ËɭŶŏɃV϶ưȻ̪Ƀ1Ь ͲğVϮˬ˾̎(1)

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ǈЮɅUW.ɸƺU96P SRD VÊϳͲ9dYбύÚɊʰZVȅ¾;χĦȁΘChJ/Ш˻˰Ω˙ǵŶϛЩ(2)CPZEN-45u®¥o´(Caprazamycin)ГVĆϊʃɠu®

´VΙƫè CPZEN-45

W.¥pj˚6JǷɚʏ˩ΔМU96PͲğǷŀǱ̭ɠͫ(H37Rv)V^TeGεƆğͅǱ̭ɠͫ (XDR-TB) UƧDPaɆĪQ5gBRj΄ĒDJ/]JIVƗĄ
ǱΔМU96Pˑū]QUˉUśАRTgd7TʅǱWΘ`ehP6T6/ȼǈǏUǗ<̳<.ɌĮŇˈVϮˬUŋ@Pĝ͛ǋΔМj̲̳ÁQ5g/]J.̭ɠͫj˚6Pé˚ɶǌVΉȻjώ`.ɌĮŇˈ;Bh]QVḘ̑ɠͲRWˢTgɲ˰Ϟ̨jϴƞFgBRQ.̭ɠͫV̪͍ŽVȲ΅Ňǻ;ƏAehgBRjȻe:UDJ/
CeUǗ<̳<.ɌĮŇˈVƈϤí̯ʔV˿̐Uŋ@JɬΌj͸MP6g/Ш̔Я˘ˈʛǱ˾̎ϛ.ģͲĮƕ˾̎ϛ.ŧĊƅÞɭ.̜ŧŧ̐ͺ˘˾̎ǿ.̜ŧ|²®
ƺ̐ƈЩ
(3)

2-OH-ABKm¦ϝ̠èȆ˘ˈβm°u´(Arbekacin : ABK)VΙƫè 2-OH-ABK W

ABK dfa͕ʅǱ;åʪD.ABK ǷŀǱͫV^TeG ABK ͅǱͫUƧDPaɆĪQ5gBRj΄ĒDJ/ɌĮŇˈjϢ˧̪ͫǷɚ˧UƧFg|´·­´˩ʔVνRTgͲğRDPϮˬF[>.͛ǋΔМUǭ΂TΔȰjǦgJ`VŇǻʔj
FQU˿̐DJ/CeU.ƻɭ˰ŇǻʔVϮˬUŋ@PͿϋ|ĜʪUʗĤDJ
Ňǻ°·VɬΌjώ`J/ШģͲĮƕ˾̎ϛЩ(4)¯²¡´Ȇy®§ϼǱͫʛǱĵF¯²¡´ C VϮˬUŋ@.ǿĊņ˾̎ϛTeYUŧĊƅV˾̎ɶϰRVĆŉ˾̎j͸MP6g/ɌĮŇˈWĸğQ¥pV
MRSA ĄκǷɚ©°U96P̔ЮϕȈͲQ5g´|¥o´Rŉ̕VühJ
ʏ˩ĪɗĵFBR;ƈ<TˉǪQ5g/ɌĮŇˈWȶƓͲRWˢTgųβjɲ˰

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Pώ`J/CeU·®x§ğШ¡§.q§.u°¡§ЩRê˚F

gBRQ in vitro Q˷Æ˰UǛ6ȆͫʛǱĵFBRj΄6KDJJ`.¥p
V MRSA VǷɚ©°j˚6Pê˚˩ʔU9@gʏ˩ĪɗVɬΌjϮƐDJ/]J.À͸DP¯²¡´VĵŇǻΙƫèj˚6PɰϋʛǱ˷ϰ˾̎.˷ÆǱVɶǌΉɕjFF`J/Ш̔Я˘ˈʛǱ˾̎ϛ.īˈȵΏ.ģͲĮƕ˾̎ϛ.ŧĊ˾̎ɶϰ.ʢƅƈƕЩ(5)m¦|®¥o´m¦|®¥o´WϢ˧Ƿɚ˧.ƿÁǷɚ˧9dYƟˠV͋őōŠ˧VδŢͫUƧ
DPʛǱĵD.̪ͫV DNA ªo±·R¤o¨®·IV jϕȈ˰UϴƞFgȲD6ȆͫğQ5g/m¦|®¥o´VĮƕēΉˈ9dYIVΙƫèj˚6
P.»ϛ̠ϛēVɰϋʋƙ9dYɌĮŇˈV̱ƧɰϋjΉȻDJ/]J.ɰϋƂĮVĚǧj˵ȐDJΙƫèVŇǻ˾̎U˺ȀDJ/m¦|®¥o´RIVɲ˰´
xβQ5g DNA ªo±·RV˷Íé˚VΉɕj˵ȐD.ɓƻƈ9dY˓˾RVķŉ˾̎QĆ̭ɀ X ̶ɰϋΉɕjώ`P6g/x²¯p§ưͫǷɚ©°¥pj˚6Γïj͸T6.ɆĪǱj˿ΘDJ/Ш̔Я˘ˈʛǱ˾̎ϛ.ēƒɰϋΉɕϛ.ģͲĮƕ˾̎ϛ.ɓÑƻɭƈ.˓˾Щ

2ЬͲğϮˬUŋ@Jų́˾̎
2.1

ȆǷɚ˧Ͳ

(1)

ȆͫͲVȘ̩˾̎ 
1)

MRSA-VRE Γï̢.m¦y¯|ͅǱͫΓï̢.x²¯p§Γï̢.
¯|x·²¯Γï̢.ȆϟͫΓï̢̕Vņ̊Γï̢j˚6Ȇ˘ˈβVΓïj͸MJ/Ш̔Я˘ˈʛǱ˾̎ϛЩ2)ĝǈǏUǗ<̳<.16S rRNA ¨®·˙˘m¦y¯|̢Ȇ˘ˈβͅǱͫjƫăD.Ȳ΅m¦y¯|̢Ȇ˘ˈβVȘ̩ļYȲ΅ΙƫèVŇǻRI
VΓï˾̎j͸TMJ/Ш̔Я˘ˈʛǱ˾̎ϛ.ģͲĮƕ˾̎ϛ.ŧ̐ŧϿĲ˩˾̎´·Щ3)

MRSA/VISA UˉǪ5gȆͫʛǱĵFĮŇˈVɰϋjʋƙD.IVé˚ɶǌΉɕV̭ɗjaRU.ƛ˚ĮUŋ@PŧĊÞɭRĆŉ˾̎j͸TMP6g/Ш̔Я˘ˈʛǱ˾̎ϛ.ēƒɰϋΉɕϛ.ģͲĮƕ˾̎ϛ.ЍƉŵƈЩ

9

4)ɫˈ˦UƧDPϳϹĪɗĵF̪ͫ TCS ϴƞğy¥o´j¯·RDJȘ̩˾̎j͸T6.x²¯p§ưͫUƧDϕȈǱVП6ĮŇˈjȲJU΄ĒDJ/īˈƛМV̭ɗ:eÕǥVƯϮUN6PɬΌDP6g/Ш̔Я˘ˈʛǱ˾̎ϛ.ƳƱƈ.υˣƈЩ

5)ȷɌQĖ`PēЃChJ NDM-1 ˘˙ƈ͗ͫ;óɆFg NDM-1 j|·DP6g®¦VâȤɶɰΉɕjēЃýQ5gˋķĲ̇ƈƕRĆŉQώ`P6g/
Ǩ˘ˈŲИʤ®o®¯·Vx¯·´ydf.®¦âȤϴƞˈβVȘ̩j͸MP6g/Ш̔Я˘ˈʛǱ˾̎ϛ.ˋķĲ̇ƈЩ

6)

²¯ͫ9dY MRSA UƧFg¥pVǷɚʏ˩ƛМ̢Vɰ̛j͸MP6g/ШīˈȵΏ.̔Ю˘ˈʛǱ˾̎ϛ.̔Я˘ˈʛǱ˾̎ϛЩ(2)Ȇo´°r´po°ͲVȘ̩˾̎o´°r´po°V RNA ¤¯¨®·
m·;aNwªîƓr´x±ʛǱWơÃ̪͍UWΘ`ehT6ˉˢTĽǯQ5g/BVɶɰjģͲɲ˰RDP in vitro Ϟ̨ϴƞmo̢jɰ̛D.ĮŇˈ®o®¯·9dYǨ˘ˈŲИˈj˚6Px¯·´yj͸MJ/Ǩ˘ˈŲИˈdfŉƙDJȲ΅ĮŇˈ
UN6P.IVϴƞɶɰjΉɕDJ/Ш̔ 2 ˘ˈʛǱ˾̎ϛ.̔ 3 ˘ˈʛǱ˾̎
ϛ.įϡƈЩ
(3)

Ȇ B Ů͉ʾpo°ğVȘ̩˾̎B Ů͉ʾpo°V{§΀ͿɶɰjϴƞFgĮŇˈjȘ̩FgJ`U.m
po°

x·j˚6Jpo°{§΀ͿΓï̢jɰ̛DJ/ɰ̛DJmo̢j˚6P.Ǩ˘ˈŲИʤļYĮŇˈ®o®¯·Vx¯·´yj͸MP6g/ϴƞʛǱĵFĮŇˈUN6PWé˚ɶǌΉɕjώ`P6g/Ш̔ 2 ˘
ˈʛǱ˾̎ϛ.̔ 3 ˘ˈʛǱ˾̎ϛ.ɓÑƈ¶Ĳ̇ƕ˾̎ǿЩ

2.2

Ȇ;kğ

(1)

²¡´UϰFg˾̎o´£o¨·´yUdg͖˨Ċ²m·§ϴƞʛǱʔj˚6P.̬Łȅ¾
QɆĪǱĵF£²´ϟŮ²m·§ϴƞğjǦJ/CeUƆˬǱНӦ͖ɫ¥pU96P̬Łȅ¾QǛ6Ȇ͖˨ʛǱĵDJ/ШʐʚȦǿ.īˈȵΏ.Ɇɶ
Ňǻ˾̎ϛЩ10

(2)ɝИЕЙϕȈ˰̪͍ʅǱˈβVȘ̩˾̎ɝИЕЙˊǸV;k̪͍UϕȈ˰T̪͍ɾjΙƫFgĮŇˈjǦJ/CeUɌĮŇˈVé˚ɶǌΉɕj͸MJ/Ш̔Ю˘ˈʛǱ˾̎ϛ.ʐʚȦǿ.ЍƉŵƈ.ŧĊÞ
ɭЩ(3)m¤·jΙƫFgĮŇˈV˾̎
;kϰόϖâƒjɲ˰RDJx¯·´ydfǦehJȲ΅ĮŇˈVɰϋʋƙj͸T6.in vitro 9dY in vivo Udg˘ˈʛǱjΞ[J/ (̔Ю˘ˈʛǱ˾̎ϛ.
ʐʚȦǿ.īˈȵΏ.ŧĊÞɭ)(4)

ĝ̐͘;kUɆĪTĮŇˈVȘ̩ĝ̐͘;kUƧDPɆĪTȲ΅ĮŇˈVé˚ɶǌjΉɕDJ/]J.ĝ̐͘;kUͲğͅǱjaJeF AR ¯m´jɲ˰UDJȘ̢̩jɰ̛D.x¯·´yjϮƐDJ/Ш̔Ю˘ˈʛǱ˾̎ϛ.ʐʚȦǿ.īˈȵΏ.ɆɶŇǻ˾̎ϛЩ(5);kЫϯβ˷Íé˚jĘ˚DJȆ;kğVȘ̩˾̎;k̪͍Rϯβ̪͍U9@g˷Íé˚jĘ˚D.ȲJT;kʏ˩VJ`Vēƒɲ˰V˾̎j͸7RRaU.BV˷Íé˚jĚǧFgåēƒĮŇˈVȘ̩˾̎j̲̳D
P6g/Bh]QVΉɕ:e.pw·´y´xV GAPDH ;;k̪͍VżʀjȄĚFgʛǱjɆFgBRjȻe:UDJ/IBQ.GAPDH Vϝĕ:eŉʛǱjˬȠFg¡VģͿj͸TMP6g/]J.͌;k̪͍Rϯβ̪͍VĆŲИx¯·´y̢:eˬ΄DJȲ΅ĮŇˈo´·¯´UN6PW.Ȇ

