134 relations: ABL (gene), Acetylene, Adenosine triphosphate, Adherence (medicine), Adverse effect, Amino acid, Aminothiazole, Aniline, Apoptosis, Arene substitution pattern, ARIAD Pharmaceuticals, Aryl, Aspartic acid, Backbone chain, Bafetinib, BCR (gene), Bcr-Abl tyrosine-kinase inhibitor, Blastic phase chronic myelogenous leukemia, Blood proteins, Bosutinib, Bromine, Busulfan, C-terminus, Carboxamide, Carboxylic acid, Cell growth, Chemical structure, Chemotherapy, Chlorine, Chromosome 22, Chromosome 9, Chronic myelogenous leukemia, Chronic phase chronic myelogenous leukemia, Chronology, Cyclopentane, Cyclopropane, Cytosine, Cytotoxicity, Dasatinib, Docking (molecular), Drug design, Drug intolerance, Drug resistance, Ethynyl radical, Fluorine, Food and Drug Administration, Fusion gene, Gene, Gene duplication, Genetic code, ..., Glutamic acid, Glycine, Helix, Hematology, High-throughput screening, Histidine, Human genome, Hydrochloride, Hydrogen bond, Hydrophile, Hydrophobe, Hydroxy group, Hydroxycarbamide, Hypothesis, IC50, Imatinib, Imidazole, Immortalised cell line, Immunosuppressive drug, In vitro, Interferon, Isoleucine, Lead compound, Leucine, Lipophilicity, Metabolic pathway, Methionine, Methoxy group, Missense mutation, Molar concentration, Molecular cloning, Molecule, Nilotinib, Nitrile, Novartis, Nucleic acid sequence, Nucleotide, Oncogene, Oxygen, P-glycoprotein, Partition coefficient, Pathogenesis, Pharmacotherapy, Phenylalanine, Philadelphia chromosome, Phosphorylation, Piperazine, Plasma protein binding, Point mutation, Ponatinib, Potency (pharmacology), Protein domain, Purine, Pyridazine, Pyridine, Pyrimidine, Quinazoline, Quinoline, Retrospective, SH2 domain, SLC22A1, Solubility, Sonogashira coupling, Src family kinase, Steric effects, Structural biology, Synergy, Therapy, Thermodynamic activity, Thiazole, Thiophene, Three-dimensional space, Threonine, Thymine, Time (magazine), Two-dimensional space, Tyrosine, Tyrosine-kinase inhibitor, Valine, Van der Waals force, Vinyl group, Walker motifs, X-ray crystallography, 2-Butyne. Expand index (84 more) » « Shrink index
Abelson murine leukemia viral oncogene homolog 1 also known as ABL1 is a protein that, in humans, is encoded by the ABL1 gene (previous symbol ABL) located on chromosome 9.
Acetylene (systematic name: ethyne) is the chemical compound with the formula C2H2.
Adenosine triphosphate (ATP) is a complex organic chemical that participates in many processes.
In medicine, compliance (also adherence, capacitance) describes the degree to which a patient correctly follows medical advice.
In medicine, an adverse effect is an undesired harmful effect resulting from a medication or other intervention such as surgery.
Amino acids are organic compounds containing amine (-NH2) and carboxyl (-COOH) functional groups, along with a side chain (R group) specific to each amino acid.
2-Aminothiazole is a heterocyclic amine featuring an thiazole core.
Aniline is an organic compound with the formula C6H5NH2.
Apoptosis (from Ancient Greek ἀπόπτωσις "falling off") is a process of programmed cell death that occurs in multicellular organisms.
Arene substitution patterns are part of organic chemistry IUPAC nomenclature and pinpoint the position of substituents other than hydrogen in relation to each other on an aromatic hydrocarbon.
ARIAD Pharmaceuticals, Inc. was an American oncology company, now part of Takeda Oncology, which was founded in 1991 by Harvey J. Berger, M.D. and headquartered in Cambridge, Massachusetts.
In the context of organic molecules, aryl is any functional group or substituent derived from an aromatic ring, usually an aromatic hydrocarbon, such as phenyl and naphthyl.
