender identity, presence of disabilities, and educational background. The award consists of $6,000, a medallion, and a certificate. The medallion is presented during an award address. The award was established in 1948 by Fritzsche Dodge and Olcott Inc. to mark the 75th anniversary of the founding of the company. Since 1969,''Fritsche Award in Essential Oils Named for Dr. Guenther.'' In: ''Journal of the American Oil Chemists' Society.'' 44, 1967, S. A626– ...
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Captopril
Captopril, sold under the brand name Capoten among others, is an ACE inhibitor, angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of congestive heart failure. Captopril was the first oral ACE inhibitor found for the treatment of hypertension. It does not cause fatigue as associated with beta-blockers. Due to the adverse drug event of causing hyperkalemia, as seen with most ACE Inhibitors, the medication is usually paired with a diuretic. Captopril was patented in 1976 and approved for medical use in 1980. Structure–activity relationship Captopril has an L-proline group which allows for it to be more bioavailable within oral formulations. The thiol moiety within the molecule has been associated with two significance adverse effects: the hapten or immune response. This immune response, also known as agranulocytosis, can explain the adverse drug events which may be seen in captopril with the allergic response, which would be: hi ...
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Microtubule
Microtubules are polymers of tubulin that form part of the cytoskeleton and provide structure and shape to eukaryotic cells. Microtubules can be as long as 50 micrometres, as wide as 23 to 27  nm and have an inner diameter between 11 and 15 nm. They are formed by the polymerization of a dimer of two globular proteins, alpha and beta tubulin into protofilaments that can then associate laterally to form a hollow tube, the microtubule. The most common form of a microtubule consists of 13 protofilaments in the tubular arrangement. Microtubules play an important role in a number of cellular processes. They are involved in maintaining the structure of the cell and, together with microfilaments and intermediate filaments, they form the cytoskeleton. They also make up the internal structure of cilia and flagella. They provide platforms for intracellular transport and are involved in a variety of cellular processes, including the movement of secretory vesicles, organell ...
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Pharmacophore
300px, An example of a pharmacophore model. A pharmacophore is an abstract description of molecular features that are necessary for molecular recognition of a ligand by a biological macromolecule. IUPAC defines a pharmacophore to be "an ensemble of steric and electronic features that is necessary to ensure the optimal supramolecular interactions with a specific biological target and to trigger (or block) its biological response". A pharmacophore model explains how structurally diverse ligands can bind to a common receptor site. Furthermore, pharmacophore models can be used to identify through de novo design or virtual screening novel ligands that will bind to the same receptor. Features Typical pharmacophore features include hydrophobic centroids, aromatic rings, hydrogen bond acceptors or donors, cations, and anions. These pharmacophoric points may be located on the ligand itself or may be projected points presumed to be located in the receptor. The features need to match ...
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Structure–activity Relationship
The structure–activity relationship (SAR) is the relationship between the chemical structure of a molecule and its biological activity. This idea was first presented by Crum-Brown and Fraser in 1865. The analysis of SAR enables the determination of the chemical group responsible for evoking a target biological effect in the organism. This allows modification of the effect or the potency of a bioactive compound (typically a drug) by changing its chemical structure. Medicinal chemists use the techniques of chemical synthesis to insert new chemical groups into the biomedical compound and test the modifications for their biological effects. This method was refined to build mathematical relationships between the chemical structure and the biological activity, known as quantitative structure–activity relationships (QSAR). A related term is structure affinity relationship (SAFIR). Structure-biodegradability relationship The large number of synthetic organic chemicals currently in prod ...
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Ortataxel
Ortataxel is a drug used in chemotherapy. , Spectrum Pharmaceuticals Spectrum Pharmaceuticals is an American biopharmaceutical company. The company is located in Boston, MA. Drugs Spectrum develops and markets drugs for treatments in hematology and oncology. In January 2019, Spectrum sold off its entire comme ... has the drug in a Phase 2 clinical trial. References Mitotic inhibitors Benzoate esters Carbamates Secondary alcohols Lactones Acetate esters Taxanes {{antineoplastic-drug-stub ...