;kʛǱVé˚ɶɰVΉɕj͸T7RRaU.ȲJTʛǱRDPȆ²¯ͫʛǱU
N6PaΙƫèVϮˬjϊDPɬΌDP6g/Ш̔Ю˘ˈʛǱ˾̎ϛ.ʐʚȦǿ.
īˈȵΏ.ɆɶŇǻ˾̎ϛ.ɓÑͲ̇ƈЩ
(6)ɶ͎ǱȆèVϮˬ˾̎Ȇ;kʛǱjɆFgȆèjéͿD.ēƒɲ˰Ȇ;kğRDPϮˬj͸MP6g/é˚ɶɰ9dYϕȈĚVΉɕj͸T7RRaU.w¨®Įj͸TMJ/ШʐʚȦǿ.ŧĊÞɭ.ɓįƈЩ

(7)ǴǱ͔͖˨.̬͚͖̄ͥȄĚˈβĸЃj˵ȐDJ EGFRvIII ϴƞˈVȘ̩˾̎
EGFRvIII jϐġˬˑCHJ¥p̴̼̪͍ͥj˚6PζŷЉîƓ˰żʀjȐɲRFg˪ĺǱ EGFRvIII ϴƞˈβx¯·´yj͸6.åēƒĮŇˈjǦJ/ʛ
ǱˈβVé˚ɶɰjΉɕFgRRaU.ΙƫèĮUdMPdfǛĤTȆ;kʛǱĵFĮŇˈVģͿj͸TMP6g/Ш̔Ю˘ˈʛǱ˾̎ϛ.ɆɶŇǻ˾̎ϛЩ

11

2.3

ĲͲŕVĄ¿˟˰í̯j˵ȐDJŇǻ

(1)

ĲͲŕ9dYɆ˚˘ˈʛǱˈβVΊƑ˰½ȮŇǻʔVϮˬ
1)ΊƑ˰½Ȯo±xm°w°ĮĽǯUdf.Ȇ¥®¯mͲ KAE609 VΊƑ˰
½ȮĄŇǻjϒǻDJ/ШɆɶŇǻ˾̎ϛЩ

2)

ĝ̐͘;k̪͍VżʀjȄĚFg Resormycin 9dY Androprostamine A VŇǻʔj˿̐DJ/ШɆɶŇǻ˾̎ϛЩ
anti ϕȈ˰ΊƑ˰½Ȯ²m°·°ĽǯUɆĪT Nd/Na ˢ̊ 2 ɠϥưΊƑ(2)VȲ΅ΞͿʔRDP.ƗïT NdCl3•6H2O.NaOtBu jĺȰRFgƛ˚˰Tȳʔj˿̐DJ/ȲΞͿʔUdgΊƑWȶƓVaVRŉ̕VΊƑǱ͎jɆDP9f.
²·ŇǻUaϔ˚Ń͎Q5gBRj˿ΘDJ/ШɆɶŇǻ˾̎ϛЩ
(3)ķƋɶ͎ŮΊƑjĘ˚D.N-m°w¯´m¯°¶½Зœ²®x§VÌ̊Vʈɠ̊ĝЛèj˚6gПЄǏTz¦´ZVΊƑ˰½Ȯ Mannich ŮĽǯjϒǻDJ/BheWĀƕʛǱ%-m¦-&-²wu°£´ϟVŇǻU
˶̭D.ĲͲŕV½ȮŇǻZVǯ˚;ɈǣChg/ШɆɶŇǻ˾̎ϛЩ

(4)m¦Vr®·VΊƑ˰ˬ˘ʔjɶνRFgĀƕʛǱŌ̨ĮŇˈ̿V˖ŻΞœŮŇǻʔj˿̐DJ/ШɆɶŇǻ˾̎ϛЩ(5)u°£´ϟRm¦´:eV͓ʇUdgΊƑ˰Tm¦ǝǻĽǯUɆĪTȲ΅¢p̨ΊƑНɡj΄6KDJ/ШɆɶŇǻ˾̎ϛЩ

2.4

po°˥ǳVˬ˧ɶɰΉȻVų́˾̎9dYIVǯ˚(1)¤¯tpo°˾̎1)ŋ̬̄ǱRNApo°Q5g¤¯tpo° (PV) WèĊâȤVɋ.Áɘ̢̬̄VϏī̬̪͍̄UęϒFg/ÃTâȤ̬ηW.ͷʜÁ:eͷʤ͔ϰϭ (BBB) j
ωϐD.Áɘ̢̬̄UðăFg̬ηR̓8ehP6g/IBQ.PVVBBBωϐɶɰjēƒ±°QȻe:UFgBRj˵˰RD.˾̎jώ`P<J/ɌǈǏ]QU̪͍Ċ̈͸ǱjɆFgȲ΅VЯNVPVƅʂ¡jŉƙDJ/Ш̔3˘ˈʛ
Ǳ˾̎ϛЩ
2)

ͲğjèĊUĪɗ˰UϏȣFgJ`Vdrug delivery system (DDS)jϮˬFgJ`U.»΍PVƅʂ¡V̪͍ȐŋǱjĘ˚FgȳϦQ˾̎jώ`P6g/Õ12ǥ.Ćŉ˾̎ÿ;ˑhhX.ȲD6DDSϮˬj͸6J6R̓8P6g/
Ш̔3˘ˈ
ʛǱ˾̎ϛЩ
(2)o´°r´po°˾̎
o´°r´po°W8ɌUē̚ĮChJRNA{§jȏN/8ɌVRNA{§;¸NV̞ƒUĿfτ]hgVUǭ΂TϝĕUN6PΉɕj͸MJ/]J.
ȼǈǏUǗ<̳<͏β®ǝǻϐ̉;Ȇo´°r´ͲVɲ˰RTgŃ͎Ǳ
UN6Pϴƞğj˚6PɬΌj͸MP6g/Ш̔3˘ˈʛǱ˾̎ϛЩ(3)HIV ˾̎
HIV-1 ;˙˘Fg˼ϩ RNA (short transcriptзST)Vǳ̈́èĊU9@gƓūǶ̀jȻe:UFgBRj˵˰U HIV−ЮϼǱ̈́VͷʤÁVǷɚ̪͍ĊU9@g
ST ɬĒʔVϮˬRIVΉɕjώ`P<J/IV̭ɗ.ST VˬˑϤWāˤVʛǱ
Į¥·u·Q5g CD8+T ̪͍V HLA-DR+RǛ>˷ϰFgBR;·ƥCh.HIVǳ̈́VȲJTāˤˊǸVȃȟʔQ5gBRj΄ĒD.Πȭˬͻj͸MJ/ˑū.
ŧ̐Ƿɚ˧˾̎ǿ.ɓÑƈƕĲ̇ƕ˾̎ǿ϶ư˦ϸRVĆŉ˾̎Q.͛ǋɬɜʔϮˬj˵ȐDJų˴˾̎jǗ<̳<ώ`P6g/Ш̔ 3 ˘ˈʛǱ˾̎ϛЩ

(4)B Ů͉ʾpo°˾̎
B Ů͉ʾpo°V{§΀ͿjЛīFgpo°ŢƒbơÃŢƒVÁ:e.ȲJTģͲɲ˰ēƒjŉƙFgBRj˵˰RDP.{§΀ͿUˉĮDJŲИ̪͍Γï̢jɰ̛DJ/ˑū.ɰ̛DJΓï̢j˚6JĮŇˈ®o®¯·9dYǨ˘ˈŲИʤVx¯·´yjώ`.po°{§΀ͿVēƒų˴UφgJ`VĮŇˈVĿǦj˵ȐDP6g/CeU.΄ĒDJĮŇˈUN6PW.IVé˚ɶǌUN6PΉɕjώ`P6g/Ш̔ 3 ˘ˈʛǱ˾̎ϛ.ɓÑƈ¶Ĳ̇ƕ˾̎ǿЩ

2.5

t·l·Vɰϋ˘ˈƕ˰˾̎(1)

t·l·VƐīW.Atg1-Atg13-Atg17-Atg29-Atg31 ΀ŇèШAtg1 ΀ŇèЩ
;ȊMP6g/w·VʛǱɌèQ5g Atg1 UN6P.ĄϬ͵ˮβjȹʹ̪͍:eƈϤΞͿFg̢j˿̐DJ/CeUǦehJĄϬ Atg1 j˚6P.ϣ˘Ů
Rŉ̕V Atg1 ΀Ňèj in vitro QČɰǻFgBRUǻĥDJ/Шēƒɰϋ˾̎ϛЩ(2)m¦¡·IШApe1ЩWŀƠè͵ˮβ Atg19 UdfΘΣChgBRQ.

t·l}·§ĊUϕȈ˰UϾЃChg/ȼǈǏǦehJɰϋǵŶUųO<13ɶ͎Ήɕjώ`J̭ɗ.Atg19 W Ape1 VĐЁèͻЊˉˢ˰ṶŇFgBR.I
V̭ɗ Ape1 ĐЁèV~ojΨUĚǧD.t·l}·§ĊUĿfτ]hgVUϔDJ~oUĚǧDP6gBRjȻe:UDJ/Шēƒɰϋ˾̎ϛЩ(3)t·l·UǭЎQ5f:Nɰϋɶ͎ǵŶ;\RkSǦehP6T6ЄˬˑǱAtgŢƒ̿ШAtg2, Atg9, Atg11ЩUN6P.ȹʹ̪͍ˬˑ̢9dYĒͥϞʃˬˑ̢jʛ˚FgBRQƈϤˬˑ̢Vɰ̛UǻĥDJ/CeUɰϋɶ͎ΉɕUíD
7g.ĳēT̥Ǐ]Q̟ͿŃ͎T̢j˿̐DJ/Шēƒɰϋ˾̎ϛЩ

2.6

ȹʹ²qxĎʹƃͩTSVȹʹ˦ĺ̡ˊͫUϰFg˾̎

(1)

˘˓ʛǱˈβVȘ̩ʱRTgĎʹƃͩjÁǬRDJȹʹ˦ĺ̡ˊͫVȗĿ.ēЃ.
ŲИj͸6.Ù΢˙ˈ®o®¯·jȍþFgRRaUrqnxjÖDJÙ΢˙ˈVƆɱĮVɬΌj͸MJ/ШʐʚȦǿЩ

2.7

ЄʏǱ̬̖̄˥ǳʏ˩ͲЄʏǱ̬̖̄˥ǳUƧFgʏ˩Ͳj˵ȐDJų˴˾̎
1. ̬̖̄˥ǳUĆϊFg˦ǸV¸NRDP̬̖̄șŇϛV͐Ǚ;5g/Ɍ˾̎Q
W.̬̖̄șŇϛVζŷRTgm°|¯´±·VĐЁʛǱjŋ»CH
gĮŇˈjȘ̩Fgx¯·´yj͸MP6g/ɌǈǏU96P.Ǩ˘ˈŲИˈ:e˵˰VʛǱjɆFg²jЮɟ΄ĒD.ˑū.IVʛǱΓïļYʛǱˈ
βV̟Ϳj͸MP6g/Ш̔а˘ˈʛǱ˾̎ϛ.ɓÑƈ,Ĳ̇ƕ˾̎ǿЩ
2. ЄʏǱ̬̖̄˥ǳQ5g͑ОǱ̖̺ͮ˧(SMA)VȲD6ʏ˩ʔϮˬj˵ȐDJƆȵΏĆŉĲǂÃƫʏМVƛȵ˾̎UĻ˞D.ÿ͸˾̎UPˋ͜UϮˬDJSMA ĺŢϖâƒ˙ˈQ5g SMN ͵ˮβVʭƙʔj˚6P.ʏМ~´°Vʭƙj͸MP6g/CeU.BheV˾̎jųU.Ȳ΅ SMA ͲȘ̩x¯·´y̢Vɰ̛jώ`P6g/Ш̔ 3 ˘ˈʛǱ˾̎ϛ.ɓÑƎƒĲ̇ƈЩ

3Ь˘ˈΰʱí̯.˘˓ʛǱˈβV®o®¯·Į
3.1

˘ˈΰʱVí̯(1)ͫŲИȉĒʤVȜí
Ȩ̶ͫR̪ͫjŇiHP 2,058 ɟUN6PʤèŲИ9dYŦèŲИj͸MJ/ɌŲИʤ9dYŲИȉĒʤ 2,764 ~´°jǿĊ9dYǿƅVĆŉ˾̎ÿZȜíD
J/Ш̔ 2 ˘ˈʛǱ˾̎ϛ.ǹǯƈ.ƻƕϸƈ.ŧĊÞɭЩ(2)̟ƣβϤj˚6JǨ˘ˈŲИˈV LC/MS ·ΉɕUN6P.̟ƣβϤ-óȏȾ