Aspartic acid (symbol Asp or D; salts known as aspartates), is an α-amino acid that is used in the biosynthesis of proteins.
In polymer science, the backbone chain of a polymer is the longest series of covalently bonded atoms that together create the continuous chain of the molecule.
Bafetinib (NS-187) is an experimental cancer drug developed by Nippon Shinyaku and licensed to CytRx.
The breakpoint cluster region protein (BCR) also known as renal carcinoma antigen NY-REN-26 is a protein that in humans is encoded by the BCR gene.
Bcr-Abl tyrosine-kinase inhibitors (TKI) are the first-line therapy for most patients with chronic myelogenous leukemia (CML).
Blastic phase chronic myelogenous leukemia is a phase of chronic myelogenous leukemia in which more than 30% of the cells in the blood or bone marrow are blast cells (immature blood cells).
Blood proteins, also termed plasma proteins, are proteins present in blood plasma.
Bosutinib (rINN/USAN; codenamed SKI-606, marketed under the trade name Bosulif) is a small molecule BCR-ABL and src tyrosine kinase inhibitor used for the treatment of chronic myelogenous leukemia.
Bromine is a chemical element with symbol Br and atomic number 35.
Busulfan (Myleran, GlaxoSmithKline, Busulfex IV, Otsuka America Pharmaceutical, Inc.) is a cancer drug, in use since 1959.
The C-terminus (also known as the carboxyl-terminus, carboxy-terminus, C-terminal tail, C-terminal end, or COOH-terminus) is the end of an amino acid chain (protein or polypeptide), terminated by a free carboxyl group (-COOH).
In organic chemistry carboxamides (or amino carbonyls) are functional groups with the general structure R-CO-NR'R′′ with R, R', and R′′ as organic substituents, or hydrogen.
A carboxylic acid is an organic compound that contains a carboxyl group (C(.
The term cell growth is used in the contexts of biological cell development and cell division (reproduction).
A chemical structure determination includes a chemist's specifying the molecular geometry and, when feasible and necessary, the electronic structure of the target molecule or other solid.
Chemotherapy (often abbreviated to chemo and sometimes CTX or CTx) is a type of cancer treatment that uses one or more anti-cancer drugs (chemotherapeutic agents) as part of a standardized chemotherapy regimen.
Chlorine is a chemical element with symbol Cl and atomic number 17.
Chromosome 22 is one of the 23 pairs of chromosomes in human cells.
Chromosome 9 is one of the 23 pairs of chromosomes in humans.
Chronic myelogenous leukemia (CML), also known as chronic myeloid leukemia, is a cancer of the white blood cells.
Chronic phase chronic myelogenous leukemia is a phase of chronic myelogenous leukemia in which 5% or fewer of the cells in the blood and bone marrow are blast cells (immature blood cells).
Chronology (from Latin chronologia, from Ancient Greek χρόνος, chrónos, "time"; and -λογία, -logia) is the science of arranging events in their order of occurrence in time.
Cyclopentane is a highly flammable alicyclic hydrocarbon with chemical formula C5H10 and CAS number 287-92-3, consisting of a ring of five carbon atoms each bonded with two hydrogen atoms above and below the plane.
Cyclopropane is a cycloalkane molecule with the molecular formula C3H6, consisting of three carbon atoms linked to each other to form a ring, with each carbon atom bearing two hydrogen atoms resulting in D3h molecular symmetry.
Cytosine (C) is one of the four main bases found in DNA and RNA, along with adenine, guanine, and thymine (uracil in RNA).
Cytotoxicity is the quality of being toxic to cells.
Dasatinib, sold under the brand name Sprycel, is a chemotherapy medication used to treat certain cases of chronic myelogenous leukemia (CML) and acute lymphoblastic leukemia (ALL).
In the field of molecular modeling, docking is a method which predicts the preferred orientation of one molecule to a second when bound to each other to form a stable complex.
Drug design, often referred to as rational drug design or simply rational design, is the inventive process of finding new medications based on the knowledge of a biological target.
