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SMART Drugs Engineering Nature’s Solution to the Undruggable Target Challenge

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Mid-Scale Library Approaches (10^5)<br />

Cyclophillin Presented Library<br />

Me<br />

Me<br />

N<br />

Me<br />

Me O<br />

N<br />

N<br />

O Me<br />

OH<br />

H H<br />

N<br />

O<br />

O<br />

N<br />

Me<br />

O<br />

OH<br />

50,000 CsA-alogs syn<strong>the</strong>sized <strong>to</strong> date<br />

O<br />

Me<br />

N<br />

O<br />

Me<br />

N<br />

H<br />

Boc<br />

FKBP Presented Library<br />

Cyclosporine<br />

Constant Region<br />

1)<br />

2)<br />

3)<br />

4)<br />

pool at stage of resins<br />

HTS<br />

O<br />

HO<br />

Me<br />

OBn<br />

N<br />

O<br />

O<br />

O<br />

OMe<br />

OAc<br />

Rapamycin<br />

Constant Region<br />

PepFde<br />

syn<strong>the</strong>sis<br />

WARP DRIVE BIO, INC. 20

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