Histone deacteylase inhibtors and Hypomethylating agents Flashcards

1
Q

What is epigenetics

A

study of phenotypic changes that do not involve changes in the DNA sequence

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2
Q

T/F: Heterochromatin are the parts of the chromatin that is expressed while Euchormatin is not

A

False: Euchromatin are the parts of the chromatin that are expressed while heterochromatin are not

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3
Q

What are the three main ways that chromatin can be modified

A

Methylated, acetylated, and phosphorylated

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4
Q

What are the writers of histones, erasers

A

Acetylators, methylators, kinases/ Deacetylators, demethylators, and phosphatases

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5
Q

What is the effect that acetylators have on histones

A

Acetlylation removes the positive charge of the histone making the chromatin more relaxed and easier to access

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6
Q

What are the chromatin readers and what do they recognize

A

MBD recognize methylated DNA, Bromodomain recognize acetylated histones, chromodomain AND phd AND wd40 recognize methylated histones

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7
Q

T/F: TET remove DNA methyl marks, KDM and RDM are histonedemethylases that remove methyl marks

A

True

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8
Q

What parts of the DNA is methylated

A

Cytosine bases of Eukaryotic DNA converted to 5-methylatedcytosine

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9
Q

What motif does methylation of DNA almost always occur at

A

CPG

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10
Q

T/F: Promoters of actively transcribed genes are unmethylated while promoters of transcriptionally silecned genes are methylated

A

True

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11
Q

What proteins methylate DNA and what are they/ source of the methyl group

A

DNMT1, DNMT2, DNMT3/ SAM

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12
Q

What is the mechanism of demethylation

A

methyl groups are hydroxylated

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13
Q

How DNA hypomethylation (active genes) characterized by which promoters

A

H3K4me3, H3, and H4 acetylation

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14
Q

What is the only approved DNMT inhibitor/ how

A

5-aza-c (azacitidine, Vidaza)/ Converted to trinucleotides and incorporated into DNA/RNA respectively OR covalently modifies DNMT

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15
Q

What are the 4 most known ways histones are changed

A

Lysine acetylation, Lysine and arginine methylation, serine/threonine/tyrosine phosphorylation, serine/threonine ubiquitination

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16
Q

T/F: HAT adds acteyl group while HDAC removes acetyl groups

A

True

17
Q

What are the two most know deacetylase complexes, what are they dependent on

A

HDACs and SIRTS/ HDACs: Zinc, SIRTuins: are nicatinamide adenine di-nucleotide (NAD) dependent

18
Q

What class of HDACs are responsible for deactylation of histones

A

Class 1

19
Q

What are the HDAC inhibitors

A

Valproic acid, Vorinistat, Romidespin, Belinostat, Panobinostat

20
Q

Why is zinc important in deactylation, how do HDAC inhibitors

A

Primes the acetyl group for hydrolysis, Inhibitor forms bidentate chelate with Zinc