14

ϯ·

·jɂȲD.ŲИʤV¨£²·§Ήɕj͸MP6g/ШēƒɰϋΉ

ɕ.̔ 2 ˘ˈʛǱ˾̎ϛЩ

3.2z¦u°®o®¯·Vɰ̛(1)Bh]Qǜ˾̎ǿQĸЃŉƙChJƉˁĮŇˈ9dYŐσĮŇˈ.Ȳ΅ŇǻˈjÁǬU®o®¯·Įj͸6. ȲJU702ˈβj˭ϨDJ/Ш˻˰Ω˙ǵŶϛ.ΰʱ̙˓ƜЩ

(2)ǿĊƅZĮŇˈVí̯jÛ¼Vϊf͸MJ/Шŉ¸ˈβV΀ȫȜíŌ_Щ¶ ǿĊ 17~´°Ш̝èЩ.90±·Ш4710~´°Щ¶ ǿƅ

11~´°Ш̝èЩ.38±·Ш4212~´°ЩШ˻˰Ω˙ǵŶϛ.ΰʱ̙˓ƜЩ
(3)ĮŇˈVŐσǵŶj¸Ȏ̙˓FgJ`.··jƫăD.Č˭Ϩéɭjώ`gRŉȾU.Įƕɰϋ½ȻVaVW.ϔƚ NMR.MS jʭƙFg̕ǵŶV̟ɜjƛȵÁQ5g/Ш˻˰Ω˙ǵŶϛ.ΰʱ̙˓ƜЩ3.3ͫ®o®¯·Vɰ̛Ǩ˘ˈĮƕ˾̎ǿǿɆVx¯·´y˚ͫɟV®o®¯·ĮШČ˘.Č˭ϨЩj͸TMP6g/6]]Q.˭Ϩͫɟ̤ 40,000 ɟШȨ̶ͫ.̪ͫЩV7L 2/3 Û»jƘÉDJ/Č˘DJɟW.ŲИD²®o®¯·RDPČ˭ϨDP6g/
Шΰʱ̙˓ƜЩ4Ь˖Żϰό
4.1

˖ŻśАUƧFgǨ˘ˈVĘ˚ˬІǿ̕QϻȝAChJx®{ГVđ˓VɬΌШēΉRȖʇđ˓Щjώ`P6g/
ɌËɭVƻɭĮUŋ@P.Ȗʇđ˓˘ˈVƗƙ˰ƈϤ˘˙jϒǻDJ/ǨĮ˾RІĤá̃VËɭjÜÖFg˖Żϰόá̃RW.ǜΕȂ͹VĘ˚.Ȃ͹̈μUN6Pƌ̤;ǻ̐DŚŕĮDJШʐʚȦǿ.ŧĊÞɭЩ/ɌËɭUϰόDJˉΐWF[
Pǻ̐DJ/ШŧĊ.ŧƅW¸ϛƦɜÁЩ

15

4.2

p§.²´p§VϳϹğVȘ̩ŧĊQȗЁDJȊƒͫ Pisolithus orientalis ƒƛè:eȶ˻V Cs ϕȈ˰ȔQ5g
Norbadione A jͯϤĸЃD.ɴ͏ȊȏʔUdf Cs šľ©°ƛМj͸6 Cs šľ;Ń͎Q5gBRĵDJ/Pisolithus orientalis VʤèŲИj͸6.®|ŲИɑÝɬΌV̭ɗ Norbadione A WŲŬÁVu¯p§ʻǏjϔǏUʪEJŲŬQŲИFgBRQɄƈ 150'g/mL V˘˙ǱĵFBR;Ȼe:UTMJ/Ш˻˰Ω˙ǵŶϛ.ŧĊƈƕЩ

5Ь˻˰Ω˙.ǊŶËɭ
5.1

˻˰Ω˙
ɌǈǏVˉΐĒВȫ 16 ÝШŧĊˉΐ 10 Ý.ŧƅˉΐ 6 ÝЩQ5MJ/

5.2

ǊŶËɭ
¼΍VƑèUP˾̎ǿVɯ΂.˾̎ĊƠ.˾̎ǻɗjˬôDJ/ɌǈǏV«·¯¯·9dYǜ˾̎ǿ;Ŀf»AehJȲ͇ˬͻVΖ̪Wė̦/¶ǈŶ¶´±
¶¢·§¡·¶ «·¯¯·6Ьƕ͹ȓ͞
6.1

Ȫ͊9dY˾̎ȐƫŧĊƅVĹſ˾̎ŗ.ƈƕϸ˘.Ķɭ˾̎˘̕jŀ@ăh.Ȫ͊9dY˾̎Ȑƫ
j͸MJ/

(1)

Ȫ͊
¶

ȸɈèМƕ́VƛȵШ˾͈̎ƛŬwª¯mȪ͊9dYǿĊ΄ƕЩ/ǹǯ̀źƈƕͲƕϛЮǈ˘9dYˈ˓Įƕ˾̎Ɯ/ (2015.8.27)(2)˾̎ŗVŀ@ăh˾̎ȐƫVɌǈǏŀ@ăhˊʑj¼΍U΍F/Ш7Lʢƅ:eVŀăȫЩ¶ Ĺſ˾̎ŗ  

12 (9)

Ŋ¶ ƈƕϸ˘   2Ŋ¶ õſ˾̎ŗ  

2 (2)

Ŋ

¶ Ķɭ˾̎˘  6Ŋ¶ JSPS ˉė˾̎ŗ

1 (3)

Ŋ

16

6.2
1Щ

˾̎ǿΡ̀
mĮƕjų˴RDJ˘Œ̇ƕ˾̎UǢ̐Nēƒό̭ʔVϮˬ̪ΥƔþ ȪȕШɓÑĲ̇ɼ̇ƈƕ ˘èɏȰƻƕ˾̎ǿ ˘ŒɆɶĮƕēϣЩȴ ǨĮ˾ (2015.4.22)

2Щ

Novel Phospholipid Probes for Exploring Biomembrane Functions and Their
Behavior in Model Membranes
Dr. Jin CuiШɆɶŇǻ˾̎ϛЩȴ ǨĮ˾ (2015.5.22)

3Щ

Identification of FumarateHydratase Inhibitor̓Ċ øȭĹſШɆɶŇǻ˾̎ϛЩȴ ǨĮ˾ (2015.5.29)

4Щĸ˒R;k̪͍˷Íé˚W, ĸ˒ēĮR;k̪͍ʣʸjñώFgй̪͍ƅ¥¯xRV̪͍ș˺VǢĢйТǮ˛ĞĹſШǁÑƈƕĲƕϛ Ǩ˘ˈƕΡǐЩȴ ǨĮ˾ʐʚȦǿ (2015.6.4)

5Щ

Unfolding the New Electronic State of Phenalenyl: From Organometallics toSpin Electronics
Prof. Swadhin Mandal (Department of Chemical Sciences, Indian Institute ofChemical Education and Research, Kolkata)ȴ ǨĮ˾ (2015.6.18)

6ЩɫˈVāˤǯ̗R˦ĺͫVǷɚǼˡƹЧ ĨШυˣƈƕ¶ςƕϛЩȴ ǨĮ˾ (2015.07.10)

7Щ

Noncovalent Interactions in Organocatalysis
Prof. Petri M. Pihko (Jyväskylä University, Finland)ȴ ǨĮ˾ (2015.7.10)

8Щ

Radical-based couplings towards the total synthesis of tigliane/daphnane
diterpene
Daisuke Urabe, Ph.D(Graduate School of Pharmaceutical Sciences,
The University of Tokyo)ȴ ǨĮ˾ (2015.07.30)

9)ʢʙmx¯m˜ɒȲ΅̪͍ǯ̗ĚǧˈβVĸЃRɶ͎Ήɕƈϣ õШƻƕϸƈƕ¶ÿώƻƕϛ˘ŒĮƕ̇Щȴ ǨĮ˾ (2015.08.04)

17

10)

Ȳ΅˘˓ʛǱˈβVȘ̩ʔVˑūŬ-¯£·§ƻƕ:e{§¥o´y]QƬΥ˹ÈШЈƳƈƕςƕ˾̎̇ħȪЩȴ ǨĮ˾ (2015.10.15)

11)Studies of Natural Product Synthesis – Target-Inspired Innovation
Prof. David Ransom Williams (Department of Chemistry, Indiana
University, Bloomington, Indiana, U.S.A.)ȴ ǨĮ˾ (2015.11.12)

12)“C(sp3)-H Bond Functionalization Mediated by Hydride Shift/Cyclization
Systemɩ ŜÌШɓÑςƻƈƕƈƕϸƻƕ˾̎ϸ ǯ˚ĮƕϛϭďȪȕЩȴ ǨĮ˾ (2015.12.07)

13)

MAP w·y°̬ηĚǧɶɰVΉȻRģͲZVƯϮ

йLessons from fission yeastйɎʟ УƒШυˣƈƕͲƕϛ ēƒĲ˩¶{§ģͲƕ˾̎Ɯ ȪȕЩȴ ǨĮ˾ʐʚȦǿ (2016.1.6)
14)

ϠϞģͲU9@gȨ̶ͫVľЁRϕėɐɔ̆͸ ШƬɖͿͲЩȴ ǨĮ˾ (2016.1.13)

15)

Asymmetric Pd-NHC catalyzed C(sp3)-H activation: synthesis ofenantioenriched indolines.
Prof.Peter Kundig (Emeritus Professor, University of Geneva)ȴ ǨĮ˾ (2016.2.18)

16)

Carbene Catalysis and Breslou Intermediate
Prof. Dr. Albrecht Berkessel(Department of Chemistry University of

Colognc)ȴ ǨĮ˾ (2016.3.23)
7Ь˾̎ħǻą˲ʔÓRDP.Û¼Vħǻj͸MJ/¶

1,235 ĴċŧϿĮƕ˩ʔƕáɤʍʼƊα¶3,000 ĴċǹǺ̀źƈƕ˓ƻƕϛǯ˚Įƕ̇Ǩ˘ˈ˘˙ˈV̇ƕ˰˾̎

¶100 Ĵċ

ą˲ΩţʔÓȷɌǷɚ˧ĲͲŕķáJA Medal ƢØϥ18

8ЬɤʺʼƊ΍ǰКVĘ˚ñώĘ˚ñώVJ`¼΍Véɭj͸MJ¶Ư̂ˈVІƒĮ

¶±ompƂɂ¶Ư̂±·V¯«·m°¶Ư̂ˈVȍþ

¶ƅɒ̈́V΄ƕɢĊ

9ЬÃ΂ɶŠVë˚ˊʑ(1)ɠ̀ʆĆС (NMR) ¡x°VʭƙǨ˘ˈĮƕ˾̎ǿШɌǿЩUΏ̽ChP6gǇǻ 16 ǈƫăVȷɌІƒͿ ECA600
ɠ̀ʆĆСͼ̽W.ēĀ΋̕ɂȲVJ`Ǉǻ 28 ǈ 6 ɅÙ˽9dY¸ϛŐσɶŠjɿDPǔɹDJ/ɌǈǏVʭƙȫW.557 ÝQ5MJ/Ɍǈ 10 ɅUȲ΅ƫă
ChJȷɌІƒͿ ECZ600R ɠ̀ʆĆСͼ̽VʭƙȫW.979 ÝQ5MJ/Ǉǻ
22 ǈƫăVȷɌІƒͿ ECS400 ɠ̀ʆĆСͼ̽W.Ȳɨ̈μUã6.Ǉǻ 27 ǈ
5 ɅUʐʚȦǿÜΏDJ/Ɍͼ̽VʭƙȫW.1,897 ÝQ5MJ/
ȷňȦǿUΏ̽ChP6g°u·̃Ϳ AVANCE III 500 Ů NMR ͼ̽ШǇǻ
23 ǈ 11 ɅUƫăЩW.Ȳɨ̈μUã6.Ǉǻ 27 ǈ 5 ɅUɌǿÜΏDJ/ɌǈǏVʭƙȫW.2,638 ÝQ5MJ/
ȷňȦǿUΏ̽ChP6g°u·̃Ϳ AVANCE III HD 400 ŮШǇǻ 24 ǈ 10ɅƫăЩW.Ȳɨ̈μUã6.Ǉǻ 27 ǈ 5 ɅUɌǿÜΏDJ/ɌǈǏVʭƙ
ȫW.19,948 ÝQ5MJ/(2)ʤèx²¥y®n·/βϤēɕ¡x° (LC/MS/MS) VʭƙǨ˘ˈĮƕ˾̎ǿШɌǿЩUΏ̽ChP6gǇǻ 19 ǈ 7 ɅƫăV~·©n
ª·~or´nnx̃Ϳ LTQ Orbitrap βϤēɕ΋VɌǈǏVʭƙȫ
W.åēƒ; 4,368 Ý.²t¦x; 528 ÝQ5MJ/
ȷňȦǿUΏ̽ChP6g~·©nª·~or´nnx̃Ϳʤèx²¥y®n·ЭβϤēɕͼ̽ (Accela/LTQ XL)ШǇǻ 19 ǈ 9 ɅƫăЩǇǻ
27 ǈ 6 ɅṴŇVJ`ɌǿÜΏDJ/ɌǈǏVʭƙȫW.1,575 ÝQ5MJ/(3)

