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Farnesyltransferase Inhibitor
The farnesyltransferase inhibitors (FTIs) are a class of experimental cancer drugs that target protein farnesyltransferase with the downstream effect of preventing the proper functioning of the Ras (protein), which is commonly abnormally active in cancer. Background Studies have suggested that interference with certain post-translational modification processes seem to have quite a high selectivity for targeting cells displaying tumour phenotypes, although the reason for this is a matter of controversy. After translation, Ras goes through four steps of modification: isoprenylation, proteolysis, methylation and palmitoylation. Isoprenylation involves the enzyme farnesyltransferase (FTase) transferring a farnesyl group from farnesyl pyrophosphate (FPP) to the pre-Ras protein. Also, a related enzyme geranylgeranyltransferase I (GGTase I) has the ability to transfer a geranylgeranyl group to K and N-Ras (the implications of this are discussed below). Farnesyl is necessary to attach R ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tipifarnib
Tipifarnib (INN, proposed trade name Zarnestra) is a farnesyltransferase inhibitor. Farnesyltransferase inhibitors block the activity of the farnesyltransferase enzyme by inhibiting prenylation of the CAAX tail motif, which ultimately prevents Ras from binding to the membrane, rendering it inactive. History The compound was discovered by Johnson & Johnson Pharmaceutical Research & Development, L.L.C, with registration number R115777. For treatment of progressive plexiform neurofibromas associated with neurofibromatosis type I, it passed phase I clinical trials but was suspended (NCT00029354) in phase II. Tipifarnib was submitted to the FDA by Johnson & Johnson for the treatment of AML in patients aged 65 and over with a new drug application (NDA) to the FDA on January 24, 2005. In June 2005, the FDA issued a "not approvable" letter for tipifarnib. Kura Oncology in-licensed tipifarnib from Janssen in 2014. Investigations Cancer The inhibitor is being investigated in pat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
FPT Inhibitor III
FPT may refer to: * Female pipe tapered; see National pipe thread * F/P/T, an acronym used by Canadian governments to designate a joint Special Advisory Committee of Federal/Provincial/Territorial civil servants * Fiat Powertrain Technologies, an Italian automotive company * Fixed-parameter tractability, in computer science * Florida Playwrights' Theatre, an erstwhile theatre group in Hollywood, Florida, United States * Forced perfect termination, in electronics * FPT Group, a Vietnamese IT company ** FPT Software, a Vietnamese software company * FPT Industries, an American aerospace engineering company * FPT University, in Vietnam * Full Pressure Turbo Automatic Performance Control (APC) was the first engine knock and boost control system. The APC was invented by Per Gillbrand at the Swedish car maker SAAB. SAAB introduced it on the turbo charged Saab H engines in 1982, and the APC was fitted ..., in Saab automobiles * Portuguese Tennis Federation (Portuguese: ') {{disa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
FPT Inhibitor II
FPT may refer to: * Female pipe tapered; see National pipe thread * F/P/T, an acronym used by Canadian governments to designate a joint Special Advisory Committee of Federal/Provincial/Territorial civil servants * Fiat Powertrain Technologies, an Italian automotive company * Fixed-parameter tractability, in computer science * Florida Playwrights' Theatre, an erstwhile theatre group in Hollywood, Florida, United States * Forced perfect termination, in electronics * FPT Group, a Vietnamese IT company ** FPT Software, a Vietnamese software company * FPT Industries, an American aerospace engineering company * FPT University, in Vietnam * Full Pressure Turbo Automatic Performance Control (APC) was the first engine knock and boost control system. The APC was invented by Per Gillbrand at the Swedish car maker SAAB. SAAB introduced it on the turbo charged Saab H engines in 1982, and the APC was fitted ..., in Saab automobiles * Portuguese Tennis Federation (Portuguese: ') {{disa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
FPT Inhibitor I
FPT may refer to: * Female pipe tapered; see National pipe thread * F/P/T, an acronym used by Canadian governments to designate a joint Special Advisory Committee of Federal/Provincial/Territorial civil servants * Fiat Powertrain Technologies, an Italian automotive company * Fixed-parameter tractability, in computer science * Florida Playwrights' Theatre, an erstwhile theatre group in Hollywood, Florida, United States * Forced perfect termination, in electronics * FPT Group, a Vietnamese IT company ** FPT Software, a Vietnamese software company * FPT Industries, an American aerospace engineering company * FPT University, in Vietnam * Full Pressure Turbo Automatic Performance Control (APC) was the first engine knock and boost control system. The APC was invented by Per Gillbrand at the Swedish car maker SAAB. SAAB introduced it on the turbo charged Saab H engines in 1982, and the APC was fitted ..., in Saab automobiles * Portuguese Tennis Federation (Portuguese: ') {{disa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clavaric Acid
