. 2020 Nov 26;85(11):1389–1421. doi: 10.1134/S0006297920110097

Table 1.

Small-molecule inhibitors of eukaryotic ribosome

Name	Class, group of chemical substances	Specificity (B, A, E)^#	Interacting ribosomal subunit	Binding site^##	Stage of the translation cycle^###	Effect on polysomes^####	Mechanism of action
Anisomycin/flagecidin	pyrrolidine, anisomycin group	A, E	60S	PTC (A)	E	stab	PTC inhibitor
Deacetylanisomycin	– // –	E	60S	PTC (A)	E	stab?	– // –
Preussin/L-657,398	– // –	E	60S	PTC (A)?	E?		– // –
Calonectrin	trichothecene A		60S?	PTC (A)?	E	stab/dis	– // –
Neosolaniol	– // –	E	60S?	PTC (A)?	E?	?	– // – ?
Scirpentriol	– // –	B, A, E	60S	PTC (A)	E	dis	– // –
Diacetoxyscirpenol/anguidine	– // –	B, A, E	60S	PTC (A)	E	dis	– // –
T-2 toxin	– // –	E	60S	PTC (A)	E	dis	– // –
T-2 triol	– // –	E	60S?	PTC (A)?	E?	?	– // – ?
Trichodermin	– // –	E	60S	PTC	E	stab/dis	– // –
Trichodermol	– // –	E	60S	PTC	E	stab	– // –
Diacetylverrucarol	– // –	E	60S?	PTC (A)?	E?	?	– // – ?
Trichothecolone	– // –	B, A, E	60S?	PTC (A)?	E?	stab/dis	– // – ?
Trichothecin	trichothecene B	E	60S	PTC (A)?	E	stab/dis	– // –
Fusarenone X	– // –	E	60S	PTC	E	stab	– // –
Vomitoxin/deoxynivalenol	– // –	E	60S	PTC (A)	E	dis	– // –
Nivalenol	– // –	E	60S?	PTC (A)?	E?	dis	– // – ?
Crotocin	trichothecene C	E	60S	PTC (A)	E, T?	stab	– // – ?
Satratoxin G	trichothecene D	E	60S	PTC (A)	E?	dis	– // – ?
Roridin A	– // –	E	60S?	PTC (A)?	E?	?	– // – ?
Myrothecin A	– // –	E	60S?	PTC (A)?	E?	?	– // – ?
Verrucarin A/muconomycin A	trichothecene D, muconomycin	E	60S	PTC (A)	E	stab	– // –
Muconomycin B	– // –	E	60S?	PTC (A)?	E?	stab	– // –
Narciclasine	tetraheterocyclic alkaloid	B, A, E	60S	PTC (A)	E	stab	– // –
Isonarciclasine	– // –	B, A, E	60S?	PTC (A)?	E	stab	– // –
Lycorine	– // –	B, A, E	60S	PTC (A)	E	?	– // –
Pseudolycorine	– // –	B, A, E	60S	PTC (A)	E	?	– // –
Haemanthamine	– // –	A, E	60S	PTC (A)	E	stab	– // –
Haemanthidine	– // –	A, E	60S	PTC (A)	E	(stab)	– // –
Bulbispermine/hamayne	– // –	E	60S	PTC (A)	E	(stab)	– // –
Pretazettine	– // –	E	60S	PTC (A)	E	stab	– // –
Jonquailine	– // –	E?	60S?	PTC (A)?	E?	?	– // – ?
Crinamine	– // –	B, A, E	60S	PTC (A)	E	(stab)	– // –
Agelastatin A	heterocyclic alkaloid	E	60S	PTC (A)	E	?	– // –
Cephalotaxine	heterocyclic alkaloid, cephalotaxine group	(E)	60S	PTC (A)?	(E)	(stab)	– // – (weak)
Harringtonine	– // –	A, E	60S	PTC (A)	E	dis	– // –
Homoharringtonine/omacetaxine mepesuccinate	– // –	A, E	60S	PTC (A)	E	dis	– // –
