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AI-10-49, the Glossary

AI-10-49 is a small molecule inhibitor of leukemic oncoprotein CBFβ-SMHHC developed by the laboratory of John Bushweller (University of Virginia) with efficacy demonstrated by the laboratories of Lucio H. Castilla (University of Massachusetts Medical School) and Monica Guzman (Cornell University).^[1]

35 relations: Adhesion (medicine), Allosteric regulation, BCL6, Binding selectivity, BRD4, Carcinogenesis, Cell cycle, Cellular differentiation, Chemotherapy, Chromosomal inversion, Chromosomal translocation, Clinical trial, Cornell University, Cytarabine, Doxorubicin, ETV6, Haematopoiesis, IC50, JQ1, Leukemia, Lymphatic system, Myeloid leukemia, Myeloid tissue, Nutlin, Oncogene, P53, Pharmacokinetics, Polyethylene glycol, Progenitor cell, Protein dimer, Protein–protein interaction, RUNX1, Transcription factor, UMass Chan Medical School, University of Virginia.
Trifluoromethyl ethers

Adhesion (medicine)

Adhesions are fibrous bands that form between tissues and organs, often as a result of injury during surgery.

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Allosteric regulation

In the fields of biochemistry and pharmacology an allosteric regulator (or allosteric modulator) is a substance that binds to a site on an enzyme or receptor distinct from the active site, resulting in a conformational change that alters the protein's activity, either enhancing or inhibiting its function.

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BCL6

Bcl-6 (B-cell lymphoma 6) is a protein that in humans is encoded by the BCL6 gene.

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Binding selectivity

In chemistry, binding selectivity is defined with respect to the binding of ligands to a substrate forming a complex.

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BRD4

Bromodomain-containing protein 4 is a protein that in humans is encoded by the BRD4 gene.

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Carcinogenesis

Carcinogenesis, also called oncogenesis or tumorigenesis, is the formation of a cancer, whereby normal cells are transformed into cancer cells.

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Cell cycle

The cell cycle, or cell-division cycle, is the sequential series of events that take place in a cell that causes it to divide into two daughter cells.

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Cellular differentiation

Cellular differentiation is the process in which a stem cell changes from one type to a differentiated one.

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Chemotherapy

Chemotherapy (often abbreviated chemo, sometimes CTX and CTx) is the type of cancer treatment that uses one or more anti-cancer drugs (chemotherapeutic agents or alkylating agents) in a standard regimen.

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Chromosomal inversion

An inversion is a chromosome rearrangement in which a segment of a chromosome becomes inverted within its original position.

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Chromosomal translocation

In genetics, chromosome translocation is a phenomenon that results in unusual rearrangement of chromosomes.

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Clinical trial

Clinical trials are prospective biomedical or behavioral research studies on human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, drugs, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison.

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Cornell University

Cornell University is a private Ivy League land-grant research university based in Ithaca, New York.

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Cytarabine

Cytarabine, also known as cytosine arabinoside (ara-C), is a chemotherapy medication used to treat acute myeloid leukemia (AML), acute lymphocytic leukemia (ALL), chronic myelogenous leukemia (CML), and non-Hodgkin's lymphoma.

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Doxorubicin

Doxorubicin, sold under the brand name Adriamycin among others, is a chemotherapy medication used to treat cancer.

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ETV6

ETV6 (i.e. translocation-Ets-leukemia virus) protein is a transcription factor that in humans is encoded by the ETV6 (previously known as TEL) gene.

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Haematopoiesis

Haematopoiesis (from Greek αἷμα, 'blood' and ποιεῖν 'to make'; also hematopoiesis in American English; sometimes also h(a)emopoiesis) is the formation of blood cellular components.

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IC50

Half maximal inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function.

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JQ1

JQ1 is a thienotriazolodiazepine and a potent inhibitor of the BET family of bromodomain proteins which include BRD2, BRD3, BRD4, and the testis-specific protein BRDT in mammals. AI-10-49 and JQ1 are Experimental cancer drugs.

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Leukemia

Leukemia (also spelled leukaemia; pronounced) is a group of blood cancers that usually begin in the bone marrow and produce high numbers of abnormal blood cells.

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Lymphatic system

The lymphatic system, or lymphoid system, is an organ system in vertebrates that is part of the immune system, and complementary to the circulatory system.

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Myeloid leukemia

Myeloid leukemia is a type of leukemia affecting myeloid tissue.

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Myeloid tissue

Myeloid tissue, in the bone marrow sense of the word myeloid (myelo- + -oid), is tissue of bone marrow, of bone marrow cell lineage, or resembling bone marrow, and myelogenous tissue (myelo- + -genous) is any tissue of, or arising from, bone marrow; in these senses the terms are usually used synonymously, as for example with chronic myeloid/myelogenous leukemia.

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Nutlin

Nutlins are cis-imidazoline analogs which inhibit the interaction between mdm2 and tumor suppressor p53, and which were discovered by screening a chemical library by Vassilev et al. Nutlin-1, nutlin-2, and nutlin-3 were all identified in the same screen; however, Nutlin-3 is the compound most commonly used in anti-cancer studies.

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Oncogene

An oncogene is a gene that has the potential to cause cancer.

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P53

p53, also known as Tumor protein P53, cellular tumor antigen p53 (UniProt name), or transformation-related protein 53 (TRP53) is a regulatory protein that is often mutated in human cancers.

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Pharmacokinetics

Pharmacokinetics (from Ancient Greek pharmakon "drug" and kinetikos "moving, putting in motion"; see chemical kinetics), sometimes abbreviated as PK, is a branch of pharmacology dedicated to describing how the body affects a specific substance after administration.

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Polyethylene glycol

Polyethylene glycol (PEG) is a polyether compound derived from petroleum with many applications, from industrial manufacturing to medicine.

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Progenitor cell

A progenitor cell is a biological cell that can differentiate into a specific cell type.

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Protein dimer

In biochemistry, a protein dimer is a macromolecular complex or multimer formed by two protein monomers, or single proteins, which are usually non-covalently bound.

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Protein–protein interaction

Protein–protein interactions (PPIs) are physical contacts of high specificity established between two or more protein molecules as a result of biochemical events steered by interactions that include electrostatic forces, hydrogen bonding and the hydrophobic effect.

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References

[1] https://en.wikipedia.org/wiki/AI-10-49

Also known as C30H22F6N6O5.