Drug intolerance or drug sensitivity refers to an inability to tolerate the adverse effects of a medication, generally at therapeutic or subtherapeutic doses.
Drug resistance is the reduction in effectiveness of a medication such as an antimicrobial or an antineoplastic in curing a disease or condition.
The ethynyl radical (systematically named λ3-ethyne and hydridodicarbon(C—C)) is an organic compound with the chemical formula C≡CH (also written or). It is a simple molecule that does not occur naturally on Earth but is abundant in the interstellar medium.
Fluorine is a chemical element with symbol F and atomic number 9.
The Food and Drug Administration (FDA or USFDA) is a federal agency of the United States Department of Health and Human Services, one of the United States federal executive departments.
A fusion gene is a hybrid gene formed from two previously separate genes.
In biology, a gene is a sequence of DNA or RNA that codes for a molecule that has a function.
Gene duplication (or chromosomal duplication or gene amplification) is a major mechanism through which new genetic material is generated during molecular evolution.
The genetic code is the set of rules used by living cells to translate information encoded within genetic material (DNA or mRNA sequences) into proteins.
Glutamic acid (symbol Glu or E) is an α-amino acid with formula.
Glycine (symbol Gly or G) is the amino acid that has a single hydrogen atom as its side chain.
A helix, plural helixes or helices, is a type of smooth space curve, i.e. a curve in three-dimensional space.
Hematology, also spelled haematology, is the branch of medicine concerned with the study of the cause, prognosis, treatment, and prevention of diseases related to blood.
High-throughput screening (HTS) is a method for scientific experimentation especially used in drug discovery and relevant to the fields of biology and chemistry.
Histidine (symbol His or H) is an α-amino acid that is used in the biosynthesis of proteins.
The human genome is the complete set of nucleic acid sequences for humans, encoded as DNA within the 23 chromosome pairs in cell nuclei and in a small DNA molecule found within individual mitochondria.
In chemistry, a hydrochloride is an acid salt resulting, or regarded as resulting, from the reaction of hydrochloric acid with an organic base (e.g. an amine).
A hydrogen bond is a partially electrostatic attraction between a hydrogen (H) which is bound to a more electronegative atom such as nitrogen (N), oxygen (O), or fluorine (F), and another adjacent atom bearing a lone pair of electrons.
A hydrophile is a molecule or other molecular entity that is attracted to water molecules and tends to be dissolved by water.
In chemistry, hydrophobicity is the physical property of a molecule (known as a hydrophobe) that is seemingly repelled from a mass of water.
A hydroxy or hydroxyl group is the entity with the formula OH.
Hydroxycarbamide, also known as hydroxyurea, is a medication used in sickle-cell disease, chronic myelogenous leukemia, cervical cancer, and polycythemia vera.
A hypothesis (plural hypotheses) is a proposed explanation for a phenomenon.
The half maximal inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function.
Imatinib, sold under the brand names Gleevec among others, is a medication used to treat cancer.
Imidazole is an organic compound with the formula C3N2H4.
An immortalized cell line is a population of cells from a multicellular organism which would normally not proliferate indefinitely but, due to mutation, have evaded normal cellular senescence and instead can keep undergoing division.
Immunosuppressive drugs or immunosuppressive agents or antirejection medications are drugs that inhibit or prevent activity of the immune system.
In vitro (meaning: in the glass) studies are performed with microorganisms, cells, or biological molecules outside their normal biological context.
Interferons (IFNs) are a group of signaling proteins made and released by host cells in response to the presence of several pathogens, such as viruses, bacteria, parasites, and also tumor cells.
Isoleucine (symbol Ile or I) is an α-amino acid that is used in the biosynthesis of proteins.
A lead compound (i.e. a "leading" compound, not to be confused with various compounds of the metallic element lead) in drug discovery is a chemical compound that has pharmacological or biological activity likely to be therapeutically useful, but may nevertheless have suboptimal structure that requires modification to fit better to the target; lead drugs offer the prospect of being followed by back-up compounds.