Nagilactone C	diterpenoid	E	60S	PTC (A)	E	dis	– // –
Nagilactone E	– // –	E	60S?	PTC (A)?	E	?	– // – ?
Bruceantin	quassinoid	A, E	60S	PTC (A)	E	?	– // –
Grandilactone A	– // –	E	60S?	PTC (A)?	E	?	– // –
Brusatol	– // –	E	60S?	PTC (A)	E?	?	– // – ?
Holacanthone	– // –	E?	60S	PTC (A)	?	?	– // –
Baccharinol	– // –	E	60S?	PTC (A)?	E?	?	– // – ?
Ailanthinone	– // –	E	60S?	PTC (A)?	E?	?	– // – ?
Quassin	– // –	E?	60S?	PTC (A)?	E?	?	– // – ?
Sparsomycin	pyrimidone, sparsomycin group	B, A, E	60S	PTC (A, P)	E	stab	– // –
Deshydroxysparsomycin	– // –	E	60S?	PTC (A, P)?	E?	?	– // – ?
Octylsparsomycin	– // –	E	60S?	PTC (A, P)?	E?	?	– // – ?
Phenol-alanine sparsomycin	– // –	B, A, E	60S?	PTC (A, P)?	E?	?	– // – ?
MDL 20828	– // –	E	60S?	PTC (A, P)?	E?	?	– // – ?
Anthelmycin/hikizimycin	nucleoside, pyrimidone	B, A, E	60S	PTC (P)	E	(stab)	– // –
Blasticidin S	nucleoside, blasticidin group	B, A, E	60S	PTC (P)	E	?	– // –
Gougerotin	– // –	B, A, E	60S	PTC	E	dis	– // –
Bagougeramine A	– // –	B, A, E?	60S?	PTC?	E?	?	– // – ?
Amicetin	– // –	B, A, E	60S	PTC	E	stab	– // –
Bamicetin	– // –	B, A, E	60S	PTC	E	?	– // –
Mildiomycin	– // –	B, A, E	60S	PTC	E	?	– // –
Plicacetine	– // –	B, A, E	60S?	PTC?	E?	?	– // – (weak)
Arginomycin	– // –	B, A, E	60S?	PTC?	E?	?	– // – ?
Puromycin	aminoacyl-nucleoside	B, A, E	60S	A	E	dis	indices premature termination
A201A	– // –	B, A, E	60S	A	E		PTC inhibitor
Bactobolin	isocoumarin	B, A, E?	60S	PTC (P)	E	?	– // –
Actinobolin	– // –	B, A, E	60S	PTC	E	?	– // –
Amicoumacin A	– // –	B, A, E	40S	E-site	E	?	translocation inhibitor
Baciphelacin	– // –	B, A, E	?	?	I?	?	?
Oosponol	– // –	B, A, E?	?	?	?	?	?
AHR-1911	thiopseudourea	B, A, E	60S?	PTC?	E		PTC inhibitor
Tenuazonic acid	pyrroline	E	60S?	PTC (A, P)	?	stab	– // –
Bottromycin A2	cyclic peptide	B, A, E?	60S?	PTC?	E?	stab?	– // – ?
Griseoviridin	cyclodepsipeptide	B, A, E	60S	PTC	E	?	– // – ?
Cyclopiazonic acid	ergoline alkaloid	B, A, E	60S?	?	E	?	– // – ?
PF-06446846/PF846		B, A, E	60S	PET	E	?	alters path of nascent peptide, blocks translocation
PF-06378503/PF8503		E	60S?	PET?	E	?	– // – ?
Tetracenomycin X	aromatic polyketide, tetracenomycin group	B, A, E	60S	PET	E?	?	blocks PET, hinder peptide progression
Tetracycline Col-3	aromatic polyketide, tetracycline group	B, A, E	40S, 60S	PET and other	E?	?	?
Doxycycline	– // –	B, A, E	40S, 60S	PET and other	E?	?	?
Tigecycline	– // –	B, A, E	40S? 60S?	?	E	?	inhibits Aa-tRNA binding?
Minocycline	– // –	B, A, E	40S? 60S?	?	E?	?	?