βϤēɕ¡x° (MS) VʭƙǨ˘ˈĮƕ˾̎ǿШɌǿЩUΏ̽ChP6gǇǻ 14 ǈǏƫăVȷɌІƒͿ
T100LC βϤēɕͼ̽VɌǈǏVʭƙȫW.9,874 ÝQ5MJ/Ǩ˘ˈĮƕ˾̎ǿШɌǿЩUǇǻ 25 ǈ 9 ɅƫăVƴʚͿéǿͿ AXIMA TOF2 β19Ϥēɕͼ̽VɌǈǏVʭƙȫW.1,910 ÝQ5MJ/(4)γɜŮІƒБǨϪVȥǡǨ˘ˈĮƕ˾̎ǿUΏ̽ChP6gȷ̐ SU1510 Ůj˚6P.Ȩ̶ͫ̕ 6 šVȥǡj͸MJ/ɶɥWЍΞUϏμChP6g/(5)ωϐŮІƒБǨϪVȥǡǨ˘ˈĮƕ˾̎ǿUΏ̽ChP6gUΏ̽ChP6gȷ̐ H-7100 ŮШǇǻ 2 ǈǏȷɌ͜μλȓ͞á;ħϥЩ̪ͫ̕ 4 šVȥǡj͸MJ/ɶɥWЍΞUϏμCh
P6g/

(6)

ƈŮǨ˘ˈŲИͼ̽Ǩ˘ˈĮƕ˾̎ǿUΏ̽ChP6gΏ̽ChP6g(ɟ)Âͬotr´̃Ϳ
MSJ-U3 30L Ů.9dY MPF-U3 200L Ůª·l·¨´·ШǇǻ 4 ǈǏȷɌ͜μλȓ͞á;ħϥЩW.ЍΞǓīDP6g/ɌǈǏUϏμChJšȫW.
MSJ-U3 30L Ů; 28 š.MPF-U3200L Ů; 8 šQ5g/

(7)

˶ΜŮ

·up´Ш¥¯x 9600 u·ЩǨ˘ˈĮƕ˾̎ǿШɌǿЩUΏ̽ChP6gu·¥¯x9600)˶ΜŮ·up´ШǇǻ6ǈǏȷɌ͜μλȓ͞á;ħϥЩWë˚ChT:MJ/ϛ

ŕ̕ͿϋÁɹǥǈȫa̬MP9fǔɧÊƙQ5g/(8)ʤè´±·­´up´ШTri-Carb2800TR·w´r°¥·ЩǨ˘ˈĮƕ˾̎ǿШɌǿЩUΏ̽ChP6g·w´r°¥·Tri-Carb2800TR ʤè´±·­´up´WЍΞǓīDP9f.18š.3240~´°ʭƙ
j͸MJ/

(9)

ĺƒōĀͼ̽
Ǉǻ 21 ǈ 3 ɅUǨ˘ˈĮƕ˾̎ǿШɌǿЩUΏ̽/ʢ˙ʉȢ˘ˈVđ˓ƻ̉Qˬ˘FgǔʇUŌ]hgϢϥưШˉUu¦p§ЩVʭƙj͸MP6g/(10)и̶ɰϋΉɕͼ̽Ш¯vx VariMax with RAPIDЩǇǻ 23 ǈ 7 Ʌ.Ǩ˘ˈĮƕ˾̎ǿШɌǿЩUΏ̽/´xβ̭ɀVwª®x¯·­´9dYšȇ·ľЁ.åēƒĮŇˈVšȇ·ľЁUĘ˚D

P6g/ɌǈǏÁU 4 ̊ГV´xβ̭ɀVwª®x¯·­´UĘ˚D.

IheWȨƩĀȵΏjĘ˚FgBRQɰϋʋƙUǻĥDJ/]JåēƒĮŇˈU

20

N6PW.58 ̊ГV̭ɀUN6Pšȇ·ľЁ9dYɰϋʋƙUǻĥDJ/(11)¯·ēʗ§ШTTP LabTech mosquitoЩǇǻ 23 ǈ 6 Ʌ.Ǩ˘ˈĮƕ˾̎ǿШɌǿЩUΏ̽/´xβ9dYåēƒĮ
ŇˈV̭ɀĮɑÝx¯·´yUĘ˚DP6g/ɌǈǏÁṲ 15 ¹ɑÝV̭ɀĮɑÝɬΌUë˚Ch.´xβ9dY´xβ-ĮŇˈ΀ŇèUϰDP
18 ̊ГV̭ɀɕĒUǻĥDJ/(12)

In vivo o¨·´y§¶t¯´ OV110
Ǉǻ 19 ǈ 11 ɅʐʚȦǿUΏ̽/ͶĀ´xβ GFP jƗƙƫăDJ;k̪͍ɟj·5g6Ww¥pV˱¼9dYŉǿÜɫDJ̢j˚6
P.x¯·´yQDJĮŇˈVĚ˪ʛǱjΓïDP6g/(13)ʤèx²¥y®n·/βϤēɕ¡x° (LC/MS/MS) VʭƙʐʚȦǿUǇǻ 24 ǈ 12 ɅƫăV~·©nª·~or´nnx̃ͿQ Exactive βϤēɕ΋VɌǈǏVʭƙȫW 3,162 ÝQ5MJ/

10ЬǨ˘ˈĮƕ˾̎̕UϰFgŧϿÐʜ
10.1

ŧϿƕáTSZVĒǃ ШΖ̪Wė̦UʨØDJЩŧϿƕáTSUĒǃD.˾̎ǻɗVˬͻ9dY˾̎ό̮¶ǵŶÐȞTSj͸MJ/

10.2
1)

ʢƅdfVɒΎ̈́
Prof. Swadhin Mandal
Department of Chemical Sciences, Indian Institute of Chemical Education andResearch/Kolkataȴ ǨĮ˾ (2015.06.18)

2)

Prof. Petri M. Pihko
Jyväskylä University/Finlandȴ ǨĮ˾ (2015.06.18)

3)

Prof. David Ransom Williams
Department of Chemistry, Indiana University, Bloomington, Indiana, U.S.A.
ȴ ǨĮ˾ (2015.11.12)

4)

Prof. Dr. Peter Kundig
Department of Organic Chemistry, University of Genevaȴ ǨĮ˾ (2016.02.18)

21

5)

Prof. Dr. Albrecht Berkessel
Department of Chemistry, University of Cologneȴ ǨĮ˾ (2016.03.23)

11ЬƧƅ˰T˾̎ˬͻ (Πȭ.ƕáˬͻ.Ȳ͇Ŷϑ.ŀα̕VΖ̪Wė̦UʨØDJ/)¶ƕáЂΗTSVˬͻΠȭ

40 Ŷ

¶

ȌǣΡʶ

25 Ý

¶

ƕáˬͻ

81 Ý

¶

ˉΐĒВ ŧĊˉΐ6Ý¶ˉΐĒВ ŧƅˉΐ

2Ý

¶

ŀα

1Ý

22

ė̦

ШЮЩƕáЂΗTSVˬͻΠȭ
1)Synthesis of caprazamycin B.
H. Abe, P. Gopinath, G. Ravi,L. Wang, T. Watanabe, M. Shibasaki.
Tetrahedron Lett., 78, 3782-3785, 20152)

Atg1 family kinases in autophagy initiation.
N. N. Noda and Y. Fujioka.
Cell. Mol. Life Sci., 72, 3083-3096, 20153);kRϯβV˷Íé˚jĘ˚DJ;kVȄĚƹ˛ƕ.ň˛ʸɷϚ.ŭɌõ¸ƛМĲƕШżĔЩ,33, 199-203, 2015

4)

Synthesis and structure-activity relationship study of NBRI16716B, an
antitumor natural product.
H. Abe, C. Sakashita, M. Kawada, A. Nomoto, T. Watanabe, M. Shibasaki.
Chem. Pharm. Bull., 63, 463-468, 20155)

The werner protein acts as a coactivator of NF-κB on HIV-1 and IL-8
promoters.
T. Mizutani, A. Ishizaka, and Y. Furuichi
J. Biol. Chem., 290, 18391-18399, 2015

6)

Structure of the Atg101–Atg13 complex reveals essential roles of Atg101 in
mammalian autophagy initiation.
H. Suzuki, T. Kaizuka, N. Mizushima and N. N. Noda.
Nat. Struct. Mol. Biol., 22, 572-580, 20157)

Asteltoxins from the entomopathogenic fungus pochonia bulbillosa 8-H-28
H. Adachi, H. Doi, Y. Kasahara, R. Sawa, K. Nakajima, Y. Kubota, N.
Hosokawa,
K. Tateishi, A. Nomoto
J Nat Prod., 78,1730-1734, 20158)

9)

A novel anti-microtubule agent with carbazole and benzohydrazide structures
suppresses tumor cell growth in vivo.
M. Ohira, Y. Iwasaki, C. Tanaka, M. Kuroki, N. Matsuo, T. Kitamura, M.
Yukuhiro, H. Morimoto, N. Pang, B. Liu, T. Kiyono, M. Amemiya, K. Tanaka,
K. Yoshida, N. Sugimoto, T. Ohshima, M. Fujita.
Biochim Biophys Acta., 1850, 1676-1684, 2015
Direct catalytic asymmetric conjugate addition of saturated and unsaturated
thioamides.
N. Majumdar, A. Saito, L. Yin, N. Kumagai and M. Shibasaki.

23

10)

11)

12)

Org. Lett.,17, 3362-3365, 2015
Natural lipopeptide antibiotic tripropeptin C revitalizes and synergisticallypotentiates the activity of beta-lactams against methicillin-resistant
Staphylococcus aureus
H. Hashizume, Y. Takahashi, S. Harada and A. Nomoto.
J Antibiot., 68, 373-378, 2015
Synthesis and antibacterial activity of 1-N-[(S)-(-amino-2-hydroxyalkyl]
derivatives of dibekacin, 5-deoxydibekacin, 3’-deoxykanamycin A andgentamicin B.
E. Umemura, Y. Sakamoto, Y. Takahashi and T. Miyake.
J Antibiot., 68, 421-423, 2015t·l·VƐījĚǧFg΀ŇèV̐èɰϋͳƳüƒЪϣ˛Ư˘ȷɌ̭ɀƕáΗ, 2015, 57, 191-197

13)

Managing the retro-pathway in direct catalytic asymmetric aldol reaction of
thioamides.
Y. Bao, N. Kumagai, M. Shibasaki.
Chem. Sci., 6, 6124-6132, 2015

14)

ĲͲŕVĪˎ˰½ȮŇǻjǮŋDJķƋɶ͎Ů½ȮΊƑVϮˬ˂Υ˶Ŗ.ɛƵɺĭĮƕƻɭ, 66, 31-41, 2015

15)

Synthesis and Determination of Absolute Configuration of Lentztrehalose A
M. Zhang, S. Wada, F. Amemiya, T. Watanabe and M. Shibasaki
Chem. Pharm. Bull., 63, 961-966, 201516)

Novel autophagy inducers lentztrehaloses A, B and C
S. Wada, Y. Kubota, R. Sawa, M. Umekita, M. Hatano, S. Ohba, C. Hayashi,
M. Igarashi and A. Nomoto.
J Antibiot., 68, 521-529, 201517)

Stereoselective total synthesis of KAE609 via directcatalytic asymmetricalkynylation to ketimine.
H. Takada, N. kumagai, M. Shibasaki.
Org. Lett., 17, 4762-4765, 201518)

