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RAS????????????????????????????????Harvery????????????Ha-MSV????Kirsten????????????Ki-MSV????????????斜????????????????????30%??????携??RAS??????????????“H-RAS??K-RAS??N-RAS”?薪?KRAS???????????????????100??????????
?????????RAS?????????????????????????芯????????40??????“??????”??“???”??????5???FDA ?? ??????RAS ??????? AMG510 ??????????????????????校?????????????? RAS ??????????????????
????????AMG-510???????????RAS???????小????????????????????RAS????????谓??????????小??????????“???”?????????????????????????????芯??????
??????????????芯?????????杈�??????????????“RAS”???????路???????????RAS???娣�???????“???”????????????????????????????芯???RAS-inhibiting biologics identify and probe druggable pockets including an SII-α3 allosteric site????????Nature communications???????
2017??????????Avacta??????????????????????????娲�??????????????????????????????????Affimer???????眉????械?Affimer??????????????????????????????????斜??????????浜�???????????????????????????????????????????????????眉????芯??????????????
????????????芯??校????????????眉????????????Affimer??????“K3 ?? K6”???芯??????????????????????????????????????路??
?????????芯???????????????????????????????????“SI/II”??“SII”?小?????Affimer K6 ????? SI/SII????校???Affimer K3???SII?????顭�??????????????????? RAS ????????澹�??携???????? SII/α3?????
???“SI/II”??“SII”?????????????芯??????SI/II???????? RAS ????? Switch I ?? Switch II ??????????????婕�??????????????????SII??????Switch II????????????????????Switch II??械????????????????RAS???????
Affimers ??????? RAS ??????????????????
??????????Affimers???????RAS??????????????芯????????????KRAS:Affimer NanoBRET ?????????SI/SII ?? SII ????械?小??????????? NanoBRET ????????????????
?芯?????????????? Affimer ??KRAS?????????????NanoBRET ????????????????K6 ?? K3 ??????????KRAS?????????Affimers ?????????效??????????
?慰??????
[1]https://www.nature.com/articles/s41467-021-24316-0#Abs1
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