Doxorubicin	aromatic polyketide, anthracycline group	E?	?	?	T	?	promotes stop-codon readthrough
Cycloheximide/naramycin A/actidion	glutarimide	E	60S	E-site	E	stab	translocation inhibitor
Naramycin B	– // –	E	60S?	E-site?	?	?	– // – ?
Acetoxycycloheximide	– // –	E	60S	E-site?	E	stab	– // – ?
Streptimidone	– // –	E	60S	E-site?	E	?	– // – ?
Streptovitacin A	– // –	E	60S	E-site?	E?	stab	– // – ?
Actiphenol	– // –	E	60S?	E-site?	E?	?	– // – ?
Lactimidomycin	– // –	E	60S	E-site	E	dis	– // –
Isomigrastatin	– // –	E	60S?	E-site?	E?	?	– // – ?
ECA-LTM	– // –	E	60S?	E-site?	E?	?	– // – ?
Streptoglutarimide H	– // –	B, A, E	60S?	E-site?	E?	?	– // – ?
Chlorolissoclimide	labdane diterpenoid, lissoclimide group	E	60S	E-site	E	stab	– // –
Lissoclimide C45	– // –	E	60S	E-site	E	stab	– // – ?
Haterumaimides Q	– // –	E	60S?	E-site?	E	stab	– // –
Phyllanthoside	glycoside	E	60S	E-site	E	dis	– // –
S3′-desacetyl phyllanthoside	– // –	E	60S?	E-site?	?	?	– // – ?
Pederin	polyketide, pederin group	E	60	E-site	E	stab	– // –
Psymberin/irciniastatin A	– // –	E	60S	E-site	E	?	– // –
Theopederin B	– // –	A, E	60S	E-site	E	?	– // –
Mycalamide B	– // –	B, A, E	60S	E-site	E	dis	– // –
Onnamide A	– // –	A? E	60S	E-site	E	?	– // –
Tedanolide	polyketide, tedanolide group	A? E	60S	E-site	E	?	– // –
13-deoxytedanolide	– // –	A, E	60S	E-site	E	?	– // –
Myriaporone 3/4	– // –	A, E	eEF2?	-	E	?	(see Table 3)
Emetine	pyridoisoquinoline alkaloid, emetine group	E	40S	E-site	E	stab	translocation inhibitor
Dehydroemetine	– // –	E	40S?	E-site?	E?	(stab)	– // –
Cephaeline	– // –	E	40S?	E-site?	E?	(stab)	– // –
Cryptopleurine	phenanthroquinolizidine alkaloid, emetine-like	E	40S, 60S?	E-site	E	?	– // –
Tylocrebrine	– // –	B? E	40S?	E-site?	E	?	– // –
Tubulosine	– // –	E	40S, 60S?	E-site?	E	?	– // –
Tylophorine/DCB-3500	– // –	B?, A, E	40S	E-site?	E	stab	– // –
Rac-cryptopleurin	– // –	E	40S?	E-site?	E	?	– // –
YXM-110	– // –	E	40S?	E-site?	E	?	– // –
Pactamycin	aminocyclopentitol, pactamycin group	B, A, E	40S	E-site	E (I?)	(dis)	– // –
de-6-MSA-pactamycin	– // –	B, A, E	40S?	E-site?	E (I?)	?	– // – ?
Zaluzanin C	sesquiterpene lactone	E	?	?	E	?	– // –
Hygromycin B	2-DOS aminoglycoside, noncanonical	B, A, E	40S?	DC	E (R?)	stab	– // –
G418/geneticin	2-DOS aminoglycoside, 4,6-disubstituted	B, E	40S, 60S	DC, PET	E, T	dis	induces miscoding, promotes stop-codon readthrough (HC inhibits translocation)
Gentamicins	– // –	B, E	40S, 60S	DC, PET	E, T	dis	– // –
Tobramycin	– // –	B, E?	40S, 60S?	DC	E, T	dis?	– // –