Clavaric acid is a triterpenoid produced by the mushroom '' Hypholoma sublateritium''. Clavaric acid was discovered by Merck Research Laboratories in a random screening of natural extracts. Clavaric acid is a reversible farnesyltransferase inhibitor The farnesyltransferase inhibitors (FTIs) are a class of experimental cancer drugs that target protein farnesyltransferase with the downstream effect of preventing the proper functioning of the Ras (protein), which is commonly abnormally active in ... with an IC50 of 1.3 μM. References {{Reflist Lanostanes Triterpenes ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Progeria
Progeria is a specific type of progeroid syndrome, also known as Hutchinson–Gilford syndrome. A single gene mutation is responsible for progeria. The gene, known as lamin A (LMNA), makes a protein necessary for holding the Nucleus of the cell together. When this gene gets mutated an abnormal form of lamin A protein called Progerin is produced. Progeroid syndromes are a group of diseases that causes individuals to age faster than usual, leading to them appearing older than they actually are. Patients born with progeria typically live to an age of mid-teens to early twenties. Severe cardiovascular complications usually develop by puberty, resulting in death. Signs and symptoms Children with progeria usually develop the first symptoms during their first few months of life. The earliest symptoms may include a failure to thrive and a localized scleroderma-like skin condition. As a child ages past infancy, additional conditions become apparent, usually around 18–24 months. Limi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LMNA
Pre-lamin A/C or lamin A/C is a protein that in humans is encoded by the ''LMNA'' gene. Lamin A/C belongs to the lamin family of proteins. Function In the setting of ZMPSTE24 deficiency, the final step of lamin processing does not occur, resulting in an accumulation of farnesyl-prelamin A. In Hutchinson–Gilford progeria syndrome, a 50-amino acid deletion in prelamin A (amino acids 607–656) removes the site for the second endoproteolytic cleavage. Consequently, no mature lamin A is formed, and a farnesylated mutant prelamin A (progerin) accumulates in cells. The nuclear lamina consist of a two-dimensional matrix of proteins located next to the inner nuclear membrane. The lamin family of proteins make up the matrix and are highly conserved in evolution. During mitosis, the lamina matrix is reversibly disassembled as the lamin proteins are phosphorylated. Lamin proteins are thought to be involved in nuclear stability, chromatin structure and gene expression. Vertebrate l ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Progeria20132-300
Progeria is a specific type of progeroid syndrome, also known as Hutchinson–Gilford syndrome. A single gene mutation is responsible for progeria. The gene, known as lamin A (LMNA), makes a protein necessary for holding the Nucleus of the cell together. When this gene gets mutated an abnormal form of lamin A protein called Progerin is produced. Progeroid syndromes are a group of diseases that causes individuals to age faster than usual, leading to them appearing older than they actually are. Patients born with progeria typically live to an age of mid-teens to early twenties. Severe cardiovascular complications usually develop by puberty, resulting in death. Signs and symptoms Children with progeria usually develop the first symptoms during their first few months of life. The earliest symptoms may include a failure to thrive and a localized scleroderma-like skin condition. As a child ages past infancy, additional conditions become apparent, usually around 18–24 months. Limite ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Geranylgeranyltransferase I
Geranylgeranyltransferase type 1 or simply geranylgeranyltransferase is one of the three enzymes in the prenyltransferase group. In specific terms, Geranylgeranyltransferase (GGTase 1) adds a 20-carbon isoprenoid called a geranylgeranyl group to proteins bearing a CaaX motif: a four-amino acid sequence at the carboxyl terminal of a protein. Geranylgeranyltransferase inhibitors are being investigated as anti-cancer agents. Function Prenyltransferases, including geranylgeranyltransferase, posttranslationally modify proteins by adding an isoprenoid lipid called a prenyl group to the carboxyl terminus of the target protein. This process, called prenylation, causes prenylated proteins to become membrane-associated due to the hydrophobic nature of the prenyl group. Most prenylated proteins are involved in cellular signaling, wherein membrane association is critical for function. Structure Geranylgeranyltransferase contains two subunits, α and β that are encoded by the ''FNT ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Malaria
Malaria is a mosquito-borne infectious disease that affects humans and other animals. Malaria causes symptoms that typically include fever, tiredness, vomiting, and headaches. In severe cases, it can cause jaundice, seizures, coma, or death. Symptoms usually begin ten to fifteen days after being bitten by an infected mosquito. If not properly treated, people may have recurrences of the disease months later. In those who have recently survived an infection, reinfection usually causes milder symptoms. This partial resistance disappears over months to years if the person has no continuing exposure to malaria. Malaria is caused by single-celled microorganisms of the ''Plasmodium'' group. It is spread exclusively through bites of infected ''Anopheles'' mosquitoes. The mosquito bite introduces the parasites from the mosquito's saliva into a person's blood. The parasites travel to the liver where they mature and reproduce. Five species of ''Plasmodium'' can infect and be spread by h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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