Lecture_20-Inhibitors_and_Ligands_as_Drugs_copy

Lecture_20-Inhibitors_and_Ligands_as_Drugs_copy -...

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INHIBITORS AND LIGANDS AS DRUGS Inhibitors and Ligands as Drugs diseases are related to some type of metabolic function or malfunction the metabolic malfunction is probably linked to some enzyme, receptor, etc. if the function of the relevant enzyme or receptor can be modiFed (blocked or activated), the disease may be treated with a small molecule (a drug) + HIV proteins HIV protease Active Site Aspartates Active Site inhibited blocked PENICILLIN The frst antibiotic
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Alexander Fleming (1881-1955) What the hell is this crap?! Alexander Fleming (1881-1955) What the hell is this crap?! Penicillin: use with care Fleming noted that bacteria could gain resistance to penicillin! dosage too small December 2011 Sunday Monday Tuesday Wednesday Thursday Friday Saturday 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 21 22 23 24 25 26 27 28 29 30 31 start pills stop pills Ah, frak it. ..I feel fine not taken long enough
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How does penicillin kill bacteria? glycopeptide transpeptidases cell wall synthesis osmotic lysis (bursting) glycopeptide transpeptidase Ser O H R C O NH HC C O N H C S C CH CH 3 CH 3 C O O - penicillin active enzyme glycopeptide transpeptidase inactivated enzyme C O NH HC C O HN CH S C CH CH
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This note was uploaded on 11/28/2011 for the course CHEM 340 taught by Professor T.baird during the Fall '11 term at S.F. State.

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Lecture_20-Inhibitors_and_Ligands_as_Drugs_copy -...

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