Amikacin	– // –	B, E	40S	DC	E, T	dis	– // –
Netilmicin	– // –	B, A, E?	40S?	DC?	E?	dis?	– // –
Paromomycin	2-DOS aminoglycoside, 4,5-disubstituted	B, E	40S, 60S	DC	E, T (R?)	dis	– // –
Lividomycin	– // –	B, A, E?	40S?	DC?	E	?	– // –
Neomycin	– // –	B, A, E?	40S?	DC?	E, T (R?)	?	– // –
TC007	– // –	B, A, E	40S, 60S	DC, PET	T	?	– // –
NB74	– // –	B? E	40S	DC	E, T	?	– // –
NB124	– // –	B? E	40S	DC?	E, T	?	– // –
NB156	– // –, NB74 derivative	B?, E	40S	DC	E, T	?	– // –
NB157	– // –, NB124 derivative	B?, E	40S	DC	E, T	?	– // –
Neamine	2-DOS aminoglycoside, 4-monosubstituted	B, E	60S?	DC	E, T	dis?	– // –
Apramycin	– // –	B, E	40S?	DC	E	?	– // – ?
Negamycin	negamycin group	B, A, E	40S	?	T	stab	– // –
3-Epi-deoxynegamycin	– // –	E	?	?	T	?	– // – ?
TCP-1109	– // –	E	40S		T	?	– // –
Ataluren/PTC124	oxadiazoles	E	60S?	A?	T?	?	– // – ?
Amlexanox	benzopyrans	E	?		T		– // –
RTC204		E	?	?	T	?	– // –
RTC219		E	?	?	T	?	– // –
GJ071		E	?	?	T	?	– // –
GJ072		E	?	?	T	?	– // –
GJ103		E	?	?	T	?	– // –
RTC13	thiazolidinone group	E	40S?	?	T	?	– // –
RTC14	– // –	E	?	?	T	?	– // –
BZ6	– // –	E	?	?	T	?	– // –
BZ16	– // –	E	?	?	T	?	– // –
CDX5-1	phthalimide	?	?	?	?	?	enhances induction of stop-codon readthrough by aminoglycosides
RP 49532A/girodazole/girolline		A, E	60S	E-site	T	?	inhibits peptide release
Sanguinamide B	cyclic peptide	B, A, E	40S, 60S	uS17, uL3, uL30, other	?	?	?
Daptomycin	cyclic lipopeptide	B, A?, E	40S	eS19	?	?	?
QL-XII-47/QL47	QL47 group	E	?	?	E?	?	?
YKL-04-085	– // –	E	?	?	E?	?	?
Mefloquine	quinoline	E*	60S	GAC	E	?	impedes accommodation of eEF1A, eEF2 (eIF5B?)
Edeine A		B, A, E	40S	E-site	I	?	affects binding or accommodation of Met-tRNA_i
MDMP		E	40S? 60S?	?	I	dis	prevents 60S joining
eIFsixty-4		E	60S	?	I	dis	precludes eIF6 binding to 60S

Notes: ^# B, bacteria; A, archaea; E, eukaryotes. * Denotes a narrower group of organisms (for example, fungi or protozoa).

^## PTC (A), A-site of the PTC; PTC (P), P-site of the PTC; other abbreviation as in the main text.

^### I, initiation; E, elongation; T, termination; R, recycling.

^#### stab, stabilizes polysomes; dis, disassembles polysomes, stab/dis, stabilizes or disassembles polysomes depending on the concentration or other conditions.

“?” means “presumably” (by analogy with a chemically similar compound, based on the information from other organisms or on controversial data); brackets, phenomenon is less pronounced than in other cases; HC, at high concentration.