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Question 3. Dihydrofolate reductase (DHFR) is capable of making one carbon moieties of various oxidation states (i.e., methanol, formaldehyde, formate). Folic acid, a B vitamin, provides the critical chemistry: This type of chemistry is utilized in the synthesis of nucleotides. Methotrexate has a significantly higher affinity (Kd ~ 50 pM) than folate for the enzyme and is used in cancer therapy to suppress DNA synthesis of rapidly dividing cancer cells. What is a tempting reason for methotrexate having such high affinity?

Question 3. Dihydrofolate reductase (DHFR) is capable of making one carbon moieties of various oxidation states (i.e., methanol, formaldehyde, formate). Folic acid, a B vitamin, provides the critical chemistry: This type of chemistry is utilized in the synthesis of nucleotides. Methotrexate has a significantly higher affinity (Kd ~ 50 pM) than folate for the enzyme and is used in cancer therapy to suppress DNA synthesis of rapidly dividing cancer cells. What is a tempting reason for methotrexate having such high affinity?

Biochemistry
Biochemistry
9th Edition
ISBN:9781319114671
Author:Lubert Stryer, Jeremy M. Berg, John L. Tymoczko, Gregory J. Gatto Jr.
Publisher:Lubert Stryer, Jeremy M. Berg, John L. Tymoczko, Gregory J. Gatto Jr.
Chapter1: Biochemistry: An Evolving Science
Section: Chapter Questions
Problem 1P
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Question 3. Dihydrofolate reductase (DHFR) is capable of making one carbon moieties of various oxidation states (i.e., methanol, formaldehyde, formate). Folic acid, a B vitamin, provides the critical chemistry: R. This type of chemistry is utilized in the synthesis of nucleotides. Methotrexate has a significantly higher affinity (Kd - 50 pM) than folate for the enzyme and is used in cancer therapy to suppress DNA synthesis of rapidly dividing cancer cells. What is a tempting reason for methotrexate having such high affinity?
Transcribed Image Text:Question 3. Dihydrofolate reductase (DHFR) is capable of making one carbon moieties of various oxidation states (i.e., methanol, formaldehyde, formate). Folic acid, a B vitamin, provides the critical chemistry: R. This type of chemistry is utilized in the synthesis of nucleotides. Methotrexate has a significantly higher affinity (Kd - 50 pM) than folate for the enzyme and is used in cancer therapy to suppress DNA synthesis of rapidly dividing cancer cells. What is a tempting reason for methotrexate having such high affinity?
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