Synthetic Informative Agents

Words: 673
Pages: 3
Open Document
CLASSICAL ANTICANCER AGENTS
CHAPTER 8

ALKYLATING AGENTS eg. Nitrogen Mustards, alkyl sulponates, nitrosureas, and platinum based (not alkylating but can cause cross bonding so grouped together).
MOA= formation of an ethyleneimonium ion, which is highly unstable and forms covalent bonds with DNA bases, guanine being the most vulnerable.
These drugs typically possess two reactive groups characterised by the presence of lone pairs of electrons on the N atom, donation of which gives rise to the unstable ethyleneimonium ion following the loss of the neg chloride ion, both intermediates being capable of bonding with two guanine bases within the DNA double helix, and allowing for cross -linking.
Platinum agents act similarly. The reactive intermediate …show more content…
F.A. is an important precursor which undergoes reduction to dihydrofolate and then tetrahydrofolate by the enzyme dihydrofolate reductase (DHFR), the primary target of methotrexate F.A. analogue, acting as a folate antagonist inhibiting de novo synthesis. Another effect of DHFR inhibition is decreased intracellular reduced folate pool. Reduced folate acts as a cofactor for thymidylate synthase, which catalyses the synthesis of pyrimidine nucleotides by converting deoxyuridine monophosphate (dUMP) to deoxythymidine monophosphate (dTMP). Folate analogues inhibit synthesis of purines and pyrimidines. Polyglutamination of folates increases their intracellular accumulation and retention. Methotrexate and other folate analogues enter cells through the membrand-bound reduced folate carrier (RFC-1), where sequential addition of glutamine residues by the enzyme folypolyglutamate synthase (FPGS) leasd to the formation of polyglutamates eg methotrexate polyglutamate (MTXPG). The concentration of folate polyglutaminates and patient response to antifolate drug response is determined by the expression and activity of FPGS and the opposing enzyme gama-gltamyl hydrolase …show more content…
They are activated by the enzyme hypoxanthine: guanine phosphoribosyl transferase (HGPRT) This enzyme ordinarily transfers phosphoribosyl pyrophosphate (PRPP) which can consists of a ribose and a phosphate group, to a free purine base to form a nucleotide. This process known as the purine nucleotide salvage pathway, maintains the intracellular purine nucleotide pool necessary for various cellular
Show More

Related Documents: Synthetic Informative Agents

Estrogen and Vertebrate Steroid Hormones Essay

The term “endocrine disrupting chemicals” is commonly used to describe environmental agents that alter the endocrine system. Laboratories working in this emerging field—environmental endocrine research—have looked at chemicals that mimic or block endogenous vertebrate steroid hormones by interacting with the hormone’s receptor. Environmental chemicals known to do this do so most often with receptors derived from the steroid/thyroid/retinoid gene family. They include ubiquitous and persistent organochlorines…

Words 380 - Pages 2

Kota Fibre Case Study

Fibres provided synthetic Fibre yarns to local textile weavers mainly to make the traditional women’s dress in India; the saris. Ms. Pundir was both the managing director and principal owner of the company. Kota Fibres used new technology and domestic raw materials to produce their quality product. The demand for saris amounted to 12 billion yards of fabric The Case Papers Kota Fibres, Ltd. was founded in 1962 in Kota, India. Created to produce nylon Fibre, Kota Fibres provided synthetic Fibre yarns…

Words 3329 - Pages 14

Corporate Governance and Auditors Essay

CHAPTER 1 INTRODUCTION BACKGROUND There are a number of positive developments in the economy since the introduction of foreign currency (multi currency system), which if sustained, will spearhead economic recovery in the short to medium term horizon. These developments included the introduction of the multi currency system and the liberalization of the exchange control, the formation of government of national unity (GNU) and the engagement with multilateral institutions and the donor community…

Words 14732 - Pages 59