2014 ǈ ʞ˛αŀαΠȭ Ȩ̶ͫjĖ`RFgŪž̪ͫ˜ɒVɆ˚ȆͫˈβVȘ̩Ré˚ɶǌΉɕɵ˄̆ɴȷɌȨ̶ͫƕáΗ, 29, 8-12, 2015

19)

Open and closed HORMAs regulate autophagy initiation.
H. Suzuki, T. Kaizuka, N. Mizushima and N. N. Noda.
Autophagy., 11, 2123-2124, 2015

24

20)

The thermotolerant yeast kluyveromyces marxianus is a useful organism forstructural and biochemical studies of autophagy.
H. Yamamoto, T. Shima, M. Yamaguchi, Y. Mochizuki, H. Hoshida, S. Kakuta,
C. Kondo-Kakuta, N. N. Noda, F. Inagaki, T. Itoh, R. Akada and Y. Ohsumi
J. Biol. Chem., 290, 29506-18, 201521)

Direct catalytic asymmetric mannich-type reaction of α-N3 amide.
Z. Sun, K. Widener, N. Kumagai and M. Shibasaki.
Chem. Eur. J., 21, 17574, 201522)

Direct catalytic asymmetric mannich-type reaction of α-and β-fluorinatedamides.
L. Brewitz, F. Arteaga, L. Yin, K. Alagiri, N. Kumagai, M. Shibasaki.
J. Am. Chem. Soc., 137, 15929-15939, 201523)

Coccoquinones A and B, new anthraquinone derivatives produced by
Staphylotrichum coccosporum PF1460
D. Tatsuda, M. Amemiya, R. Sawa, K. Sumiyoshi, T. Watanabe, I. Momose,
M. Kawada, A. Nomoto and M. Shibasaki
J Antibiot., 69, 176-178, 201624)

The therapeutic potential of microbial proteasome inhibitors.
I. Momose and M. Kawada
Int Immunopharmacol. 2015 in press

25)

Synthesis and antibacterial activity of tripropeptin C derivatives containing
the pyrimidine ring system.
S. Hirosawa, Y. Takahashi, A. Murotani, H. Hashizume, T. Miyake and Y.
Akamatsu.
Heterocycles, 91, 2143-2151, 2015

26)

Structural basis of the differential function of the two C. elegans Atg8
homologs, LGG-1 and LGG-2, in autophagy.
F. Wu, Y. Watanabe, X. Y. Guo, X. Qi, P. Wang, H. Y. Zhao, Z. Wang, Y.
Fujioka, H. Zhang, J. Q. Ren, T. C. Fang, Y. X. Shen, W. Feng, J. J. Hu, N. N.
Noda, H. Zhang.
Mol. Cell 60, 914-929, 201527)П̕˘ˈVt·l·ƐīUǭЎTŢƒ Atg101 VɰϋRɶ͎
ϧɉʠĈ.ϣ˛Ư˘ȷɌ̭ɀƕáΗ, 57, 324-330, 2015

28)

Synthesis and antibacterial activity of 4” or 6”-alkanoylamino derivatives ofarbekacin.

25

K. Sasaki, Y. Kobayashi, T. Kurihara, Y. Yamashita, Y. Takahashi, T. Miyake
and Y. Akamatsu.
J Antibiot., 68 741-747, 201529)

Transferrin Receptor 1 Facilitates Poliovirus Permeation of Mouse Brain
Capillary Endothelial Cells
T. Mizutani, A. Ishizaka and C. Nihei
J. Biol. Chem., 291, 2829-2836, 201630)

Catalytic asymmetric synthesis of key intermediate for scytophycin C
J. Cui, T. Watanabe, M. Shibasaki
Tetrahedron Lett., 57, 446-448, 201631)

Bladder cancer stem-like cells: their origin and therapeutic perspectives.
T. Ohishi, F. Koga, T. Migita.
Int. J. Mol. Sci., 17, 201632)

Direct catalytic asymmetric mannich-type reaction of α,β-unsaturated
γ-butyrolactam to ketimines.
S. Lin, N. Kumagai, M. Shibasaki
Chem. Eur. J., 22, 3296-3299, 201633)

Atg101: not just an accessory subunit in the autophagy-initiation complex
N. N. Noda and N. Mizushima.

Cell Struct. Funct., 41, 13-20, 201634)

Electrophilic activation of α,β-unsaturated amides; catalytic asymmetricvinylogous conjugate addition of unsaturated γ-butyrolactones
M. Zhang, N. Kumagai, M. Shibasaki.
Chem. Eur. J., Accepted, 2016

35)

Report on the use of non-clinical studies in the regulatory evalution of
oncology drugs.
Y. Hayakawa, M. Kawada, H. Nishikawa, T. Ochiya, H. Saya, H. Seimiya, R.
Yao, M. Hayashi, C. Kai, A. Matsuda, T. Naoe, A. Ohtsu, T. Okazaki, H. Saji,
M. Sata, H. Sugimura, Y. Sugiyama, M. Toi, T. Irimura.
Cancer Sci., 107, 189-202, 2016

36)

Structural basis for the regulation of enzymatic activity of Regnase-1 bydomain-domain interactions.
M. Yokogawa, T. Tsushima, N. N. Noda, H. Kumeta, Y. Enokizono, K.
Yamashita, D. M. Standley, O. Takeuchi, S. Akira and F. Inagaki.
Sci. Rep., 6, 22324, 201637)

Heparanase augments inflammatory chemokine production from colorectal

26carcinoma cell lines
N. Tsunekawa, N. Higashi, Y. Kogane, M. Waki, H. Shida, Y. Nishimura, H.
Adachi, M. Nakajima, T. Irimura,

Biochem. Biophys. Res. Commun., 469, 873-83, 201638)

Preparation of Nd/Na heterogeneous catalyst from bench-stable andinexpensive Nd salt for an anti-selective catalytic asymmetric nitroaldol
reaction.
Nonoyama, K. Hashimoto, A. Saito, N. Kumagai, M. Shibasaki.
Tetrahedron Lett., 57, 1815-1819, 201639)w®¯n·jĚǧDPʿ̨jNTAg―ƉˁˈVΊƑ˰½ȬŇǱ
ɛЧɺĭ.ʫσİĮƕŉÓ Įƕ ˉЁ, Vol. 71, No. 4

40)

Short intracellular HIV-1 transcripts as biomarkers of residual immune
activation in patients on antiretroviral therapy.
A. Ishizaka, H. Sato, H. Nakamura, M. Koga, T. Kikuchi, N. Hosoya, T.
Koibuchi,A. Nomoto, A. Kawana-Tachikawa and T. Mizutani
J Virol, In press, 2016ШЯЩͯɃ,̷Ё,˳õ̕1)ƈƕϸΡ̀ ɆɶĮƕШ̔ЯˆЩɛЧɺĭ ̷ЁɓÑĮƕŉÓ(2015)2)ȷɌͲƕá̷ ´·Ͳƕ¯· II̔ 8 ƾ Ͳƕ˾̎ɛЧɺĭɓÑĮƕŉÓ(2015)
3)

ps·±´ ɆɶĮƕ ¼ ̔ЯˆɛЧɺĭ ˳ΑɓÑĮƕŉÓ(2015)4)ĮƕɰϋRͲ˓é˚)ĲͲŕjĮƕ˰UΜ_)Ш̔ЯˆЩ
ɛЧɺĭ
ǕƹɃǎ

5)

(2015)

Įƕ˩ʔƕШ̔ЯˆЩɛЧɺĭ ˳õǕƹɃǎ Ш2016Щ27

ШаЩȌǣΡʶ1)2015 Merck Millipore Asia Forum
A novel evaluation method of survival motor neuron protein as a biomarker ofspinalmuscular atrophy by imaging flow cytometry
Masayuki Arakawa
2015 ǈ 4 Ʌ 20 ȷ (ɓÑ)2)

BIT's 8th Annual World
Protein & Peptide Conference-2015
A novel evaluation method of survival motor neuron protein as a biomarker ofspinal muscular atrophy
Masayuki Arakawa
2015 ǈ 4 Ʌ 27 ȷ (Nanjing/China)

3)

̔ 25 š΍ǰ¹Ɇ̅Ƴ´¤p§ķƋɶ͎½ȮΊƑ¶ɄυVώɻɛЧɺĭ
2015 ǈ 5 Ʌ 16 ȷ (ÇƺƈƕĲƕϛ/̅Ƴ)4)

̔ 245 šɅìͲƕ¦·ķƋɶ͎½ȮΊƑ¶ɄȲVώɻɛЧɺĭ
2015 ǈ 6 Ʌ 19 ȷ (ЈƳ˸̐ƈƕ/ЈƳ)5)

̔ 15 šȷɌ͵ˮβ̇ƕáǈá
1t·l·UdgϕȈ˰͵ˮβēΉVɰϋų˴2ϣ˛Ư˘2015 ǈ 6 Ʌ 24 ȷ (5i=k¢·°/ǩƴ)6)˓˾´¤p§ж̔ 10 šɆɶŇǻĮƕV²´nmķƋɶ͎Ů½ȮΊƑVϮˬRĲͲŕŇǻZVǯ˚˂Υ˶Ŗ2015 ǈ 6 Ʌ 26 ȷ (˓Įƕ˾̎ǿ/œĀ)7)

Organic Synthesis Symposium
Recent progress in cooperative asymmetric catalysis.
ɛЧɺĭ2015 ǈ 7 Ʌ 1 ȷ (ɓÑƻɭƈƕ/ɓÑ)

8)

University of Alicante
Exploration of Cooperative Asymmetric Catalysis Toward Efficient Synthesis ofTherapeutics

28

Naoya Kumagai2015 ǈ 7 Ʌ 06 ȷ (University of Alicante/ Spain)
9)

21st European Conference on Organometallic Chemistry (EuCOMC XXI)
Recent progress in cooperative asymmetric catalysis.
Masakatsu Shibasaki
2015 ǈ 7 Ʌ 9 ȷ (Bratislava/Slovakia)

10)

Symposium the 8th Negishi-Brown Lectures
Recent progress in cooperative asymmetric catalysis.
Masakatsu Shibasaki
2015 ǈ 7 Ʌ 14 ȷ (Indiana/USA)

11)

Meiji Seika l°¥ķƋɶ͎Ů½ȮΊƑVϮˬRĲͲŕŇǻZVǯ˚˂Υ˶Ŗ2015 ǈ 7 Ʌ 24 ȷ (ɳʞ)12)

University of Bern, special lectures
Exploration of Cooperative Asymmetric Catalysis Toward Efficient Synthesis ofTherapeutics.
Naoya Kumagai2015 ǈ 8 Ʌ 21 ȷ (Bern/Switzerland)

13)

University of Bologna, special lectures
Exploration of Cooperative Asymmetric Catalysis Toward Efficient Synthesis ofTherapeutics.
Naoya Kumagai2015 ǈ 9 Ʌ 1 ȷ (Bologna/Italy)  Aalto University, special lectures
Exploration of Cooperative Asymmetric Catalysis Toward Efficient Synthesis ofTherapeutics.
Naoya Kumagai2015 ǈ 9 Ʌ 4 ȷ (Helsinki/Finland)
15)

University of Jyvaskyla, special lectures
Exploration of Cooperative Asymmetric Catalysis Toward Efficient Synthesis ofTherapeutics.
Naoya Kumagai2015 ǈ 9 Ʌ 7 ȷ (Jyvaskyla/Finland)16)

̔ 53 šȷɌ˘ˈˈ˓ƕáǈát·l·VƐījȊ7 Atg1/ULK ΀ŇèVɰϋRɶ͎

29

ϣ˛Ư˘
2015 ǈ 9 Ʌ 15 ȷ (ϥʍƈƕΈϯwª´/ϥʍƿ)17)υˣƈƕͲƕϛåēƒĮŇˈUdg;k·ϯβ˷Íé˚jÖDJ;kVȄĚƹ˛ƕ
2015 ǈ 9 Ʌ 26 ȷ (υˣƈƕͲƕϛ/ƈϲ)18)ɓÑςƻƈƕ
ķƋɶ͎Ů½ȮΊƑVϮˬRĲͲŕŇǻZVǯ˚˂Υ˶Ŗ2015 ǈ 10 Ʌ 16 ȷ (ɓÑςƻƈƕ/ɓÑ)

19)

ʟœПɞ
·

°Įƕαŀα÷;̈́RŶϑ(2012 ǈɇȷ.2013 ǈΜƁ.2014 ǈʄȷ.˙̬.