Leucine (symbol Leu or L) is an essential amino acid that is used in the biosynthesis of proteins.
Lipophilicity (from Greek λίπος "fat" and φίλος "friendly"), refers to the ability of a chemical compound to dissolve in fats, oils, lipids, and non-polar solvents such as hexane or toluene.
In biochemistry, a metabolic pathway is a linked series of chemical reactions occurring within a cell.
Methionine (symbol Met or M) is an essential amino acid in humans.
A methoxy group is the functional group consisting of a methyl group bound to oxygen.
In genetics, a missense mutation is a point mutation in which a single nucleotide change results in a codon that codes for a different amino acid.
Molar concentration (also called molarity, amount concentration or substance concentration) is a measure of the concentration of a chemical species, in particular of a solute in a solution, in terms of amount of substance per unit volume of solution.
Molecular cloning is a set of experimental methods in molecular biology that are used to assemble recombinant DNA molecules and to direct their replication within host organisms.
A molecule is an electrically neutral group of two or more atoms held together by chemical bonds.
Nilotinib (AMN107, trade name Tasigna), in the form of the hydrochloride monohydrate salt, is a small-molecule tyrosine kinase inhibitor approved for the treatment of imatinib-resistant chronic myelogenous leukemia.
A nitrile is any organic compound that has a −C≡N functional group.
Novartis International AG is a Swiss multinational pharmaceutical company based in Basel, Switzerland.
A nucleic acid sequence is a succession of letters that indicate the order of nucleotides forming alleles within a DNA (using GACT) or RNA (GACU) molecule.
Nucleotides are organic molecules that serve as the monomer units for forming the nucleic acid polymers deoxyribonucleic acid (DNA) and ribonucleic acid (RNA), both of which are essential biomolecules within all life-forms on Earth.
An oncogene is a gene that has the potential to cause cancer.
Oxygen is a chemical element with symbol O and atomic number 8.
P-glycoprotein 1 (permeability glycoprotein, abbreviated as P-gp or Pgp) also known as multidrug resistance protein 1 (MDR1) or ATP-binding cassette sub-family B member 1 (ABCB1) or cluster of differentiation 243 (CD243) is an important protein of the cell membrane that pumps many foreign substances out of cells.
In the physical sciences, a partition-coefficient (P) or distribution-coefficient (D) is the ratio of concentrations of a compound in a mixture of two immiscible phases at equilibrium.
The pathogenesis of a disease is the biological mechanism (or mechanisms) that leads to the diseased state.
Pharmacotherapy is therapy using pharmaceutical drugs, as distinguished from therapy using surgery (surgical therapy), radiation (radiation therapy), movement (physical therapy), or other modes.
Phenylalanine (symbol Phe or F) is an α-amino acid with the formula.
The Philadelphia chromosome or Philadelphia translocation (Ph) is a specific genetic abnormality in chromosome 22 of leukemia cancer cells (particularly chronic myeloid leukemia (CML) cells).
In chemistry, phosphorylation of a molecule is the attachment of a phosphoryl group.
Piperazine is an organic compound that consists of a six-membered ring containing two nitrogen atoms at opposite positions in the ring.
Plasma protein binding refers to the degree to which medications attach to proteins within the blood.
A point mutation is a genetic mutation where a single nucleotide base is changed, inserted or deleted from a sequence of DNA or RNA.
Ponatinib (trade name Iclusig, previously AP24534) is an oral drug developed by ARIAD Pharmaceuticals for the treatment of chronic myeloid leukemia (CML) and Philadelphia chromosome–positive (Ph+) acute lymphoblastic leukemia (ALL).
In the field of pharmacology, potency is a measure of drug activity expressed in terms of the amount required to produce an effect of given intensity.
A protein domain is a conserved part of a given protein sequence and (tertiary) structure that can evolve, function, and exist independently of the rest of the protein chain.
A purine is a heterocyclic aromatic organic compound that consists of a pyrimidine ring fused to an imidazole ring.
Pyridazine is a heterocyclic organic compound with the molecular formula (CH)4N2.