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Taxol
Paclitaxel (PTX), sold under the brand name Taxol among others, is a chemotherapy medication used to treat a number of types of cancer. This includes ovarian cancer, esophageal cancer, breast cancer, lung cancer, Kaposi's sarcoma, cervical cancer, and pancreatic cancer. It is administered by intravenous injection. There is also an albumin-bound formulation. Common side effects include hair loss, bone marrow suppression, numbness, allergic reactions, muscle pains, and diarrhea. Other serious side effects include heart problems, increased risk of infection, and lung inflammation. There are concerns that use during pregnancy may cause birth defects. Paclitaxel is in the taxane family of medications. It works by interference with the normal function of microtubules during cell division. Paclitaxel was first isolated in 1971 from the Pacific yew and approved for medical use in 1993. It is on the World Health Organization's List of Essential Medicines. It has been made from p ...
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Ojima Lactam
Ojima may refer to: *Ojima (surname), a Japanese surname *Ojima, Gunma, a town merged into the city of Ōta, Gunma Prefecture, Japan *Ojima Station, a railway station in Kōtō, Tokyo, Japan *Higashi-ojima Station, a railway station in Kōtō, Tokyo, Japan *Nishi-ojima Station, a railway station in Kōtō, Tokyo, Japan *Ojima Domain, also known as Kojima Domain, a Japanese domain of the Edo period *Ojima River, a tributary of Turgeon Lake in Quebec, Canada * Rivière-Ojima, Quebec, an unorganized territory of RCM Abitibi-Ouest, in Quebec, Canada *Ou Island, an island in Okinawa, Japan See also *Ojima lactam Ojima may refer to: *Ojima (surname), a Japanese surname *Ojima, Gunma, a town merged into the city of Ōta, Gunma Prefecture, Japan *Ojima Station, a railway station in Kōtō, Tokyo, Japan *Higashi-ojima Station, a railway station in Kōtō, Toky ...
, an organic compound of some importance in the commercial production of Taxol {{Disambiguation, geo ...
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Taxane
Taxanes are a class of diterpenes. They were originally identified from plants of the genus ''Taxus'' (yews), and feature a taxadiene core. Paclitaxel (Taxol) and docetaxel (Taxotere) are widely used as chemotherapy agents. Cabazitaxel was FDA approved to treat hormone-refractory prostate cancer. Taxanes present difficulties in formulation as medicines because they are poorly soluble in water. Production As their name suggests, taxanes were first derived from natural sources, but some have been semisynthesized. Paclitaxel was originally derived from the Pacific yew tree. Taxanes are difficult to synthesize because of their numerous chiral centres—taxol has 11 of these. Recently, the presence of taxanes in the shells and leaves of ''Corylus avellana'' (the common hazel plant) has been reported. Mechanism of action The principal mechanism of action of the taxane class of drugs is the disruption of microtubule function. Microtubules are essential to cell division, and ta ...
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Peptidomimetic
A peptidomimetic is a small protein-like chain designed to mimic a peptide. They typically arise either from modification of an existing peptide, or by designing similar systems that mimic peptides, such as peptoids and Beta-peptide, β-peptides. Irrespective of the approach, the altered chemical structure is designed to advantageously adjust the molecular properties such as stability or biological activity. This can have a role in the development of drug-like compounds from existing peptides. Peptidomimetics can be prepared by cyclization of linear peptides or coupling of stable unnatural amino acids. These modifications involve changes to the peptide that will not occur naturally (such as altered backbones and the incorporation of nonnatural amino acids). Unnatural amino acids can be generated from their native analogs via modifications such as amine alkylation, side chain substitution, structural bond extension cyclization, and isosteric replacements within the amino acid backb ...
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Oligopeptide
An oligopeptide, often just called peptide ('' oligo-'', "a few"), consists of two to twenty amino acids and can include dipeptides, tripeptides, tetrapeptides, and pentapeptides. Some of the major classes of naturally occurring oligopeptides include aeruginosins, cyanopeptolins, microcystins, microviridins, microginins, anabaenopeptins, and cyclamides. Microcystins are best studied, because of their potential toxicity impact in drinking water. A review of some oligopeptides found that the largest class are the cyanopeptolins (40.1%), followed by microcystins (13.4%). Production Oligopeptide classes are produced by nonribosomal peptides synthases (NRPS), except cyclamides and microviridins are synthesized through ribosomic pathways. Examples Examples of oligopeptides include: * Amanitins - Cyclic peptides taken from carpophores of several different mushroom species. They are potent inhibitors of RNA polymerases in most eukaryotic species, the prevent the production of mRNA a ...
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