2015 ǈɓÑ.ΜƁ.˙̬)Chg]QVϑ̉ɛƵɺĭ2015 ǈ 11 Ʌ 6 ȷ (ʟœПɞ/Ŵˏ)20)̔еšt·l·˾̎á
ϕȈ˰t·l·Vɰϋ˘ˈƕ˰˾̎ϣ˛Ư˘2015 ǈ 11 Ʌ 16 ȷ (ʥηƇ͠ńćǑ˸)

21)

International Conference on “Current Challenges in Drug Discovery Research"(CCDDR 2015)
Synthesis of anti-TB and anti-cancer natural products
Takumi Watanabe
2015 ǈ 11 Ʌ 23 ȷ (Jaipur/India)

22)

ICAT International Symposium in Madrid: Asymmetric C-C Bond Formation &Organometallics
Recent Progress in Cooperative Asymmetric Catalysis
Masakatsu Shibasaki
2015 ǈ 11 Ʌ 30 ȷ (Madrid/SpainЩ

23)

PACIFICHEM 2015
Recent Progress in Cooperative Asymmetric Catalysis.
ɛЧɺĭ2015 ǈ 12 Ʌ 20 ȷ (Hawaii/USA)24)

The 8th Korea-Japan Chemical Biology Symposium
Modulators of the Tumor-Stromal Cell Interactions Reveal New Targets for
Anti-Tumor Strategy

30

Manabu Kawada
2016 ǈ 1 Ʌ 19 ȷ (nx¢°ʌ̹/Ϙ΃)25)

̔ 89 šȷɌͲ˓ƕáǈát·l·ăϭϣ˛Ư˘2016 ǈ 3 Ʌ 11 ȷ (n|ɳʞ/ɳʞ)ШбЩƕáˬͻ
1)

̔ 69 š ɆɶŇǻĮƕķáϰɓȦϛ´¤p§Direct catalytic asymmetric mannich-type eaction of α-azido amide.
Zhongdong Sun, Karin Weidner, Naoya Kumagai, Masakatsu Shibasaki
2015 ǈ 5 Ʌ 16 ȷ (ɳʞŧ̐ƈƕ/ɳʞ)2)

̔ 69 š ɆɶŇǻĮƕķáϰɓȦϛ´¤p§Catalytic asymmetric mannich-type reaction of N-alkylidene-αaminoacetonitrile with ketimines.
Shaquan Lin, Yuji Kawato, Naoya Kumagai, Masakatsu Shibasaki
2015 ǈ 5 Ʌ 16 ȷ (ɳʞŧ̐ƈƕ/ɳʞ)3)

̔ 69 š ɆɶŇǻĮƕķáϰɓȦϛ´¤p§
Spirastrellolide A VΊƑ˰½ȮĄŇǻ˾̎П˛ř.ł͟ô.ϺЈʕ.ʫσİ.ɛЧɺĭ2015 ǈ 5 Ʌ 16 ȷ (ɳʞŧ̐ƈƕ/ɳʞ)4)

̔ 13 šɷ¿ÙjȊ7ɆɶĮƕ´¤p§Catalytic generation of α-CF3 enolate for the asymmetric synthesis of chiralCF3-substituted carbon atoms: direct catalytic asymmetric addition of
α-CF3 amide to C=N/C=O electrophiles
Lennart Brewitz, Liang Yin, Akinobu Matsuzawa, Naoya Kumagai, Masakatsu
Shibasaki
2015 ǈ 5 Ʌ 23 ȷ (̐ŒКƈƕ/ʴί˸)5)ȷɌēƒɲ˰ʏ˩ƕá ̔ 19 šƕ͹Ёá
1GAPDH VēʓjÖDJϯβ̪͍Udg;k̪͍VżʀȄĚ2
ƹ˛ƕ.ň˛ʸɷϚ.Ï»ͽǉ.ƈǒò¸.ż˛ǫ.ƱЧƕ.Ɩç̾ßó̾.
ŭɌõ¸.ϵϛĀ.ʫϗİ.ϣɌȻ˝.ɛЧɺĭ2015 ǈ 6 Ʌ 11 ȷ (ɔƱĄȷ̏¢°/ɔƱ)6)ȷɌēƒɲ˰ʏ˩ƕá ̔ 19 šƕ͹Ёá
1Ȳ΅ĮŇˈw®´ГVp53îƓ˰T̪͍żʀϴƞ2̐˛ƈπ.˯ʽ ĥ.ЖƴɺƤ.ƈǒò¸.ŨƙƔƊ.ƹ˛ƕ.ɛЧɺĭ312015 ǈ 6 Ʌ 11 ȷ (ɔƱĄȷ̏¢°/ɔƱ)7)ȷɌēƒɲ˰ʏ˩ƕá ̔ 19 šƕ͹Ёá
1Ȇ;kʛǱĵF GAPDH :eΏ΋DJåēƒ¡Vɶ͎Ήɕ2ň˛ʸɷϚ.ƹ˛ ƕ.ϣɌȻ˝.ɛЧɺĭ2015 ǈ 6 Ʌ 11 ȷ (ɔƱĄȷ̏¢°/ɔƱ)8)ȷɌēƒɲ˰ʏ˩ƕá ̔ 19 šƕ͹Ёá
1Ȳ΅Ȇĝ̐͘;kˈβandroprostamine AVȆ͖˨ʛǱ2
ƱƵʙƒ.ż˛ǫ.ƹ˛ƕ.˯ʽĥ.ɛЧɺĭ2015 ǈ 6 Ʌ 12 ȷ (ɔƱĄȷ̏¢°/ɔƱ)

9)Molecular Chirality Symposium 2015
Managing the Retro-Pathway in Direct Catalytic Asymmetric Aldol Reactions of
Thioamides.
Youmei Bao, Naoya Kumagai, Masakatsu Shibasaki
2015 ǈ 6 Ʌ 12 ȷ (Waseda University/Tokyo)

10)

Negative Stand Virus Meeting 2015
Oseltamivir Expands Quasispecies of Influenza Virus through Cell-to-cell
Transmission.
Kohtaro Mori
2015 ǈ 6 Ʌ 14-20 ȷ (Siena /Italy)

11)

ISACS16 (Challenges in Chemical Biology)
Natural product as tool for exploration of tumor-stroma interaction
Takumi Watanabe, Hikaru Abe, Manabu Kawada, Junjiro Yoshida, Akio Nomoto
and Masakatsu Shibasaki
2015 ǈ 6 Ʌ 16-17 ȷ (Zurich /Switzerland)

12)

Organometallic Chemistry Directed Toward Organic Synthesis 18 (OMCOS 18)
Catalytic Generation of α-CF3 Enolate for Producing Chiral Building Blocks with
CF3-Containing Stereogenicity
Naoya Kumagai, Lennart Brewitz, Liang Yin, Fernando Arteaga, Akinobu
Matsuzawa, Kaliyamoorthy Alagiri, Masakatsu Shibasaki
2015 ǈ 6 Ʌ 30 ȷ (Barcelona/Spain)13)

̔ 4 š NGS ˑŷVá
NGS jĘ˚DJo´°r´po°{§ RNA ̞ƒĊ̐èϝ̽ΉɕʔVϮˬʵʍ˶Ƽ
2015 ǈ 7 Ʌ 2-3 ȷ (N>XŧϿáΤŷ/ͨŰ) ̔  š BMS |´l±´
MALDI-TOFMS j˚6JɆ˚Ǩ˘ˈQ5gȨ̶ͫVΣėUN6P

32

ʺ̑¸.Пɵͽƒ.ʕƆϣœɴ.ÎĳƷЀÅ.ɤʍʙÌ.ĦͳĴȻ.ɛЧɺĭ
2015 ǈ 7 Ʌ 6 ȷ (Ʋϱ)15)

̔ 42 š BMS |´l±´
MALDI-TOFMS j˚6JȨ̶ͫVēГVΔ^
Пɵͽƒ.ʺ ̑¸.ʕƆϣœɴ.ÎĳƷЀÅ.ɤʍʙÌ.ĦͳĴȻ.ɛЧɺĭ2015 ǈ 7 Ʌ 7 ȷ (Ʋϱ)16)

̔ 17 šȷɌ RNA ƕáǈáo´°r´po° RNA {§Vz·´yUϢ΂T RNA ©·Vŉƙʵʍ˶Ƽ.Ƭɪ̀ò.ɖ ŘÈ.Фƹ БШɍǆЩ

17)

̔ 24 šȷɌ;kμ̈ƕáƕ͹Ёá
1Ƭ̪͍͋˪V͜ˁμ̈©°U9@g͙´xβ CXADR VǶ̀VɬΌ2ŭɌõ¸.ƹ˛ ƕ.Ï»ͽǉ.ƈǒò¸.ǉ˛ʘƒ.ɦƹ˲̣.ɎʟЀÔ.ʟϣŔƒ.
ʇΥƀĘ.Ɩç̾ßó̾.ż˛ ǫ.ϣɌȻ˝.ɛƵɺĭ2015 ǈ 7 Ʌ 23 ȷ (n®ƈϲ/ƈϲ)18)

̔ 24 šȷɌ;kμ̈ƕáƕ͹Ёá
1ϯβ̪͍Udg GAPDH VēʓjÖDJ;k̪͍VżʀĚǧ2ƹ˛ ƕ.ŭɌõ¸.ň˛ʸɷϚ.Ï»ͽǉ.ƈǒò¸.ż˛ ǫ.ƱЧ ƕ.
Ɩç̾ßó̾.ϵϛ Ā.ʫϗ İ.ϣɌȻ˝.ɛЧɺĭ2015 ǈ 7 Ʌ 24 ȷ (n®ƈϲ/ƈϲ)19)̔ЮšȷɌ̖ƕáƕ͹Ёá
1͑ОǱ̖̺ͮ˧ĺŢϖâƒ˙ˈ  ͵ˮβVȲ΅ɬĒʔ2ͪƹɺ͸.ͪƹːƒ.ЇɉÒƒ.ƈɅĈƒ.ϣɌȻ˝.ɛƵɺĭ.ȯͳĦÙƒ
2015 ǈ 8 Ʌ 8 ȷŧ̟̐̄¶̬̄Ĳ˩˾̎´·ɓÑ

20)

21st International Symposium on Fluorine Chemistry, Como, Italy
Catalytic Generation of α-CF3 Enolate: Direct Catalytic Mannich-type anAldol
Reactions.
Naoya Kumagai, Lennart Brewitz, Fernando A. Arteaga, Liang Yin,
Kaliyamoorthy Alagiri, Akinobu Matsuzawa, Masakatsu Shibasaki
2015 ǈ 8 Ʌ 28 ȷ (Como/Italy)

21)

1;k˾̎ēϣVˉǱ̕jι]8JȦȡʛī2;kͦȀ˾̎̈́³·x­
Ȇ;kʛǱˈβȘ̩VJ`V°·mo̢Vɰ̛ƸɌ͆ƒ.ϣŭĴϡ.ʬ̾ũƒ.ʹΥɺŅ.ƹ˛ƕ2015 ǈ 9 Ʌ 4 ȷͱ̇y®´¢°ʵVʯϬϣ
22)

̔ 30 šȷɌȨ̶ͫƕáƈá
Lentzea ưȨ̶ͫ˜ɒ trehalose Г̸è lentztrehalose ГVɰϋR˘ˈʛǱ

33œ˛ò¸.ʺ̑¸.ƈǒò¸.ɚϣŘÈ.Äó˛˜̾ƒ.ʕƆϣœɴ.ɤį]b.
ǚȻ.ʫσİ.ɖĴͩ.ƹ˛ƕ.ÎĳƷЀÅ.ɛЧɺĭ2015 ǈ 9 Ʌ 8 ȷ (ƤƱŧϿáΤŷ/ƤƱ)23)

̔ 30 šȷɌȨ̶ͫƕáƈá
MALDI-TOF MS j˚6Jʦʢ˜ɒ Micromonospora ưͫ̊VΣėʕƆϣœɴ.Пɵͽƒ.ʺ̑¸.ÎĳƷЀÅ.ĦͳĴȻ. ɛЧɺĭ2015 ǈ 9 Ʌ 8 ȷ (ƤƱŧϿáΤŷ/ƤƱ)24)̔šȷɌƢ˘ʹƕá¶ɓȷɌȦϛƈáw®ГVƬ͍èU9@gϕėρψUϰigēƒͼ̽VΉɕÌ˗ʠ¸.Ǉ˛ЦŎ.Пɵ͢œ.ɤʍʙÌ.ɛЧɺĭ
2015 ǈ 9 Ʌ 26 ȷ (ĴÙ˛ı/ɓÑ)
25)

The 20th International World Muscle Society Congress
A novel evaluation method of survival motor neuron protein as a biomarker ofspinal muscular atrophy
Masayuki Arakawa, Reiko Arakawa, Ryoko Aoki, Akio Nomoto, Masakatsu
Shibasaki, Kayoko Saito
2015 ǈ 10 Ʌ 1 ȷ (Brighton/UK)

26)

̔ 74 šȷɌ˪ƕáƕ͹̵áQuinofuracins: new bioactive compounds induced p53-dependent growth
suppression.
Daisuke Tatsuda, Masatomi Iijima, Manabu Kawada, Isao Momose, Akio
Nomoto, Masakatsu Shibasaki.