Pyridine is a basic heterocyclic organic compound with the chemical formula C5H5N.
Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine.
Quinazoline is an organic compound with the formula C8H6N2.
Quinoline is a heterocyclic aromatic organic compound with the chemical formula C9H7N.
A retrospective (from Latin retrospectare, "look back"), generally, is a look back at events that took place, or works that were produced, in the past.
The SH2 (Src Homology 2) domain is a structurally conserved protein domain contained within the Src oncoprotein and in many other intracellular signal-transducing proteins.
Solute carrier family 22 member 1 is a protein that in humans is encoded by the SLC22A1 gene.
Solubility is the property of a solid, liquid or gaseous chemical substance called solute to dissolve in a solid, liquid or gaseous solvent.
The Sonogashira reaction is a cross-coupling reaction used in organic synthesis to form carbon–carbon bonds.
Src kinase family is a family of non-receptor tyrosine kinases that includes nine members: Src, Yes, Fyn, and Fgr, forming the SrcA subfamily, Lck, Hck, Blk, and Lyn in the SrcB subfamily, and Frk in its own subfamily.
Steric effects are nonbonding interactions that influence the shape (conformation) and reactivity of ions and molecules.
Structural biology is a branch of molecular biology, biochemistry, and biophysics concerned with the molecular structure of biological macromolecules (especially proteins, made up of amino acids, and RNA or DNA, made up of nucleic acids), how they acquire the structures they have, and how alterations in their structures affect their function.
Synergy is the creation of a whole that is greater than the simple sum of its parts.
Therapy (often abbreviated tx, Tx, or Tx) is the attempted remediation of a health problem, usually following a diagnosis.
In chemical thermodynamics, activity (symbol) is a measure of the "effective concentration" of a species in a mixture, in the sense that the species' chemical potential depends on the activity of a real solution in the same way that it would depend on concentration for an ideal solution.
Thiazole, or 1,3-thiazole, is a heterocyclic compound that contains both sulfur and nitrogen; the term 'thiazole' also refers to a large family of derivatives.
Thiophene is a heterocyclic compound with the formula C4H4S.
Three-dimensional space (also: 3-space or, rarely, tri-dimensional space) is a geometric setting in which three values (called parameters) are required to determine the position of an element (i.e., point).
Threonine (symbol Thr or T) is an amino acid that is used in the biosynthesis of proteins.
---> Thymine (T, Thy) is one of the four nucleobases in the nucleic acid of DNA that are represented by the letters G–C–A–T.
Time is an American weekly news magazine and news website published in New York City.
Two-dimensional space or bi-dimensional space is a geometric setting in which two values (called parameters) are required to determine the position of an element (i.e., point).
Tyrosine (symbol Tyr or Y) or 4-hydroxyphenylalanine is one of the 20 standard amino acids that are used by cells to synthesize proteins.
A tyrosine kinase inhibitor (TKI) is a pharmaceutical drug that inhibits tyrosine kinases.
Valine (symbol Val or V) is an α-amino acid that is used in the biosynthesis of proteins.
In molecular physics, the van der Waals forces, named after Dutch scientist Johannes Diderik van der Waals, are distance-dependent interactions between atoms or molecules.
In chemistry, vinyl or ethenyl is the functional group with the formula −CH.
The Walker A and Walker B motifs are protein sequence motifs, known to have highly conserved three-dimensional structures.
X-ray crystallography is a technique used for determining the atomic and molecular structure of a crystal, in which the crystalline atoms cause a beam of incident X-rays to diffract into many specific directions.
2-Butyne (dimethylacetylene, crotonylene or but-2-yne) is an alkyne with chemical formula CH3C≡CCH3.
Bcr-Abl inhibitor, Bcr-Abl tyrosine kinase inhibitor, Bcr-Abl tyrosine kinase inhibitors, Bcr-abl inhibitor, Discovery and development of Bcr-Abl tyrosine kinase inhibitors, Discovery and development of Bcr-Abl tyrosine-kinase inhibitors, Rebastinib, Second generation CML drugs, T315i.