What is BIBR1532?

What is BIBR1532?

BIBR1532 is a potent telomerase inhibitor that showed potential anti-tumor activities in several types of cancer, by triggering replicative senescence and apoptosis.

Is telomere the same as telomerase?

Telomeres function by preventing chromosomes from losing base pair sequences at their ends. Telomerase, also called telomere terminal transferase, is an enzyme made of protein and RNA subunits that elongates chromosomes by adding TTAGGG sequences to the end of existing chromosomes.

Is there a drug that can inhibit telomerase?

Small molecules such as AZT (azidothymidine, a non-specific reverse transcriptase inhibitor) [16], chemicals such as retinoids [17], tamoxifen [18], or EGCG (epigallocatechin gallate) [19], and molecules which interfere with telomere structure (i.e., G-quadruplex stabilizers) [20, 21] have been shown to be effective in …

What is the role of telomerase?

Telomerase is a cellular reverse transcriptase that helps to provide genomic stability in highly proliferative normal, immortal, and tumor cells by maintaining the integrity of the chromosome ends, the telomeres. The activity of telomerase is associated with the majority of malignant human cancers.

Are telomeres shortened by telomerase?

Telomeres help prevent genes from being lost in this process. But this means that as your chromosomes replicate, your telomeres shorten. That’s where an enzyme called telomerase comes in. It’s found in certain cells and helps prevent too much wear and tear.

Are telomeres?

A telomere is the end of a chromosome. Telomeres are made of repetitive sequences of non-coding DNA that protect the chromosome from damage. Each time a cell divides, the telomeres become shorter. Eventually, the telomeres become so short that the cell can no longer divide.

What is the consequence of inhibiting telomerase?

The inhibition of telomerase activity is associated with: 1) a complete erosion of telomeres of majority of chromosomes and growth arrest of the cancer cells without affecting the normal cells from stomach and intestine; 2) induction of both senescence and apoptosis; and 3) up-regulation of key regulatory genes …

What happens when telomerase is inhibited?

Inhibiting telomerase, an enzyme that rescues malignant cells from destruction by extending the protective caps on the ends of chromosomes, kills tumor cells but also triggers resistance pathways that allow cancer to survive and spread, scientists report in the Feb. 17 issue of Cell.

What is the significance of telomeres and telomerase?

Telomeres, repetitive (TTAGGG) DNA–protein complexes at the ends of chromosomes, are crucial for the survival of cancer cells. They are maintained by an enzyme called telomerase in the vast majority of tumors.

What happens if there is no telomerase?

Without telomerase activity, these cells would become inactive, stop dividing and eventually die. Drugs that inhibit telomerase activity, or kill telomerase-producing cells, may potentially stop and kill cancer cells in their tracks.

What are telomeres and telomerase and how are they involved in determining longevity?

Telomeres are known to be one of the major determinants of aging. It helps to maintain telomere length by adding telomeric repeats “TTAGGG” to ends of the chromosome during DNA replication. Lifestyle plays an important factor in determining telomere length and telomerase activity.