27)

̔ 74 šȷɌ˪ƕáƕ͹̵á
A small peptide from the region of cell growth inhibitory activity in GAPDH
inhibits the growth of gastric cancer cells
Junjiro Yoshida, Manabu Kawada, Akio Nomoto, Masakatsu Shibasaki.
2015 ǈ 10 Ʌ 8 ȷ (ŊłƮŧϿáΤŷ/ŊłƮ)28)̔šȷɌ˪ƕáƕ͹̵áInhibitory activity of Ertredin on in vitro sphere formation and in vivo tumor
growth of EGFRvIII expressing cells
Sonoko Atsumi, Chisato Nosaka, Hayamitu Adachi, Tomoyuki Kimura,
Yoshihiko Kobayashi, Hisashi Takada, Takumi WatanabeShun-ichi Ohba,
Hiroyuki Inoue, Manabu Kawada, Masakatsu Shibasaki, Akio Nomoto, M
Shibuya2015 ǈ 10 Ʌ 9 ȷ (ŊłƮŧϿáΤŷ/ŊłƮ)29)̔šȷɌ˪ƕáƕ͹̵á

34

Analysis of the role of a membranous protein CXADR in an orthotopic metastatic
model for human small cell lung cancer.
Shuichi Sakamoto, Manabu Kawada, Hiroyuki Inoue, Shunichi Ohba, Yasuko
Kohda, Masunori Kajiakawa, Masahito Sugiura, Sakiko Urano, Taketoshi
Mizutani, Ihomi Usami, Tohru Masuda, Akio Nomoto, Masakatsu Shibasaki.
2015 ǈ 10 Ʌ 9 ȷ (ŊłƮŧϿáΤŷ/ŊłƮ)30)̔šȷɌ˪ƕáƕ͹̵á

Construction of screening system for a novel AR signaling inhibitor
Yohko Yamazaki, Isao momose, Manabu Kawada, Masakatsu Shibasaki
2015 ǈ 10 Ʌ 9 ȷ (ŊłƮŧϿáΤŷ/ŊłƮ)31)̔šȷɌ˪ƕáƕ͹̵á

Stromal cells negatively modulates the growth of cancer cells by the secretion of
GAPDH
Manabu Kawada, Junjiro Yoshida, Hiroyuki Inoue, Shun-ichi Ohba, Shuichi
Sakamoto, Tohru Masuda, Manabu Yamasaki, Ihomi Usami, Hikaru Abe,
Takumi Watanabe, Akio Nomoto, Masakatsu Shibasaki 2015 ǈ 10 Ʌ 10 ȷŊłƮŧϿáΤŷŊłƮ32)

̔  šĽǯRŇǻVώɻ´¤p§˶ǽ˰T½Ȯm°w°ĮUdgȆ¥®¯mͲ   V½ȮŇǻП˛Äş.˂Υ˶Ŗ.ɛƵɺĭ
2015 ǈ 10 Ʌ 26 ȷυˣƈƕ  Ʌ¢·°ƈϲ

33)

̔  šɆɶŇǻ´¤p§mo´¯°m¦j˚6Jo±xŮΊƑ˰½Ȯm°·°ĽǯVϮˬϣ˛̆ò.# ! !#.ɔʺǠô."!"!$!.ЅƝĎɴ.˂Υ˶ɴ.
ɛЧɺĭ
2015 ǈ 11 Ʌ 5 ȷȸ̋˛ƈƕŧϿáΤŷɓÑ

34)

27th AACR- NCI-EORTC International Conference on Molecular Targets andCancer Therapeutics
Stromal cells suppress cancer development by secreted GAPDH-E-cadherininteraction
Manabu Kawada, Junjiro Yoshida, Hiroyuki Inoue, Shun-ichi Ohba, Manabu
Yamasaki, Ihomi Usami, Shuichi Sakamoto, Hikaru Abe, Takumi Watanabe,
Akio Nomoto, Masakatsu Shibasaki 2015 ǈ 11 Ʌ 6 ȷ£´̜ŧ

35)

The 13th International Kyoto Conference on New Aspects of Organic Chemistry(IKCOC-13)

35

Catalytic Generation of α-CF3 Enolates for Asymmetric Mannich-Type Reactions
Lennart Brewitz, Fernando Arteaga Arteaga, Liang Yin, Kaliyamoorthy Alagiri,
Naoya Kumagai, Masakatsu Shibasaki
2015 ǈ 11 Ʌ 10 ȷRihga Royal Hotel KYOTO/ÑϜ
36)

The Eighth International Forum on Chemistry of Functional Organic Chemicals(IFOC-8)
Development of Direct Catalytic Asymmetric Aldol Reaction of 7-Azaindoline
AmidesHidetoshi Noda, Karin Weidner, Akinobu Matsuzawa, Zhongdong Sun, Fuyuki
Amemiya, Naoya Kumagai, and Masakatsu Shibasaki
2015 ǈ 11 Ʌ 16 ȷRihga Royal Hotel KYOTO/ÑϜ37)

The Eighth International Forum on Chemistry of Functional Organic Chemicals(IFOC-8)
Enantioselective Synthesis of KAE609 Based on Direct Catalytic AsymmetricAlkynylation of Ketimine
Hisashi Takada, Naoya Kumagai, Masakatsu Shibasaki
2015 ǈ 11 Ʌ 16 ȷRihga Royal Hotel KYOTO/ÑϜ38)

The Eighth International Forum on Chemistry of Functional Organic Chemicals(IFOC-8)
Managing Retro-Reaction in Direct Catalytic Asymmetric Aldol Reaction of
Thioamides
Youmei Bao, Naoya Kumagai, Masakatsu Shibasaki
2015 ǈ 11 Ʌ 16 ȷRihga Royal Hotel KYOTO/ÑϜ

39)

The Eighth International Forum on Chemistry of Functional Organic Chemicals(IFOC-8)
Enantioselective Synthesis of α,β-Diamino Acid Derivatives through Direct
Catalytic Asymmetric Mannich-Type Reaction of α-Azido Amide
Zhongdong Sun, Karin Weidner, Naoya Kumagai, Masakatsu Shibasaki
2015 ǈ 11 Ʌ 16 ȷ (Rihga Royal Hotel KYOTO/ÑϜ)

40)̔еšt·l·˾̎á
PAS VÁɠ΀ŇèV in vitro ČɰǻRʳʤɰϋΉɕͳƳüƒ
2015 ǈ 11 Ʌ 16 ȷʥηƇ͠ń/ćǑ˸41)̔еšt·l·˾̎áϕȈ˰t·l·U9@gu·}͵ˮβVζŷǱUǯEJŀƠèUdgΘΣɶɰVϓ6VΉȻ36ƱƵ̒ǩ
2015 ǈ 11 Ʌ 16 ȷ (ʥηƇ͠ń/ćǑ˸)42)

6th International Symposium on Advances in Synthetic and Medicinal
Chemistry
Catalytic Asymmetric Synthesis of Caprazamycin B and Caprazol
Takumi Watanabe, Purushothaman Gopinath, Lu Wang, Hikaru Abe,
Gandamala Ravi, Takashi Masuda, Masakatsu Shibasaki Oral presentation
2015 ǈ 11 Ʌ 18 ȷ (Rehovot/Israel)43)̔šȷɌpo°ƕáƕ͹Ёámpo°x·jų˴RDJpo°{§΀ͿΓï̢UdgȆ  ğVȘ̩ƱЧƕ.ɔ˛ʔǲ.υͳƬέ.ϧɉ]fB.ϫµʊͽ̾.ȯͳʒ.ϣɌȻ˝.ɛЧɺĭ2015 ǈ 11 Ʌ 22 ȷ (̅ƳŧϿáΤŷ̅Ƴ)44)

̔ 63 šȷɌpo°ƕáƕ͹Ёá
AdV j˚6JĪˎ˰ HBV ΀Ϳ{§ɬĒʔVϮˬυͳƬέ.ϧɉ]fB.ƱЧƕ.ɛЧɺĭ.ȯͳʒ.ϫµʊͽ̾2015 ǈ 11 Ʌ 22 ȷ (̅ƳŧϿáΤŷ/̅Ƴ)45)

̔ 63 šȷɌpo°ƕáƕ͹Ёá
Identification of RNA motifs for efficient packaging of influenza A virus genome.
Naoki Takizawa, Akio Nomoto, Masakatsu Shibasaki

2015 ǈ 11 Ʌ 22 ȷ (̅ƳŧϿáΤŷ/̅Ƴ)46)

̔ 38 šȷɌēƒ˘ˈƕáǈá¶̔ 88 šȷɌ˘ĮƕáƈáŇŉƈá
ĺʹ GPI m´u·Ů´xβϕė±·VΉɕÌ˗ʠ¸.Ǉ˛ЦŎ.Пɵ͢œ.ɤʍʙÌ.ɛЧɺĭ2015 ǈ 12 Ʌ 1 ȷ (̄Ǿ¤·mo®´/ćǑ)47)

BMB2015(̔ 38 šȷɌēƒ˘ˈƕáǈá,̔ 88 šȷɌ˘Įƕáƈá Ňŉƈá)t·l·Ɛī΀ŇèU9@gП̕˘ˈUŦɆTŢƒ Atg101 VɰϋRɶ͎
ϧɉʠĈ.ΧŸĞǮ.ʇƴȺ.ϣ˛Ư˘2015 ǈ 12 Ʌ 3 ȷ (̄Ǿ¤·mo®´ćǑ)

48)

MB2015(̔ 38 šȷɌēƒ˘ˈƕáǈá,̔ 88 šȷɌ˘Įƕáƈá Ňŉƈá)
±t·l}·§ɰϋèVÁɠ΀ŇèV in vitro ČɰǻRǱˊΉɕͳƳüƒЪƱɌɖЪϧɉ͂, ƈϽ͢Ĉ, ϣ˛Ư˘2015 ǈ 12 Ʌ 3 ȷ (̄Ǿ¤·mo®´ćǑ)49)

BMB2015(̔ 38 šȷɌēƒ˘ˈƕáǈá,̔ 88 šȷɌ˘Įƕáƈá Ňŉƈá)ϕȈ˰t·l·ȾU9@gʤ͍ĦʇēΉϞ̨ Ape1 VΘΣɶɰVΉȻ

37ƱƵ̒ǩ, ʫϗỤ̌, ζ̐i:T, ˰ŷ¸ȿ, ɣʡͽƽ, ϧɉϙǤ, ÁǾƹÔ, ƈϽ͢Ĉ, ̋ůĎǞ, ϣ˛Ư˘2015 ǈ 12 Ʌ 3 ȷ (̄Ǿ¤·mo®´ćǑ)
50)

JST ȲȂ͹ΛȻáƙϤ˰ PCR ʔUdg HIV ʷàǷɚ̪͍VɬĒR˦ǸȃȟʔʇΥƀĘ.˽ŭǟ2015 ǈ 12 Ʌ 8 ȷ (JST ɓÑɌϛėК 1F ¢·°/ɓÑ¶ƿzΥ)

51)International Symposium on Molecular Technology(pre-symposium of Pacifichem 2015)
Interplayof

Self-Assembling

Catalyst

andCarbonNanotubes

forContinuous-Flow Catalysis
Naoya Kumagai2015 ǈ 12 Ʌ 13 ȷ (Aqua Waikiki Wave, Hawaii/USA)
52)

Pacifichem 2015
Solid Phase Catalysts Confined in Multiwalled Carbon Nanotubes: Catalytic
Asymmetric Nitroaldol and Mannich-type Reactions in a Continuous-Flow
Platform
Naoya Kumagai, Kazuki Hashimoto, Masakatsu Shibasaki
2015 ǈ 12 Ʌ 16 ȷ (Hilton Hawaiian Village, Hawaii/USA)

53)

Pacifichem 2015
Synthesis and structure activity relationship study of Intervenolin and
NBRI16716 B, modulators of tumor-stroma interaction of natural origin
Hikaru Abe, Chiharu Sakashita, Manabu Kawada, Junjiro Yoshida, Hiroyuki
Inoue, Shun-ichi Ohba, Tohru Masuda, Akio Nomoto, Takumi Watanabe,
Masakatsu Shibasaki
2015 ǈ 12 Ʌ 18 ȷ (Hawaii Convention Center, Hawaii/USA)54)

The 8th Korea-Japan Chemical Biology Symposium
Novel compounds suppressing p53-dependent growth of tumor cells
Daisuke Tatsuda, Isao Momose, Shun-ichi Ohba, Yoji Umezawa, Ryuichi Sawa,
Takumi Watanabe, Takao Kunisada, Masatomi Iijima, Manabu Kawada, Akio
Nomoto, Masakatsu Shibasaki
2016 ǈ 1 Ʌ 19 ȷ (nx¢°ʌ̹/Ϙ΃)55)

Ǉǻ 27 ǈǏ1öè±°QV;k˾̎Ȧȡʛī2³·x­·¥pZVŉǿ̈ɫUdgƬ̪͍͋˪V͜ˁμ̈©°VϮˬRǯ˚ŭɌõ¸.Ï»ͽǉ.ƈǒò¸.ɦƹ˲̣.ɎʟЀÔ.ʟϣŔƒ.ǉ˛ʘƒ.
Ɩç̾ßó̾.ż˛ǫ.ϣɌȻ˝.ɛƵɺĭ.ƹ˛ƕ2016 ǈ 2 Ʌ 4 ȷ (˔˕ʮ¢°/ʴί)

38

56)

̔ 10 šȷ̜˪ŇŉáΤ
Stromal cells negatively modulate the growth of cancer cells by the secretion of
GAPDH
Manabu Kawada, Junjiro Yoshida, Hiroyuki Inoue, Shun-ichi Ohba, Manabu
Yamasaki, Ihomi Usami, Shuichi Sakamoto, Hikaru Abe, Takumi Watanabe,
Akio Nomoto, Masakatsu Shibasaki
2016 ǈ 2 Ʌ 17 ȷ (Hawaii/USA)57)

̔  šȷ̜˪ŇŉáΤ
Papyracillic acid and penicillic acid show preferential cytotoxicityto humanpancreatic cancer cells under nutrient-deprived conditions.
Isao Momose, Yohko Yamazaki, Hayamitsu Adachi, Kengo Sumiyoshi,
Manabu Kawada, Masakatsu Shibasaki
2016 ǈ 2 Ʌ 19 ȷ (Hawaii/USA)58)

̔  šȷ̜˪ŇŉáΤ
Construction of screening system for new AR signaling inhibitors
Yohko Yamazaki, Isao Momose, Manabu Kawada, Masakatsu Shibasaki
2016 ǈ 2 Ʌ 19 ȷ (Hawaii/USA)59)

̔ 85 šȷɌƢ˘ʹƕáƈá¯·¥U9@gƬ͍èϕėρψ§VΉɕÌ˗ʠ¸.Пɵ͢œ.ɤʍʙÌ.ɛЧɺĭ
2016 ǈ 3 Ʌ 19 ȷƝƵ

60)

Gordon Research Seminar; Autophagy in Stress, Development & Disease
Structural Mechanisms Underlying Receptor-Mediated Selective Autophagy of
Aggregated Aminopeptidase I
Akinori Yamasaki, Yasunori Watanabe, Wakana Adachi, Kuninori Suzuki,
Kazuaki Matoba, Hiromi Kirisako, Hiroyuki Kumeta, Hitoshi Nakatogawa,Yoshinori Ohsumi, Fuyuhiko Inagaki and Nobuo N. Noda
2016 ǈ 3 Ʌ 19, 21-22 ȷVentura Beach Marriott, Ventura, CA, USA

61)

Gordon Research Conference: Autophagy in Stress, Development & Disease
Structural basis of the autophagy initiating PAS assembly.
Nobuo N. Noda
2016 ǈ 3 Ʌ 22 ȷ (Ventura Beach Marriott/Ventura, CA, USA)62)ȷɌͲƕá̔ 136 ǈá
α-m-7-mo´¯´m¦j˚6J¯°t²¨°z´ZVo±xŮΊƑ˰½Ȯm°·°ĽǯVϮˬЅƝĎɴ.ϣ˛̆ò.Karin Weidner.˂Υ˶Ŗ.ɛƵɺĭ

39

2016 ǈ 3 Ʌ 28 ȷ (ɳʞ)
63)ȷɌͲƕá̔ 136 ǈá
Pd(II)ΊƑUdg¨±´ sp3 ʿ̨-ʇ̨̭ŇʛǱĮjĘ˚DJx²m°w°m¦´V 3 äm¯·°ĮRm°z°Įϰʧ, Рɵ͢Ƚ, ɛЧɺĭ
2016 ǈ 3 Ʌ 28 ȷ (ɳʞ)

64)ȷɌͲƕá̔136ǈá»˱ǻϬŢƒŀƠèƂˢèv-ˬˑ̪͍VζŷЉîƓǱżʀϴƞʛǱjɆFgåēƒĮŇˈVɰϋʛǱ˷ϰ˾̎ɉɐɁÅ.ʬ̾ũƒ.łɖ͢Ǟ.ϣŭĴϡ.ƸɌ͆ƒ.ƹ˛ƕ.ʹΥɺŅ.ʫσİ.
ɛЧɺĭ
2016 ǈ 3 Ʌ 28 ȷ (ɳʞ)

65)ȷɌͲƕá̔136ǈá
RubratoxinVΊƑ˰½ȮĄŇǻ˾̎
ƈĊÔǮ.ʫσİ.ɛЧɺĭ2016 ǈ 3 Ʌ 28 ȷ (ɳʞ)

66)

2nd International Symposium for Medicinal Sciences
Androprostamine A, a New Antitumor Agent for Castration Resistant Prostate
CancerYohko Yamazaki, Tohru Masuda, Isao Momose, Manabu Kawada, Akio Nomoto,
Masakatsu Shibasaki
2016 ǈ 3 Ʌ 28 ȷɳʞ

67)

2nd International Symposium for Medicinal Sciences
Anti-Tumor Activity of Geraniin in Osteosarcoma
Daisuke Tatsuda, Isao Momose, Shun-ichi Ohba, Yoji Umezawa, Manabu
Kawada, Akio Nomoto, Masakatsu Shibasaki
2016 ǈ 3 Ʌ 28 ȷɳʞ

68)

2nd International Symposium for Medicinal Sciences
Natural lipopeptide antibiotic tripropeptin C revitalizes and synergisticallypotentiates the activity of beta-lactams against methicillin–resistant
Staphylococcus aureus
Hideki Hashizume, Yoshiaki Takahashi, Shigeko Harada, Masayuki Igarashi
and Akio Nomoto
2016 ǈ 3 Ʌ 28 ȷɳʞ

69)ȷɌςͤĮƕáMALDI-TOF MS j˚6JȨ̶ͫVΣė40Пɵͽƒ.ʕƆϣœɴ.ÎĳƷЀÅ.ʺ̑¸.ɤʍʙÌ.ĦͳĴȻ2016 ǈ 3 Ʌ 29 ȷ (ɍǆ)
70)ȷɌͲƕá̔ 136 ǈá
Direct Catalytic Asymmetric Mannich-Type Reaction of α-Alkyl Amide
Fernando A. Arteaga, Zijan Liu, Lennart Brewitz, Jianyang Chen, Bo Sun,
Naoya Kumagai, Masakatsu Shibasaki
2016 ǈ 3 Ʌ 29 ȷ (ɳʞ)71)ȷɌͲƕá̔ 136 ǈá
Direct Catalytic Asymmetric Mannich-type Reaction of α- and β-FluorinatedAmidesLennart Brewitz, Fernando A. Arteaga, Liang Yin, Kaliyamoorthy Alagiri, Naoya
Kumagai, Masakatsu Shibasaki
2016 ǈ 3 Ʌ 29 ȷ (ɳʞ)72)ȷɌͲƕá̔ 136 ǈá
Cu/Pd o¨¯xΊƑUdg α-¯°t²¨°m¦V α-½Ȯm¯°ĮĽǯVϮˬХͳΚ.˂Υ˶Ŗ.ɛƵɺĭ2016 ǈ 3 Ʌ 29 ȷ (ɳʞ)73)ȷɌͲƕá̔ 136 ǈá
DirectCatalytic

Asymmetric

Mannich-type

Reactionof

α,β-Unsaturated

γ-Butyrolactam with Ketimines
Shaoquan Lin, Naoya Kumagai, and Masakatsu Shibasaki
2016 ǈ 3 Ʌ 29 ȷ (ɳʞ)74)ȷɌͲƕá̔ 136 ǈáƗï¶ƗƙT Nd Źj˚6g Nd/Na ˢ̊ЯɠϥưΊƑVȲ΅ΞͿʔVϮˬ
ϣ0ƱǠÓ.ɵɌœɴ.ХͳΚ.˂Υ˶Ŗ.ɛƵɺĭ2016 ǈ 3 Ʌ 29 ȷ (ɳʞ)75)ȷɌͲƕá̔ 136 ǈá
α,β-½Зœ 7-mo´¯´m¦VʈІƒ˰ʛǱĮUdg½Зœ²®x´ГVΊƑ˰½Ȯo±xŮĆǢØĦĽǯ
ǚȻ.˂Υ˶Ŗ.ɛƵɺĭ2016 ǈ 3 Ʌ 29 ȷ (ɳʞ)76)ȷɌͲƕá̔ 136 ǈá
7-mo´¯´m¦j˚6Jo±xŮΊƑ˰½Ȯm°·°ĽǯVϮˬϣ˛̆ò.Karin Weidner.ɔʺǠô.Zhongdong Sun. ЅƝĎɴ.˂Υ˶Ŗ.
ɛƵɺĭ

41

2016 ǈ 3 Ʌ 29 ȷ (ɳʞ)77)ȷɌςͤĮƕá 2016 ǈǏƈáʦʢǍʖ˜ɒȨ̶ͫÌɷÙ΢˙ˈ:eVȲ΅²smVˬ΄̓ͣǓǘ.ʺ̑¸.ÎĳƷЀÅ.ʕƆϣœɴ.ɤį]b.ɖĴͩ.ɤʍʙÌ.
ĦͳĴȻ
2015 ǈ 3 Ʌ 29 ȷ (ɍǆ)78)ȷɌςͤĮƕá 2015 ǈǏƈáʦʢǍʖ:eVȨ̶ͫVēЃ.ēГRÙ΢ˈVƆɱǱʕƆϣœɴ.Пɵͽƒ.ʺ̑¸.ÎĳƷЀÅ.ĦͳĴȻ2016 ǈ 3 Ʌ 29 ȷ (ɍǆ)79)ȷɌͲƕá̔136ǈá
ȆεƆğͅǱ̭ɠĮŇˈCPZEN-45VŇǻ˾̎̓Ċøȭ.ʫσİ.ɛЧɺĭ2016 ǈ 3 Ʌ 29 ȷ (ɳʞ)80)ȷɌͲƕá̔136ǈá
ScytophycinCVΊƑ˰½ȮĄŇǻ˾̎ƶώ.ʫσİ.ɛЧɺĭ2016 ǈ 3 Ʌ 29 ȷ (ɳʞ)81)ȷɌͲƕá̔136ǈá;k-ϯβ˷Íé˚Uû>ƉˁˈLeucinostatinAVΊƑ˰½ȮĄŇǻ˾̎ϵϛĀ.ƹ˛ƕ.ʫσİ.ɛЧɺĭ2016 ǈ 3 Ʌ 29 ȷ (ɳʞ)ШвЩ«·¯¯·1)П̕˘ˈVt·l·VƐīUǭЎTŢƒV̐èɰϋjΉȻēƒɰϋΉɕϛ2015 ǈ 6 Ʌ 2 ȷ

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2015ǈ8Ʌ20ȷ

2)ʐʚȦǿ˯ʽʙƒ»̧˾̎ŗVΠȭ;.The Journal of AntibioticsU96P.

42

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